1164 articles for thisTarget
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Article Title
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Cyclic mu-opioid receptor ligands containing multiple N-methylated amino acid residues.
Medical University of Lodz
Design and Synthesis of Enantiomerically Pure Decahydroquinoxalines as Potent and Selective¿-Opioid Receptor Agonists with Anti-Inflammatory Activity in Vivo.
Dr. August Wolff Gmbh & Co. Kg Arzneimittel
Benzylideneoxymorphone: A new lead for development of bifunctional mu/delta opioid receptor ligands.
West Virginia University School of Pharmacy
(+)-and (-)-Phenazocine enantiomers: Evaluation of their dual opioid agonist/s
University of Catania
Role of the sugar moiety on the opioid receptor binding and conformation of a series of enkephalin neoglycopeptides.
Instituto De Qu£Mica Avanzada De Catalu£A (Iqac-Csic)
Opioid Receptor Activity and Analgesic Potency of DPDPE Peptide Analogues Containing a Xylene Bridge.
D'Annunzio University of Chieti���Pescara
Design and Synthesis of Potent and Highly Selective Orexin 1 Receptor Antagonists with a Morphinan Skeleton and Their Pharmacologies.
University of Tsukuba
Discovery, structure-activity relationship studies, and anti-nociceptive effects of N-(1,2,3,4-tetrahydro-1-isoquinolinylmethyl)benzamides as novel opioid receptor agonists.
National Health Research Institutes
8-acenaphthen-1-yl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one derivatives as orphanin FQ receptor agonists.
F. Hoffmann-La Roche
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH
Jagiellonian University Medical College
Hydrazone Linker as a Useful Tool for Preparing Chimeric Peptide/Nonpeptide Bifunctional Compounds.
Mossakowski Medical Research Centre Polish Academy of Sciences
Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.
University of Kansas
A Cyclic Tetrapeptide ("Cyclodal") and Its Mirror-Image Isomer Are Both High-Affinityµ Opioid Receptor Antagonists.
Clinical Research Institute of Montreal
Structural determinants of diphenethylamines for interaction with the¿ opioid receptor: Synthesis, pharmacology and molecular modeling studies.
University of Innsbruck
The"Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules.
St. John'S University
[Dmt(1)]DALDA analogues modified with tyrosine analogues at position 1.
Nanjing Medical University
Effects of N-Substitutions on the Tetrahydroquinoline (THQ) Core of Mixed-Efficacyµ-Opioid Receptor (MOR)/d-Opioid Receptor (DOR) Ligands.
University of Michigan
Discovery of Potent and Selective Agonists ofd Opioid Receptor by Revisiting the"Message-Address" Concept.
Fudan University
Bifunctional Peptide-Based Opioid Agonist-Nociceptin Antagonist Ligands for Dual Treatment of Acute and Neuropathic Pain.
Vrije Universiteit Brussel
Evaluation of N-substituent structural variations in opioid receptor profile of LP1.
University of Catania
Synthesis and evaluation of novel opioid ligands with a C-homomorphinan skeleton.
Kitasato University
Discovery of small-molecule nonpeptide antagonists of nociceptin/orphanin FQ receptor: The studies of design, synthesis, and structure-activity relationships for (4-arylpiperidine substituted-methyl)-[bicyclic (hetero)cycloalkanobenzene] derivatives.
Pfizer
Dual Alleviation of Acute and Neuropathic Pain by Fused Opioid Agonist-Neurokinin 1 Antagonist Peptidomimetics.
Vrije Universiteit Brussel
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.
Jagiellonian University Medical College
Tetrahydroisoquinoline Phenols: Selective Estrogen Receptor Downregulator Antagonists with Oral Bioavailability in Rat.
Astrazeneca
Tactical Approaches to Interconverting GPCR Agonists and Antagonists.
University of Minnesota
Rapid Synthesis of Boc-2',6'-dimethyl-l-tyrosine and Derivatives and Incorporation into Opioid Peptidomimetics.
University of Michigan
Synthesis, biological evaluation and structural analysis of novel peripherally active morphiceptin analogs.
Medical University of Lodz
Synthesis of mixed MOR/KOR efficacy cyclic opioid peptide analogs with antinociceptive activity after systemic administration.
Medical University of Lodz
Multitarget opioid ligands in pain relief: New players in an old game.
University of Catania
Receptor binding profiles and quantitative structure-affinity relationships of some 5-substituted-N,N-diallyltryptamines.
The Alexander Shulgin Research Institute
Potentµ-Opioid Receptor Agonists from Cyclic Peptides Tyr-c[D-Lys-Xxx-Tyr-Gly]: Synthesis, Biological, and Structural Evaluation.
Torrey Pines Institute For Molecular Studies
Design synthesis and structure-activity relationship of 5-substituted (tetrahydronaphthalen-2yl)methyl with N-phenyl-N-(piperidin-2-yl)propionamide derivatives as opioid ligands.
University of Arizona
Synthesis, Biological Evaluation, and Utility of Fluorescent Ligands Targeting theµ-Opioid Receptor.
University of Nottingham
Further Optimization and Evaluation of Bioavailable, Mixed-Efficacyµ-Opioid Receptor (MOR) Agonists/d-Opioid Receptor (DOR) Antagonists: Balancing MOR and DOR Affinities.
University of Michigan
Structure-Activity Relationships of the Peptide Kappa Opioid Receptor Antagonist Zyklophin.
The University of Kansas
Conformationally restricted¿-opioid receptor agonists: Synthesis and pharmacological evaluation of diastereoisomeric and enantiomeric decahydroquinoxalines.
Mercachem
Design, synthesis, and evaluation of new endomorphin analogs with enhanced central antinociception after peripheral administration.
Lanzhou University
Identification of Substituted Naphthotriazolediones as Novel Tryptophan 2,3-Dioxygenase (TDO) Inhibitors through Structure-Based Virtual Screening.
National Health Research Institutes
Synthesis and biological evaluation of 2-alkyl-2-methoxymethyl-salvinorin ethers as selective¿-opioid receptor agonists.
Harvard Medical School
Design and synthesis of novel bivalent ligands (MOR and DOR) by conjugation of enkephalin analogues with 4-anilidopiperidine derivatives.
University of Arizona
Design, synthesis and biological evaluation of multifunctional ligands targeting opioid and bradykinin 2 receptors.
University of Arizona
Discovery of 5-substituted tetrahydronaphthalen-2yl-methyl with N-phenyl-N-(piperidin-4-yl)propionamide derivatives as potent opioid receptor ligands.
University of Arizona
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacologies: Part 5, novel pentacyclic propellane derivatives with a 6-amide side chain.
University of Tsukuba
Design, synthesis, pharmacological evaluation and molecular dynamics ofß-amino acids morphan-derivatives as novel ligands for opioid receptors.
Universidad De Salamanca
Naltrindole derivatives with fluorinated ethyl substituents on the 17-nitrogen asd opioid receptor inverse agonists.
Kitasato University
Design, synthesis, and structure-activity relationship of novel opioid¿ receptor selective agonists:a-iminoamide derivatives with an azabicyclo[2.2.2]octene skeleton.
Kitasato University
Synthesis and analgesic activity of alkylated, reduced and constrained oligoheterocyclic peptidomimetic analogs of Leu-enkephalin.
University of Monastir
Synthesis and Pharmacology of a Novel¿ Opioid Receptor (KOR) Agonist with a 1,3,5-Trioxazatriquinane Skeleton.
Kitasato University
Discovery of a Potent Analgesic NOP and Opioid Receptor Agonist: Cebranopadol.
Pharmacokinetics
Discovery of Spiro[cyclohexane-dihydropyrano[3,4-b]indole]-amines as Potent NOP and Opioid Receptor Agonists.
Pharmacokinetics
'Carba'-carfentanil (trans isomer): aµ opioid receptor (MOR) partial agonist with a distinct binding mode.
Clinical Research Institute of Montreal
Potency enhancement of the¿-opioid receptor antagonist probe ML140 through sulfonamide constraint utilizing a tetrahydroisoquinoline motif.
University of Kansas Specialized Chemistry Center
Parallel Synthesis of Hexahydrodiimidazodiazepines Heterocyclic Peptidomimetics and Their in Vitro and in Vivo Activities atµ (MOR),d (DOR), and¿ (KOR) Opioid Receptors.
Torrey Pines Institute For Molecular Studies
Synthesis of mixed opioid affinity cyclic endomorphin-2 analogues with fluorinated phenylalanines.
Medical University of Lodz
C7ß-methyl analogues of the orvinols: the discovery of kappa opioid antagonists with nociceptin/orphanin FQ peptide (NOP) receptor partial agonism and low, or zero, efficacy at mu opioid receptors.
University of Bath
Discovery, synthesis, and molecular pharmacology of selective positive allosteric modulators of thed-opioid receptor.
Bristol-Myers Squibb
CNS drug design: balancing physicochemical properties for optimal brain exposure.
Eli Lilly
Probes for narcotic receptor mediated phenomena 49. N-substituted rac-cis-4a-arylalkyl-1,2,3,4,4a,9a-hexahydrobenzofuro[2,3-c]pyridin-6-ols.
National Institute On Drug Abuse
Synthesis and biological evaluations of novel endomorphin analogues containinga-hydroxy-ß-phenylalanine (AHPBA) displaying mixedµ/d opioid receptor agonist andd opioid receptor antagonist activities.
Zhejiang University
Synthesis and biological evaluation of compact, conformationally constrained bifunctional opioid agonist - neurokinin-1 antagonist peptidomimetics.
Vrije Universiteit Brussel
Design, syntheses, and pharmacological characterization of 17-cyclopropylmethyl-3,14ß-dihydroxy-4,5a-epoxy-6a-(isoquinoline-3'-carboxamido)morphinan analogues as opioid receptor ligands.
Virginia Commonwealth University
trans-(3S,4S)-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part I: prime site exploration using an amino linker.
Novartis Pharma
trans-3,4-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part II: prime site exploration using an oxygen linker.
Novartis Pharma
Novel fluoroalkyl derivatives of selective kappa opioid receptor antagonist JDTic: Design, synthesis, pharmacology and molecular modeling studies.
University of Caen Normandie
Optimisation of in silico derived 2-aminobenzimidazole hits as unprecedented selective kappa opioid receptor agonists.
Dr. Reddy'S Laboratories
Methoxyflavones from Stachys glutinosa with binding affinity to opioid receptors: in silico, in vitro, and in vivo studies.
National Research Council
A selective small molecule NOP (ORL-1 receptor) partial agonist for the treatment of anxiety.
West Chester University
Design, synthesis, and biological evaluation of (3R)-1,2,3,4-tetrahydro-7-hydroxy-N-[(1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl]-3-isoquinolinecarboxamide (JDTic) analogues: in vitro pharmacology and ADME profile.
Research Triangle Institute
Discovery, structure-activity relationship studies, and anti-nociceptive effects of 1-phenyl-3,6,6-trimethyl-1,5,6,7-tetrahydro-4H-indazol-4-one as novel opioid receptor agonists.
National Health Research Institutes
Synthesis and pharmacological evaluation of 5-pyrrolidinylquinoxalines as a novel class of peripherally restricted¿-opioid receptor agonists.
Westf£Lische Wilhelms-Universit£T M£Nster
Antinociceptive and antidepressant-like action of endomorphin-2 analogs with proline surrogates in position 2.
Medical University of Lodz
Pyrrolo- and pyridomorphinans: non-selective opioid antagonists and delta opioid agonists/mu opioid partial agonists.
University of Bath
Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).
Glaxosmithkline
Cyclic side-chain-linked opioid analogs utilizing cis- and trans-4-aminocyclohexyl-D-alanine.
TBA
Nonpeptide small molecule agonist and antagonist original leads for neuropeptide FF1 and FF2 receptors.
The University of Mississippi
Synthesis of a novel universal opioid receptor agonist with the 1,3,5-trioxazatriquinane skeleton and its pharmacologies.
Kitasato University
Novel cyclic biphalin analogue with improved antinociceptive properties.
D'Annunzio University of Chieti���Pescara
Michael acceptor approach to the design of new salvinorin A-based high affinity ligands for the kappa-opioid receptor.
University of Mississippi
Combination of cyclohexane and piperazine based¿-opioid receptor agonists: Synthesis and pharmacological evaluation of trans,trans-configured perhydroquinoxalines.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Synthesis and evaluation of three structurally related¹8F-labeled orvinols of different intrinsic activities: 6-O-[¹8F]fluoroethyl-diprenorphine ([¹8F]FDPN), 6-O-[¹8F]fluoroethyl-buprenorphine ([¹8F]FBPN), and 6-O-[¹8F]fluoroethyl-phenethyl-orvinol ([¹8F]FPEO).
University of Oslo
4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.
Astrazeneca
Design and synthesis of quinolinopropellane derivatives with selectived opioid receptor agonism.
University of Tsukuba
Selectively promiscuous opioid ligands: discovery of high affinity/low efficacy opioid ligands with substantial nociceptin opioid peptide receptor affinity.
University of Bath
Discovery of a neuroprotective chemical, (S)-N-(3-(3,6-dibromo-9H-carbazol-9-yl)-2-fluoropropyl)-6-methoxypyridin-2-amine [(-)-P7C3-S243], with improved druglike properties.
University of Texas Southwestern Medical Center
Designing bifunctional NOP receptor-mu opioid receptor ligands from NOP-receptor selective scaffolds. Part II.
Astraea Therapeutics
Novel delta opioid receptor agonists with oxazatricyclodecane structure.
Kitasato University
In Vitro Membrane Permeation Studies and in Vivo Antinociception of Glycosylated Dmt
Vrije Universiteit Brussel
Endomorphin analogues with mixedµ-opioid (MOP) receptor agonism/d-opioid (DOP) receptor antagonism and lackingß-arrestin2 recruitment activity.
Nanjing Medical University
[Dmt(1)]DALDA analogues with enhancedµ opioid agonist potency and with a mixedµ/¿ opioid activity profile.
Nanjing Medical University
Discovery of a novel series of orally active nociceptin/orphanin FQ (NOP) receptor antagonists based on a dihydrospiro(piperidine-4,7'-thieno[2,3-c]pyran) scaffold.
Eli Lilly
Development of a bioavailableµ opioid receptor (MOPr) agonist,d opioid receptor (DOPr) antagonist peptide that evokes antinociception without development of acute tolerance.
University of Michigan
3D-QSAR comparative molecular field analysis on opioid receptor antagonists: pooling data from different studies.
University of Medicine & Dentistry of New Jersey-Robert Wood Johnson Medical School (Umdnj-Rwjms)
Imidazole-derived agonists for the neurotensin 1 receptor.
Sanford-Burnham Medical Research Institute
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 9: Synthesis, characterization and molecular modeling of pyridinyl isosteres of N-BPE-8-CAC (1), a high affinity ligand for opioid receptors.
Rensselaer Polytechnic Institute
Design, synthesis, and pharmacological characterization of novel endomorphin-1 analogues as extremely potentµ-opioid agonists.
Lanzhou University
Biological active analogues of the opioid peptide biphalin: mixeda/ß(3)-peptides.
D'Annunzio University of Chieti���Pescara
Opioid peptidomimetics: leads for the design of bioavailable mixed efficacyµ opioid receptor (MOR) agonist/d opioid receptor (DOR) antagonist ligands.
University of Michigan
Systematic exploration of dual-acting modulators from a combined medicinal chemistry and biology perspective.
Astrazeneca
The effect of 17-N substituents on the activity of the opioid¿ receptor in nalfurafine derivatives.
Kitasato University
Highly potent and selective zwitterionic agonists of the delta-opioid receptor. Part 1.
Pfizer
Development of LC-MS/MS-based receptor occupancy tracers and positron emission tomography radioligands for the nociceptin/orphanin FQ (NOP) receptor.
Eli Lilly
Structure-activity studies on the nociceptin/orphanin FQ receptor antagonist 1-benzyl-N-{3-[spiroisobenzofuran-1(3H),4'-piperidin-1-yl]propyl} pyrrolidine-2-carboxamide.
University of Ferrara
Further studies at neuropeptide s position 5: discovery of novel neuropeptide S receptor antagonists.
National Institute of Neuroscienc
Assessment of substitution in the second pharmacophore of Dmt-Tic analogues.
University of Naples
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 8. High affinity ligands for opioid receptors in the picomolar Ki range: oxygenated N-(2-[1,1'-biphenyl]-4-ylethyl) analogues of 8-CAC.
Rensselaer Polytechnic Institute
Synthesis of novel triplet drugs with 1,3,5-trioxazatriquinane skeletons and their pharmacologies. 3: synthesis of novel triplet drugs with the bis(epoxymethano) or bis(dimethylepoxymethano) structure (double-capped triplet).
Kitasato University
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacologies: part 3, novel propellane derivatives with pentacyclic skeletons.
Kitasato University
Essential structure of opioid¿ receptor agonist nalfurafine for binding to the¿ receptor 3: synthesis of decahydro(iminoethano)phenanthrene derivatives with an oxygen functionality at the 3-position and their pharmacologies.
Kitasato University
As(1) receptor pharmacophore derived from a series of N-substituted 4-azahexacyclo[5.4.1.0(2,6).0(3,10).0(5,9).0(8,11)]dodecan-3-ols (AHDs).
The University of Sydney
Novel TIPP (H-Tyr-Tic-Phe-Phe-OH) analogues displaying a wide range of efficacies at thed opioid receptor. Discovery of two highly potent and selectived opioid agonists.
Clinical Research Institute of Montreal
Discovery and pharmacological evaluation of a diphenethylamine derivative (HS665), a highly potent and selective¿ opioid receptor agonist.
University of Innsbruck
Design, synthesis, and biological evaluation of 17-cyclopropylmethyl-3,14ß-dihydroxy-4,5a-epoxy-6ß-[(4'-pyridyl)carboxamido]morphinan derivatives as peripheral selectiveµ opioid receptor Agents.
Virginia Commonwealth University
Variation of the net charge, lipophilicity, and side chain flexibility in Dmt(1)-DALDA: Effect on Opioid Activity and Biodistribution.
Vrije Universiteit Brussel
Fumaroylamino-4,5-epoxymorphinans and related opioids with irreversibleµ opioid receptor antagonist effects.
University of Bristol
14-Alkoxy- and 14-acyloxypyridomorphinans:µ agonist/d antagonist opioid analgesics with diminished tolerance and dependence side effects.
Southern Research Institute
Opioid activity profiles of oversimplified peptides lacking in the protonable N-terminus.
University of Bologna
The effect of Pro(2) modifications on the structural and pharmacological properties of endomorphin-2.
Biological Research Center of The Hungarian Academy of Sciences
cis-4-amino-L-proline residue as a scaffold for the synthesis of cyclic and linear endomorphin-2 analogues: part 2.
D'Annunzio University of Chieti���Pescara
Synthesis and evaluation of aryl-naloxamide opiate analgesics targeting truncated exon 11-associatedµ opioid receptor (MOR-1) splice variants.
Memorial Sloan-Kettering Cancer Center
A new class of highly potent and selective endomorphin-1 analogues containinga-methylene-ß-aminopropanoic acids (map).
Lanzhou University
Synthesis, biological activity and structure-activity relationship of endomorphin-1/substance P derivatives.
The University of Queensland
An efficient synthesis of 3-OBn-6ß,14-epoxy-bridged opiates from naltrexone and identification of a related dual MOR inverse agonist/KOR agonist.
University of New England
Identification of a duald OR antagonist/µ OR agonist as a potential therapeutic for diarrhea-predominant Irritable Bowel Syndrome (IBS-d).
Janssen Research and Development
Synthesis and biological evaluation of an orally active glycosylated endomorphin-1.
The University of Queensland
Superpotent [Dmt¹] dermorphin tetrapeptides containing the 4-aminotetrahydro-2-benzazepin-3-one scaffold with mixedµ/d opioid receptor agonistic properties.
Vrije Universiteit Brussel
Tuned-Affinity Bivalent Ligands for the Characterization of Opioid Receptor Heteromers.
TBA
Synthesis of quinolinomorphinan derivatives as highly selectived opioid receptor ligands.
Kitasato University
Discovery of 1-(ß-amino substituted-ß-alanyl)-N,N-dimethylindoline-2-carboxamides as novel nonpeptide antagonists of nociceptin/orphanin FQ receptor: efficient design, synthesis, and structure-activity relationship studies.
Pfizer
Essential structure of opioid¿ receptor agonist nalfurafine for binding to the¿ receptor 2: synthesis of decahydro(iminoethano)phenanthrene derivatives and their pharmacologies.
Kitasato University
Deconstructing 14-phenylpropyloxymetopon: minimal requirements for binding to mu opioid receptors.
University of Maryland
Synthesis, binding affinity, and functional in vitro activity of 3-benzylaminomorphinan and 3-benzylaminomorphine ligands at opioid receptors.
Harvard Medical School
The cis-4-amino-L-proline residue as a scaffold for the synthesis of cyclic and linear endomorphin-2 analogues.
D'Annunzio University of Chieti���Pescara
NOpiates: Novel Dual Action Neuronal Nitric Oxide Synthase Inhibitors with µ-Opioid Agonist Activity.
TBA
Discovery of a novel melanin concentrating hormone receptor 1 (MCHR1) antagonist with reduced hERG inhibition.
Amgen
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacology. Part 2: Propellane derivatives with an amide side chain.
Kitasato University
Design and synthesis of novel opioid ligands with an azabicyclo[2.2.2]octane skeleton and their pharmacologies.
Kitasato University
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacology: part 1.
Kitasato University
Generation of novel radiolabeled opiates through site-selective iodination.
Memorial Sloan-Kettering Cancer Center
Syntheses of 2-amino and 2-halothiazole derivatives as high-affinity metabotropic glutamate receptor subtype 5 ligands and potential radioligands for in vivo imaging.
National Institute of Mental Health
Opioid bifunctional ligands from morphine and the opioid pharmacophore Dmt-Tic.
University of Cagliari
Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: design, synthesis, and structure-activity rela
Pfizer
Development of potent µ and d opioid agonists with high lipophilicity.
University of Arizona
Discovery of a novel 5-HT(3) antagonist/5-HT(1A) agonist 3-amino-5,6,7,8-tetrahydro-2-{4-[4-(quinolin-2-yl)piperazin-1-yl]butyl}quinazolin-4(3H)-one (TZB-30878) as an orally bioavailable agent for irritable bowel syndrome.
Aska Pharmaceutical
Morphinans and isoquinolines: acetylcholinesterase inhibition, pharmacophore modeling, and interaction with opioid receptors.
University of Innsbruck and Center For Molecular Biosciences Innsbruck-Cmbi
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
H. Lundbeck
Design and synthesis of trivalent ligands targeting opioid, cholecystokinin, and melanocortin receptors for the treatment of pain.
University of Arizona
Analogues of (3R)-7-hydroxy-N-[(1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl)-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide (JDTic). Synthesis and in vitro and in vivo opioid receptor antagonist activity.
Research Triangle Institute
Conformationally constrained kappa receptor agonists: stereoselective synthesis and pharmacological evaluation of 6,8-diazabicyclo[3.2.2]nonane derivatives.
Wilhelms-Universit£T M£Nster
"Carba"-analogues of fentanyl are opioid receptor agonists.
Clinical Research Institute of Montreal
Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine.
Hunter College and The Graduate Center of The City University of New York
Drug design and synthesis of a novel kappa opioid receptor agonist with an oxabicyclo[2.2.2]octane skeleton and its pharmacology.
Kitasato University
Synthesis and pharmacological evaluation of 6-naltrexamine analogs for alcohol cessation.
Human Biomolecular Research Institute
mu-Opioid/5-HT4 dual pharmacologically active agents-efforts towards an effective opioid analgesic with less GI and respiratory side effects (Part I).
Sepracor
Synthesis and opioid receptor activity of indolopropellanes.
Chinese Academy of Sciences
Improving metabolic stability by glycosylation: bifunctional peptide derivatives that are opioid receptor agonists and neurokinin 1 receptor antagonists.
University of Arizona
Design and synthesis of novel delta opioid receptor agonists and their pharmacologies.
Kitasato University
Synthesis of a new opioid ligand having the oxabicyclo[3.2.1]octane skeleton using a new rearrangement reaction.
Kitasato University
Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208.
Adolor
Syntheses of novel high affinity ligands for opioid receptors.
Rensselaer Polytechnic Institute
14-O-Heterocyclic-substituted naltrexone derivatives as non-peptide mu opioid receptor selective antagonists: design, synthesis, and biological studies.
Virginia Commonwealth University
Synthesis and biological evaluation of C-12 triazole and oxadiazole analogs of salvinorin A.
Harvard Medical School
Ligand binding to nucleic acids and proteins: Does selectivity increase with strength?
Universit£T Des Saarlandes
14 beta-O-cinnamoylnaltrexone and related dihydrocodeinones are mu opioid receptor partial agonists with predominant antagonist activity.
University of Bath
Synthesis of N-isobutylnoroxymorphone from naltrexone by a selective cyclopropane ring opening reaction.
Kitasato University
Novel non-peptide nociceptin/orphanin FQ receptor agonist, 1-[1-(1-Methylcyclooctyl)-4-piperidinyl]-2-[(3R)-3-piperidinyl]-1H-benzimidazole: design, synthesis, and structure-activity relationship of oral receptor occupancy in the brain for orally potent antianxiety drug.
Pfizer
Design, synthesis, and biological evaluation of 6alpha- and 6beta-N-heterocyclic substituted naltrexamine derivatives as mu opioid receptor selective antagonists.
Virginia Commonwealth University
Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamide (ADL5859).
Adolor
Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.
Rensselaer Polytechnic Institute
Synthesis of a novel 6,14-epoxymorphinan derivative and its pharmacology.
Kitasato University
Structure-antitussive activity relationships of naltrindole derivatives. Identification of novel and potent antitussive agents.
Toray Industries
Conformation-opioid activity relationships of bicyclic guanidines from 3D similarity analysis.
Torrey Pines Institute For Molecular Studies
High specific activity tritium-labeled N-(2-methoxybenzyl)-2,5-dimethoxy-4-iodophenethylamine (INBMeO): a high-affinity 5-HT2A receptor-selective agonist radioligand.
Purdue University
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 6: Opioid receptor binding properties of cyclic variants of 8-carboxamidocyclazocine.
Rensselaer Polytechnic Institute
Syntheses of 4,6'-epoxymorphinan derivatives and their pharmacologies.
Kitasato University
Use of receptor chimeras to identify small molecules with high affinity for the dynorphin A binding domain of the kappa opioid receptor.
Adolor
Herkinorin analogues with differential beta-arrestin-2 interactions.
The University of Iowa
Blood-brain barrier penetration by two dermorphin tetrapeptide analogues: role of lipophilicity vs structural flexibility.
Vrije Universiteit Brussel
Synthesis of a potent and selective (18)F-labeled delta-opioid receptor antagonist derived from the Dmt-Tic pharmacophore for positron emission tomography imaging.
Stanford University School of Medicine
Synthesis and pharmacological evaluation of bicyclic SNC80 analogues with separated benzhydryl moiety.
Westf£Lische Wilhelms-Universit£T
Role of benzimidazole (Bid) in the delta-opioid agonist pseudopeptide H-Dmt-Tic-NH-CH(2)-Bid (UFP-502).
University of Ferrara
Novel coumarin glycoside and phenethyl vanillate from Notopterygium forbesii and their binding affinities for opioid and dopamine receptors.
Harvard Medical School
Standard protecting groups create potent and selective kappa opioids: salvinorin B alkoxymethyl ethers.
Mclean Hospital
The influence of esters and carboxylic acids as the N-substituent of opioids. Part 1: Benzomorphans.
University of Maryland
Identification of novel benzimidazole series of potent and selective ORL1 antagonists.
Banyu Tsukuba Research Institute
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.
Abbott Laboratories
Toward a structure-based model of salvinorin A recognition of the kappa-opioid receptor.
University of Minnesota
Endomorphin-2 with a beta-turn backbone constraint retains the potent micro-opioid receptor agonist properties.
Biological Research Center of The Hungarian Academy of Sciences
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. 5. Opioid receptor binding properties of N-((4'-phenyl)-phenethyl) analogues of 8-CAC.
Institute
3-Hydroxy-4-methoxyindolomorphinans as delta opioid selective ligands.
University of Maryland
Structure activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 2.
Eli Lilly
Cinnamoyl derivatives of 7alpha-aminomethyl-6,14-endo-ethanotetrahydrothebaine and 7alpha-aminomethyl-6,14-endo-ethanotetrahydrooripavine and related opioid ligands.
University of Bath
Synthesis of bridged piperazines with sigma receptor affinity.
Institut F£R Pharmazeutische Und Medizinische Chemie
Differential receptor binding characteristics of consecutive phenylalanines in micro-opioid specific peptide ligand endomorphin-2.
Kyushu University
Synthetic studies of neoclerodane diterpenes from Salvia divinorum: preparation and opioid receptor activity of salvinicin analogues.
The University of Iowa
Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1.
Schering-Plough Research Institute
High-affinity carbamate analogues of morphinan at opioid receptors.
Harvard Medical School
Novel piperazines: potent melanocortin-4 receptor antagonists with anxiolytic-like activity.
Taisho Pharmaceutical
Pharmacological properties of bivalent ligands containing butorphan linked to nalbuphine, naltrexone, and naloxone at mu, delta, and kappa opioid receptors.
Harvard Medical School
Indium-labeled macrocyclic conjugates of naltrindole: high-affinity radioligands for in vivo studies of peripheral delta opioid receptors.
University of Missouri-Columbia
Effects of substitution on the pyrrole N atom in derivatives of tetrahydronaltrindole, tetrahydrooxymorphindole, and a related 4,5-epoxyphenylpyrrolomorphinan.
University of Bath
Elucidation of the bioactive conformation of the N-substituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine class of mu-opioid receptor antagonists.
Adolor
Synthesis and pharmacological evaluation of novel octahydro-1H-pyrido[1,2-a]pyrazine as mu-opioid receptor antagonists.
Adolor
Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effects of changes to the chain linking of the C14-amino group to the aryl ring.
University of Bristol
Synthesis and receptor binding properties of chimeric peptides containing a mu-opioid receptor ligand and nociceptin/orphanin FQ receptor ligand Ac-RYYRIK-amide.
Tohoku Pharmaceutical University
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. 4. Opioid receptor binding properties of 8-[N-(4'-phenyl)-phenethyl)carboxamido] analogues of cyclazocine and ethylketocycalzocine.
Rensselaer Polytechnic Institute
Effect of lysine at C-terminus of the Dmt-Tic opioid pharmacophore.
University of Cagliari
Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effect of substitution in the aromatic ring of cinnamoylaminomorphinones and codeinones.
University of Bristol
4-Substituted-8-(1-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-one as a novel class of highly selective GlyT1 inhibitors with superior pharmacological and pharmacokinetic parameters.
F. Hoffmann-La Roche
Opiate receptor binding properties of morphine-, dihydromorphine-, and codeine 6-O-sulfate ester congeners.
University of Kentucky
Discovery of novel triazole-based opioid receptor antagonists.
University of Medicine and Dentistry of New Jersey and Umdnj Informatics Institute
New 2',6'-dimethyl-L-tyrosine (Dmt) opioid peptidomimetics based on the Aba-Gly scaffold. Development of unique mu-opioid receptor ligands.
Vrije Universiteit Brussels
Design and synthesis of novel hydrazide-linked bifunctional peptides as delta/mu opioid receptor agonists and CCK-1/CCK-2 receptor antagonists.
University of Arizona
Synthesis and preliminary in vitro investigation of bivalent ligands containing homo- and heterodimeric pharmacophores at mu, delta, and kappa opioid receptors.
Harvard Medical School
Novel CCR1 antagonists with oral activity in the mouse collagen induced arthritis.
Novartis Institutes For Biomedical Research
2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
University of Urbino
Synthesis and biological evaluation of 14-alkoxymorphinans. 22.(1) Influence of the 14-alkoxy group and the substitution in position 5 in 14-alkoxymorphinan-6-ones on in vitro and in vivo activities.
Sapienza University of Rome
Synthesis and biological evaluation of meperidine analogues at monoamine transporters.
University of New Orleans
Effect of a 6-cyano substituent in 14-oxygenated N-methylmorphinans on opioid receptor binding and antinociceptive potency.
University of Innsbruck
Synthesis and evaluation of the affinity toward mu-opioid receptors of atypical, lipophilic ligands based on the sequence c[-Tyr-Pro-Trp-Phe-Gly-].
University of Bologna
Identification of a new scaffold for opioid receptor antagonism based on the 2-amino-1,1-dimethyl-7-hydroxytetralin pharmacophore.
University of Bath
Synthesis and opioid receptor binding properties of a highly potent 4-hydroxy analogue of naltrexone.
Rensselaer Polytechnic Institute
18F-labeled sufentanil for PET-imaging of mu-opioid receptors.
Technische Universit£T M£Nchen
Synthesis and in vitro biological evaluation of a carbon glycoside analogue of morphine-6-glucuronide.
Human Biomolecular Research Institute
Synthesis and biological evaluation of new biphalin analogues with non-hydrazine linkers.
University of Arizona
1,3-Dihydro-2,1,3-benzothiadiazol-2,2-diones and 3,4-dihydro-1H-2,1,3-benzothidiazin-2,2-diones as ligands for the NOP receptor.
Purdue Pharma
2-aminothiazole-derived opioids. Bioisosteric replacement of phenols.
Harvard Medical School
Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone].
Southern Research Institute
Importance of phenolic address groups in opioid kappa receptor selective antagonists.
Research Triangle Institute
Synthesis and biological evaluation of 14-alkoxymorphinans. 18. N-substituted 14-phenylpropyloxymorphinan-6-ones with unanticipated agonist properties: extending the scope of common structure-activity relationships.
University of Innsbruck
14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles.
University of Bath
2,6-Dimethyltyrosine analogues of a stereodiversified ligand library: highly potent, selective, non-peptidic mu opioid receptor agonists.
Harvard University
3-(alphaR)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-hydroxybenzyl)-N-alkyl-N-arylbenzamides: potent, non-peptidic agonists of both the micro and delta opioid receptors.
Glaxosmithkline
Guanidino N-substituted and N,N-disubstituted derivatives of the kappa-opioid antagonist GNTI.
University of Bath
Design and synthesis of novel dimeric morphinan ligands for kappa and micro opioid receptors.
Harvard Medical School
Peptide science: exploring the use of chemical principles and interdisciplinary collaboration for understanding life processes.
University of Arizona
The role of the side chain in determining relative delta- and kappa-affinity in C5'-substituted analogues of naltrindole.
University of Bath
Synthesis and biological evaluation of 14-alkoxymorphinans. 20. 14-phenylpropoxymetopon: an extremely powerful analgesic.
University of Innsbruck
Synthesis, biological evaluation, and receptor docking simulations of 2-[(acylamino)ethyl]-1,4-benzodiazepines as kappa-opioid receptor agonists endowed with antinociceptive and antiamnesic activity.
University of Siena
Opioid binding and in vitro profiles of a series of 4-hdroxy-3-methoxyindolomorphinans. Transformation of a delta-selective ligand into a high affinity kappa-selective ligand by introduction of a 5,14-substituted bridge.
University of Bath
Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist.
Research Triangle Institute
Synthesis and biological evaluation of 18-methoxycoronaridine congeners. Potential antiaddiction agents.
University of Vermont
Structure-activity relationships of dynorphin a analogues modified in the address sequence.
University of California
2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy.
Research Triangle Institute
The power of visual imagery in drug design. Isopavines as a new class of morphinomimetics and their human opioid receptor binding activity.
University of Montreal
Design, synthesis, and evaluation of opioid analogues with non-peptidic beta-turn scaffold: enkephalin and endomorphin mimetics.
TBA
Evaluation of the Dmt-Tic pharmacophore: conversion of a potent delta-opioid receptor antagonist into a potent delta agonist and ligands with mixed properties.
University of Cagliary
Potent delta-opioid receptor agonists containing the Dmt-Tic pharmacophore.
University of Cagliari
Synthesis and biological evaluation of 14-alkoxymorphinans. 17. Highly delta opioid receptor selective 14-alkoxy-substituted indolo- and benzofuromorphinans.
University of Innsbruck
Probing opioid receptor interactions with azacycloalkane amino acids. Synthesis of a potent and selective ORL1 antagonist.
University of Montreal
4'-Arylpyrrolomorphinans: effect of a pyrrolo-N-benzyl substituent in enhancing delta-opioid antagonist activity.
University of Bristol
Discovery of an opioid kappa receptor selective pure antagonist from a library of N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphans.
Research Triangle Institute
Naphthalene dicarboxaldehyde as an electrophilic fluorogenic moiety for affinity labeling: application to opioid receptor affinity labels with greatly improved fluorogenic properties.
University of Minnesota
Endomorphin-1 analogues containing beta-proline are mu-opioid receptor agonists and display enhanced enzymatic hydrolysis resistance.
University of Bologna
Effect of N-alkyl and N-alkenyl substituents in noroxymorphindole, 17-substituted-6,7-dehydro-4,5alpha-epoxy-3,14-dihydroxy-6,7:2',3'-indolomorphinans, on opioid receptor affinity, selectivity, and efficacy.
National Institute of Diabetes and Digestive and Kidney Diseases
Covalently induced activation of the delta opioid receptor by a fluorogenic affinity label, 7'-(phthalaldehydecarboxamido)naltrindole (PNTI).
University of Minnesota
Factors influencing agonist potency and selectivity for the opioid delta receptor are revealed in structure-activity relationship studies of the 4-[(N-substituted-4-piperidinyl)arylamino]-N,N-diethylbenzamides.
Research Triangle Institute
Investigation of the selectivity of oxymorphone- and naltrexone-derived ligands via site-directed mutagenesis of opioid receptors: exploring the"address" recognition locus.
University of Minnesota
Pseudoproline-containing analogues of morphiceptin and endomorphin-2: evidence for a cis Tyr-Pro amide bond in the bioactive conformation.
University of Lausanne
From hit to lead. Combining two complementary methods for focused library design. Application to mu opiate ligands.
Universities of Lille
[2',6'-Dimethyltyrosine]dynorphin A(1-11)-NH2 analogues lacking an N-terminal amino group: potent and selective kappa opioid antagonists.
Clinical Research Institute of Montreal
Methylated analogues of methyl (R)-4-(3,4-dichlorophenylacetyl)- 3-(pyrrolidin-1-ylmethyl)piperazine-1-carboxylate (GR-89,696) as highly potent kappa-receptor agonists: stereoselective synthesis, opioid-receptor affinity, receptor selectivity, and functional studies.
Pharmazeutisches Institut Der Universit£T Freiburg
Identification of the first trans-(3R,4R)- dimethyl-4-(3-hydroxyphenyl)piperidine derivative to possess highly potent and selective opioid kappa receptor antagonist activity.
Research Triangle Institute
Transformation of a kappa-opioid receptor antagonist to a kappa-agonist by transfer of a guanidinium group from the 5'- to 6'-position of naltrindole.
University of Minnesota
Structural determinants of opioid activity in the orvinols and related structures: ethers of orvinol and isoorvinol.
University of Bristol
Binding of norbinaltorphimine (norBNI) congeners to wild-type and mutant mu and kappa opioid receptors: molecular recognition loci for the pharmacophore and address components of kappa antagonists.
University of Minnesota
High-affinity, non-peptide agonists for the ORL1 (orphanin FQ/nociceptin) receptor.
F. Hoffmann-La Roche
Novel ligands lacking a positive charge for the delta- and mu-opioid receptors.
Clinical Research Institute of Montr£Al
Molecular docking reveals a novel binding site model for fentanyl at the mu-opioid receptor.
University of Minnesota
Structural determinants of efficacy for kappa opioid receptors in the orvinol series: 7,7-spiro analogues of buprenorphine.
University of Bristol
Selective protection and functionalization of morphine: synthesis and opioid receptor binding properties of 3-amino-3-desoxymorphine derivatives.
Rensselaer Polytechnic Institute
3-Deoxyclocinnamox: the first high-affinity, nonpeptide mu-opioid antagonist lacking a phenolic hydroxyl group.
University of Bristol
Nonpeptide analogues of dynorphin A(1-8): design, synthesis, and pharmacological evaluation of kappa-selective agonists.
University of Catania
[Pro(3)]Dyn A(1-11)-NH(2): a dynorphin analogue with high selectivity for the kappa opioid receptor.
University of California
Enkephalin glycopeptide analogues produce analgesia with reduced dependence liability.
University of Northern Colorado
Reporter affinity labels: an o-phthalaldehyde derivative of beta-naltrexamine as a fluorogenic ligand for opioid receptors.
University of Minnesota
Synthesis and opioid receptor affinity of morphinan and benzomorphan derivatives: mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine dependence.
Harvard Medical School
delta Opioid affinity and selectivity of 4-hydroxy-3-methoxyindolomorphinan analogues related to naltrindole.
National Institute of Diabetes
Probes for narcotic receptor mediated phenomena. 26. Synthesis and biological evaluation of diarylmethylpiperazines and diarylmethylpiperidines as novel, nonpeptidic delta opioid receptor ligands.
National Institute of Diabetes and Digestive and Kidney Diseases
Design, synthesis, and evaluation of Phe-Gly mimetics: heterocyclic building blocks for pseudopeptides.
Uppsala University
Mixture-based synthetic combinatorial libraries.
Torrey Pines Institute For Molecular Studies
Synthesis, opioid receptor binding, and biological activities of naltrexone-derived pyrido- and pyrimidomorphinans.
Southern Research Institute
Identification of an opioid kappa receptor subtype-selective N-substituent for (+)-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine.
Research Triangle Institute
Side chain methyl substitution in the delta-opioid receptor antagonist TIPP has an important effect on the activity profile.
Vrije Universiteit Brussel
Mutational evidence for a common kappa antagonist binding pocket in the wild-type kappa and mutant mu[K303E] opioid receptors.
University of Minnesota
Modified ibogaine fragments: synthesis and preliminary pharmacological characterization of 3-ethyl-5-phenyl-1,2,3,4,5, 6-hexahydroazepino[4,5-b]benzothiophenes.
University of Minnesota
3-Alkyl ethers of clocinnamox: delayed long-term mu-antagonists with variable mu efficacy.
University of Bristol
Synthesis, opioid receptor binding, and bioassay of naltrindole analogues substituted in the indolic benzene moiety.
Southern Research Institute
Synthesis and biological activity of a novel methylamine-bridged enkephalin analogue (MABE): a new route to cyclic peptides and peptidomimetics.
University of California San Diego
(E)- and (Z)-7-arylidenenaltrexones: synthesis and opioid receptor radioligand displacement assays.
University of Washington
Probes for narcotic receptor mediated phenomena. 23. Synthesis, opioid receptor binding, and bioassay of the highly selective delta agonist (+)-4-[(alpha R)-alpha-((2S,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]- N,N-diethylbenzamide (SNC 80) and related novel nonpeptide delta opioid r
National Institute of Diabetes and Digestive and Kidney Diseases
Cyclic enkephalin analogues with exceptional potency and selectivity for delta-opioid receptors.
University of Arizona
Discovery of a novel class of substituted pyrrolooctahydroisoquinolines as potent and selective delta opioid agonists, based on an extension of the message-address concept.
Smithkline Beecham
Evolution of the Dmt-Tic pharmacophore: N-terminal methylated derivatives with extraordinary delta opioid antagonist activity.
University of Ferrara
Synthesis and pharmacological activity of deltorphin and dermorphin-related glycopeptides.
University of Ferrara
Probes for narcotic receptor-mediated phenomena. 25. Synthesis and evaluation of N-alkyl-substituted (alpha-piperazinylbenzyl)benzamides as novel, highly selective delta opioid receptor agonists.
National Institute of Diabetes and Digestive and Kidney Diseases
Pyrrolomorphinans as delta opioid receptor antagonists. The role of steric hindrance in conferring selectivity.
University of Minnesota
7-Spiroindanyl derivatives of naltrexone and oxymorphone as selective ligands for delta opioid receptors.
University of Minnesota
Opioid antagonist activity of naltrexone-derived bivalent ligands: importance of a properly oriented molecular scaffold to guide"address" recognition at kappa opioid receptors.
University of Minnesota
Arylacetamide-derived fluorescent probes: synthesis, biological evaluation, and direct fluorescent labeling of kappa opioid receptors in mouse microglial cells.
University of Minnesota
The use of topographical constraints in receptor mapping: investigation of the topographical requirements of the tryptophan 30 residue for receptor binding of Asp-Tyr-D-Phe-Gly-Trp-(N-Me)Nle-Asp-Phe-NH2 (SNF 9007), a cholecystokinin (26-33) analogue that binds to both CCK-B and delta-opioid recepto
University of Arizona
Probes for narcotic receptor-mediated phenomena. 21. Novel derivatives of 3-(1,2,3,4,5,11-hexahydro-3-methyl-2,6-methano-6H-azocino[4,5-b]indol- 6-yl)-phenols with improved delta opioid receptor selectivity.
National Institute of Diabetes and Digestive and Kidney Diseases
Enantiomers of diastereomeric cis-N-[1-(2-hydroxy-2-phenylethyl)- 3-methyl-4-piperidyl]-N-phenylpropanamides: synthesis, X-ray analysis, and biological activities.
Research Triangle Institute
Probes for narcotic receptor-mediated phenomena. 20. Alteration of opioid receptor subtype selectivity of the 5-(3-hydroxyphenyl)morphans by application of the message-address concept: preparation of delta-opioid receptor ligands.
National Institute of Diabetes and Digestive and Kidney Diseases
Isothiocyanate-substituted benzyl ether opioid receptor ligands derived from 6 beta-naltrexol.
University of Washington
7'-Substituted amino acid conjugates of naltrindole. Hydrophilic groups as determinants of selective antagonism of delta 1 opioid receptor-mediated antinociception in mice.
University of Minnesota
Synthesis and biological evaluation of 14-alkoxymorphinans. 11. 3-Hydroxycyprodime and analogues: opioid antagonist profile in comparison to cyprodime.
University of Innsbruck
Cyclic beta-casomorphin analogues with mixed mu agonist/delta antagonist properties: synthesis, pharmacological characterization, and conformational aspects.
Clinical Research Institute of Montreal
Synthesis of naltrexone-derived delta-opioid antagonists. Role of conformation of the delta address moiety.
University of Minnesota
Synthesis and opioid receptor affinity of a series of aralkyl ethers of 6 alpha- and 6 beta-naltrexol.
University of Washington
Antipodal alpha-N-(methyl through decyl)-N-normetazocines (5,9 alpha-dimethyl-2'-hydroxy-6,7-benzomorphans): in vitro and in vivo properties.
Virginia Commonwealth University
Isothiocyanate-substituted kappa-selective opioid receptor ligands derived from N-methyl-N-[(1S)-1-phenyl-2-(1-pyrrolidinyl)ethyl] phenylacetamide.
University of Washington
Discovery of nanomolar ligands for 7-transmembrane G-protein-coupled receptors from a diverse N-(substituted)glycine peptoid library.
Chiron
Probes for narcotic receptor mediated phenomena. 19. Synthesis of (+)-4-[(alpha R)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3- methoxybenzyl]-N,N-diethylbenzamide (SNC 80): a highly selective, nonpeptide delta opioid receptor agonist.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and delta-opioid receptor antagonist activity of a naltrindole analogue with a regioisomeric indole moiety.
University of Minnesota
Newly discovered stereochemical requirements in the side-chain conformation of delta opioid agonists for recognizing opioid delta receptors.
University of Arizona
14 alpha,14' beta-[Dithiobis[(2-oxo-2,1-ethanediyl)imino]]bis (7,8-dihydromorphinone) and 14 alpha,14' beta-[dithiobis[(2-oxo-2,1- ethanediyl)imino]]bis[7,8-dihydro-N-(cyclopropylmethyl)normorphinone]: chemistry and opioid binding properties.
Institute
[L-Ala3]DPDPE: a new enkephalin analog with a unique opioid receptor activity profile. Further evidence of delta-opioid receptor multiplicity.
University of Arizona
Structure-activity relationship of N17'-substituted norbinaltorphimine congeners. Role of the N17' basic group in the interaction with a putative address subsite on the kappa opioid receptor.
University of Minnesota
Cyclic enkephalin analogs with exceptional potency at peripheral delta opioid receptors.
University of Arizona
Possible contribution of a glutathione conjugate to the long-duration action of beta-funaltrexamine.
University of Minnesota
TIPP[psi]: a highly potent and stable pseudopeptide delta opioid receptor antagonist with extraordinary delta selectivity.
Clinical Research Institute of Montreal
A selective delta 1 opioid receptor agonist derived from oxymorphone. Evidence for separate recognition sites for delta 1 opioid receptor agonists and antagonists.
University of Minnesota
Synthesis and kappa-opioid antagonist selectivity of a norbinaltorphimine congener. Identification of the address moiety required for kappa-antagonist activity.
University of Minnesota
A potent new class of kappa-receptor agonist: 4-substituted 1-(arylacetyl)-2-[(dialkylamino)methyl]piperazines.
Glaxo Group Research
Non-peptide ligands for opioid receptors. Design of kappa-specific agonists.
University of Catania
A remarkable change of opioid receptor selectivity on the attachment of a peptidomimetic kappa address element to the delta antagonist, natrindole: 5'-[N2-alkylamidino)methyl]naltrindole derivatives as a novel class of kappa opioid receptor antagonists.
University of Minnesota
Substitution on the Phe3 aromatic ring in cyclic delta opioid receptor-selective dermorphin/deltorphin tetrapeptide analogues: electronic and lipophilic requirements for receptor affinity.
University of Michigan
Systemic analgesic activity and delta-opioid selectivity in [2,6-dimethyl-Tyr1,D-Pen2,D-Pen5]enkephalin.
Searle Research and Development
N-terminal alkylated derivatives of [D-Pro10]dynorphin A-(1-11) are highly selective for kappa-opioid receptors.
Oregon State University
O3-(2-carbomethoxyallyl) ethers of opioid ligands derived from oxymorphone, naltrexone, etorphine, diprenorphine, norbinaltorphimine, and naltrindole. Unexpected O3-dealkylation in the opioid radioligand displacement assay.
University of Washington
Incorporation of a novel conformationally restricted tyrosine analog into a cyclic, delta opioid receptor selective tetrapeptide (JOM-13) enhances delta receptor binding affinity and selectivity.
University of Michigan
Opioid agonist and antagonist activities of morphindoles related to naltrindole.
University of Minnesota
Substituted 1-(aminomethyl)-2-(arylacetyl)-1,2,3,4-tetrahydroisoquinolines: a novel class of very potent antinociceptive agents with varying degrees of selectivity for kappa and mu opioid receptors.
Zambeletti Research Laboratories
Analogs of the delta opioid receptor selective cyclic peptide [2-D-penicillamine,5-D-penicillamine]-enkephalin: 2',6'-dimethyltyrosine and Gly3-Phe4 amide bond isostere substitutions.
G.D. Searle And
Probes for narcotic receptor mediated phenomena. 18. Epimeric 6 alpha- and 6 beta-iodo-3,14-dihydroxy-17-(cyclopropylmethyl)-4,5 alpha-epoxymorphinans as potential ligands for opioid receptor single photon emission computed tomography: synthesis, evaluation, and radiochemistry of [125I]-6 beta-iodo
National Institute of Diabetes and Digestive and Kidney Diseases
Enantiomeric N-substituted N-normetazocines: a comparative study of affinities at sigma, PCP, and mu opioid receptors.
Research Triangle Institute
Electrophilic opioid ligands. Oxygen tethered alpha-methylene-gamma-lactone, acrylate, isothiocyanate, and epoxide derivatives of 6 beta-naltrexol.
University of Washington
Selective reversible and irreversible ligands for the kappa opioid receptor.
National Taiwan University
An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists.
University of Minnesota
Role of spacer and address components in peptidomimetic delta opioid receptor antagonists related to naltrindole.
University of Minnesota
Synthesis and structure-activity relationships of deltorphin analogues.
University of Ferrara
Function of negative charge in the"address domain" of deltorphins.
National Institute of Environmental Health Sciences
Role of the spacer in conferring kappa opioid receptor selectivity to bivalent ligands related to norbinaltorphimine.
University of Minnesota
Highly selective kappa opioid analgesics. 4. Synthesis of some conformationally restricted naphthalene derivatives with high receptor affinity and selectivity.
Parke-Davis Research Unit
Photoactivatable opiate derivatives as irreversible probes of the mu-opioid receptor.
Louis Pasteur University
Electrophilic alpha-methylene-gamma-lactone and isothiocyanate opioid ligands related to etorphine.
University of Washington
Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.
University of Minnesota
Conjugate addition ligands of opioid antagonists. Methacrylate esters and ethers of 6 alpha- and 6 beta-naltrexol.
University of Washington
Thiazole as a carbonyl bioisostere. A novel class of highly potent and selective 5-HT3 receptor antagonists.
Pfizer
[D-Pen2,D-Pen5]enkephalin analogues with increased affinity and selectivity for delta opioid receptors.
University of Arizona
Benzofuro[2,3-c]pyridin-6-ols: synthesis, affinity for opioid-receptor subtypes, and antinociceptive activity.
Ciba-Geigy
Highly selective kappa-opioid analgesics. 2. Synthesis and structure-activity relationships of novel N-[(2-aminocyclohexyl)aryl]acetamide derivatives.
Parke-Davis Research Unit
Synthesis, opioid receptor binding profile, and antinociceptive activity of 1-azaspiro[4.5]decan-10-yl amides.
Ciba-Geigy
Synthesis of highly mu and delta opioid receptor selective peptides containing a photoaffinity group.
University of Arizona
Cyclic enkephalin analogues containing alpha-amino-beta-mercapto-beta,beta-pentamethylenepropionic acid at positions 2 or 5.
Smith Kline and French Laboratories
Highly selective kappa opioid analgesics. Synthesis and structure-activity relationships of novel N-[(2-aminocyclohexyl)aryl]acetamide and N-[(2-aminocyclohexyl)aryloxy]acetamide derivatives.
Parke-Davis Research Unit
Synthesis and analgesic properties of N-substituted trans-4a-aryldecahydroisoquinolines.
Eli Lilly
Investigation of the structural parameters involved in the mu and delta opioid receptor discrimination of linear enkephalin-related peptides.
University of Paris
Effects of addition of a 2-methyl group to ethyl nipecotates (beta-meperidines) on receptor affinities and opiate agonist/antagonist activities.
Sri International
Hexahydro-1H-1-pyrindines from acid rearrangement of 9-alkylidene-5-(m-methoxyphenyl)-2-methylmorphans. A new structural type of narcotic antagonists.
TBA
Hybrid bivalent ligands with opiate and enkephalin pharmacophores.
University of Minnesota
N-substituent modulation of opiate agonist/antagonist activity in resolved 3-methyl-3-(m-hydroxyphenyl)piperidines.
TBA
Design and synthesis of conformationally constrained somatostatin analogues with high potency and specificity for mu opioid receptors.
TBA
Probes for narcotic receptor mediated phenomena. 7. Synthesis and pharmacological properties of irreversible ligands specific for mu or delta opiate receptors.
TBA
Synthesis and pharmacological characterization in vitro of cyclic enkephalin analogues: effect of conformational constraints on opiate receptor selectivity.
TBA
Synthesis and biological evaluation of a metazocine-containing enkephalinamide. Evidence for nonidentical roles of the tyramine moiety in opiates and opioid peptides.
TBA
Evidence of the preferential involvement of mu receptors in analgesia using enkephalins highly selective for peripheral mu or delta receptors.
TBA
Oral bioavailability of a new class of micro-opioid receptor agonists containing 3,6-bis[Dmt-NH(CH(2))(n)]-2(1H)-pyrazinone with central-mediated analgesia.
National Institutes of Environmental Health Sciences
(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents.
Virginia Commonwealth University
The design and synthesis of a novel quinolizidine template for potent opioid and opioid receptor-like (ORL1, NOP) receptor ligands.
Sri International
Synthesis and binding affinity of neuropeptide Y at opiate receptors.
University of North Carolina At Wilmington
Synthesis, opioid receptor binding, and functional activity of 5'-substituted 17-cyclopropylmethylpyrido[2',3':6,7]morphinans.
Southern Research Institute
trans-3,4-dimethyl-4-(3-carboxamidophenyl)piperidines: a novel class of micro-selective opioid antagonists.
Adolor
Synthesis and structure-activity relationships of aminoalkylazetidines as ORL1 receptor ligands.
Schering-Plough Research Institute
Synthesis and biological activities of YkFA analogues: effects of position 4 substitutions and altered ring size on in vitro opioid activity.
University of Louisville
Selective delta-opioid receptor ligands: potential PET ligands based on naltrindole.
University of Bristol
Derivatives of 17-(2-methylallyl)-substituted noroxymorphone: variation of the delta address and its effects on affinity and selectivity for the delta opioid receptor.
Niddk
Mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine abuse: synthesis and opioid receptor binding affinity of N-substituted derivatives of morphinan.
Harvard Medical School
Piperazinyl benzamidines: synthesis and affinity for the delta opioid receptor.
R. W. Johnson Pharmaceutical Research Institute
3-Carboxamido analogues of morphine and naltrexone. synthesis and opioid receptor binding properties.
Pharmacia
ORL1 receptor ligands: structure-activity relationships of 8-cycloalkyl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-ones.
F. Hoffmann-La Roche
Synthesis of enantiomerically pure (+)- and (-)-18-methoxycoronaridine hydrochloride and their preliminary assessment as anti-addictive agents.
Albany Molecular Research
Synthesis and binding activity of endomorphin-1 analogues containing beta-amino acids.
University of Bologna
N-Cyclohexylethyl-N-noroxymorphindole: a mu-opioid preferring analogue of naltrindole.
University of Maryland
Selective kappa-opioid antagonists related to naltrindole. Effect of side-chain spacer in the 5'-amidinoalkyl series.
University of Bristol
Beta-casomorphins: substitution of phenylalanine with beta-homo phenylalanine increases the mu-type opioid receptor affinity.
University of Naples Federico II
Synthesis of novel analogues of the delta opioid ligand SNC-80 using REM resin.
Organon Laboratories
Delta opioid binding selectivity of 3-ether analogs of naltrindole.
National Institute of Diabetes
Optically pure (-)-4-[(N-allyl-3-methyl-4-piperidinyl)phenyl-amino]-N,N-diethylbenzami de displays selective binding and full agonist activity for the delta opioid receptor.
Research Triangle Institute
(+/-)-4-[(N-allyl-cis-3-methyl-4-piperidinyl)phenylamino]-N,N-diethylbenzamide displays selective binding for the delta opioid receptor.
Research Triangle Institute
Synthesis and biological activity of 3-substituted 3-desoxynaltrindole derivatives.
National Institute of Diabetes
Design of a high affinity peptidomimetic opioid agonist from peptide pharmacophore models.
University of Michigan
A high affinity, mu-opioid receptor-selective enkephalin analogue lacking an N-terminal tyrosine.
University of Michigan
Selective alpha-1a adrenergic receptor antagonists. Effects of pharmacophore regio- and stereochemistry on potency and selectivity.
Merck
Syntheses of potent Leu-enkephalin analogs possessing beta-hydroxy-alpha,alpha-disubstituted-alpha-amino acid and their characterization to opioid receptors.
Institute For Bioorganic Research
Pyrrolooctahydroisoquinolines as potent and selective opioid receptor ligands: SAR analysis and docking studies
TBA
Synthesis and biological evaluation of 14-alkoxymorphinans. 14.1 14-ethoxy-5-methyl substituted indolomorphinans with opioid receptor selectivity
TBA
Synthesis and biological evaluation of 14-alkoxymorphinans.12.1 A phenethyl analogue of the -selective opioid receptor antagonist cyprodime
TBA
EMD 61 753 as a favourable representative of structurally novel arylacetamido-type K opiate receptor agonists
TBA
Neurotensin receptor binding and antinociceptive activity for lipophilic N-amido neurotensin(913) analogs
TBA
SAR and biological evaluation of 3-azabicyclo[3.1.0]hexane derivatives asµ opioid ligands.
Pfizer
Probes for narcotic receptor mediated phenomena. 44. Synthesis of an N-substituted 4-hydroxy-5-(3-hydroxyphenyl)morphan with high affinity and selectiveµ-antagonist activity.
National Institute On Drug Abuse and The National Institute On Alcohol Abuse and Alcoholism
¿-Carbolines: a novel class of cannabinoid agonists with high aqueous solubility and restricted CNS penetration.
Astrazeneca R&D Montreal
4-Piperidin-4-ylidenemethyl-benzamides asd-opioid receptor agonists for CNS indications: identifying clinical candidates.
Astrazeneca Pharmaceuticals
Differential signaling properties at the kappa opioid receptor of 12-epi-salvinorin A and its analogues.
Harvard Medical School
Synthesis, radiofluorination and pharmacological evaluation of a fluoromethyl spirocyclic PET tracer for centrals1 receptors and comparison with fluoroalkyl homologs.
Institute of Radiopharmacy
Synthesis of quinolinomorphinan-4-ol derivatives asd opioid receptor agonists.
Kitasato University
Effect of 2',6'-dimethyl-L-tyrosine (Dmt) on pharmacological activity of cyclic endomorphin-2 and morphiceptin analogs.
Medical University of Lodz
Discovery of aminobenzyloxyarylamides as¿ opioid receptor selective antagonists: application to preclinical development of a¿ opioid receptor antagonist receptor occupancy tracer.
Eli Lilly
Identification of a potent and selectives¿? receptor agonist potentiating NGF-induced neurite outgrowth in PC12 cells.
University of Pavia
Synthesis and biological evaluation of new opioid agonist and neurokinin-1 antagonist bivalent ligands.
University of Arizona
Synthesis of novel triplet drugs with 1,3,5-trioxazatriquinane skeletons and their pharmacologies. Part 2: Synthesis of novel triplet drugs with the epoxymethano structure (capped homotriplet).
Kitasato University
Synthesis, biological evaluation, and automated docking of constrained analogues of the opioid peptide H-Dmt-D-Ala-Phe-Gly-NH2 using the 4- or 5-methyl substituted 4-amino-1,2,4,5-tetrahydro-2-benzazepin-3-one scaffold.
Vrije Universiteit Brussel
Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine.
University of Bath
Derivatives of pyrrolo[3,4-d]pyridazinone, a new class of analgesic agents.
Wroclaw Medical University
Structure selectivity relationship studies of 17-cyclopropylmethyl-3,14ß-dihydroxy-4,5a-epoxy-6ß-[(4'-pyridyl)carboxamido]morphinan derivatives toward the development of the mu opioid receptor antagonists.
Virginia Commonwealth University
Design and discovery of a selective small molecule¿ opioid antagonist (2-methyl-N-((2'-(pyrrolidin-1-ylsulfonyl)biphenyl-4-yl)methyl)propan-1-amine, PF-4455242).
Pfizer
Benzyl derivatives with in vitro binding affinity for human opioid and cannabinoid receptors from the fungus Eurotium repens.
The University of Mississippi
Probes for narcotic receptor mediated phenomena. Part 42: synthesis and in vitro pharmacological characterization of the N-methyl and N-phenethyl analogues of the racemic ortho-c and para-c oxide-bridged phenylmorphans.
National Institute On Drug Abuse and The National Institute On Alcohol Abuse and Alcoholism
Discovery and synthesis of a new class of opioid ligand having a 3-azabicyclo[3.1.0]hexane core. An example of a 'magic methyl' giving a 35-fold improvement in binding.
Pfizer
Probes for narcotic receptor mediated phenomena. 43. Synthesis of the ortho-a and para-a, and improved synthesis and optical resolution of the ortho-b and para-b oxide-bridged phenylmorphans: compounds with moderate to low opioid-receptor affinity.
National Institute On Drug Abuse and The National Institute On Alcohol Abuse and Alcoholism
Synthesis of novel triplet drugs with 1,3,5-trioxazatriquinane skeletons and their pharmacologies. 1: Synthesis of triplet drugs with morphinan skeletons.
Kitasato University
Synthesis of 7,9-diazabicyclo[4.2.2]decanes as conformationally restricted κ receptor agonists: fine tuning of the dihedral angle of the ethylenediamine pharmacophore.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Design of novel neurokinin 1 receptor antagonists based on conformationally constrained aromatic amino acids and discovery of a potent chimeric opioid agonist-neurokinin 1 receptor antagonist.
Vrije Universiteit Brussel
Synthesis and binding affinity of novel mono- and bivalent morphinan ligands for κ, μ, and δ opioid receptors.
Harvard Medical School
Opioid receptor probes derived from cycloaddition of the hallucinogen natural product salvinorin A.
University of Iowa
Discovery of a potent and efficacious peptide derivative ford/µ opioid agonist/neurokinin 1 antagonist activity with a 2',6'-dimethyl-L-tyrosine: in vitro, in vivo, and NMR-based structural studies.
University of Arizona
Synthesis and pharmacological evaluation of bivalent antagonists of the nociceptin opioid receptor.
Istituto Superiore Di Sanit£
Design, synthesis, pharmacological evaluation, and structure-activity study of novel endomorphin analogues with multiple structural modifications.
Hungarian Academy of Sciences
Synthesis of 6,14-epoxymorphinan derivatives and their pharmacologies.
Kitasato University
Probes for narcotic receptor mediated phenomena. 41. Unusual inverseµ-agonists and potentµ-opioid antagonists by modification of the N-substituent in enantiomeric 5-(3-hydroxyphenyl)morphans.
National Institute On Drug Abuse
Synthesis and pharmacological activities of 6-glycine substituted 14-phenylpropoxymorphinans, a novel class of opioids with high opioid receptor affinities and antinociceptive potencies.
University of Innsbruck
Synthesis, pharmacological activity and structure affinity relationships of spirocyclics(1) receptor ligands with a (2-fluoroethyl) residue in 3-position.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Synthesis and biological evaluation of new salvinorin A analogues incorporating natural amino acids.
University of Mississippi
Synthesis and structure-activity studies of benzyl ester meperidine and normeperidine derivatives as selective serotonin transporter ligands.
University of New Orleans
Design and synthesis of KNT-127, ad-opioid receptor agonist effective by systemic administration.
Kitasato University
Synthesis, structure-affinity relationships, and radiolabeling of selective high-affinity 5-HT4 receptor ligands as prospective imaging probes for positron emission tomography.
National Institute of Mental Health
Discovery of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides as selective antagonists of the kappa opioid receptor. Part 1.
Astrazeneca Pharmaceuticals
Synthesis and activity of endomorphin-2 and morphiceptin analogues with proline surrogates in position 2.
Sapienza University of Rome
Spiroindolones, a potent compound class for the treatment of malaria.
Swiss Tropical and Public Health Institute
Novel N-methylated 8-oxoisoguanines from Pacific sponges with diverse neuroactivities.
Hokkaido University
SAR development of a series of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides as kappa opioid receptor antagonists. Part 2.
Astrazeneca Pharmaceuticals
Role of 2',6'-dimethyl-l-tyrosine (Dmt) in some opioid lead compounds.
University of Cagliari
Biological and conformational evaluation of bifunctional compounds for opioid receptor agonists and neurokinin 1 receptor antagonists possessing two penicillamines.
University of Arizona
A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.
Università
Investigation of Beckett-Casy model 2: synthesis of novel 15-16 nornaltrexone derivatives and their pharmacology.
Kitasato University
Synthesis and evaluation of new endomorphin-2 analogues containing (Z)-alpha,beta-didehydrophenylalanine (Delta(Z)Phe) residues.
Sapienza University of Rome
Synthesis and opioid activity of novel 6-substituted-6-demethoxy-ethenomorphinans.
University of Debrecen
Hasubanan alkaloids with delta-opioid binding affinity from the aerial parts of Stephania japonica.
Griffith University
Effect of linker substitution on the binding of butorphan univalent and bivalent ligands to opioid receptors.
Harvard Medical School
Synthesis and evaluation of opioid receptor-binding affinity of elaeocarpenine and its analogs.
Kyorin Pharmaceutical
Novel multiple opioid ligands based on 4-aminobenzazepinone (Aba), azepinoindole (Aia) and tetrahydroisoquinoline (Tic) scaffolds.
Vrije Universiteit Brussel
Identification of piperazine-bisamide GHSR antagonists for the treatment of obesity.
Amgen
Rapid access towards follow-up NOP receptor agonists using a knowledge based approach.
Schering-Plough Research Institute
Synthesis and in vitro autoradiographic evaluation of a novel high-affinity radioiodinated ligand for imaging brain cannabinoid subtype-1 receptors.
National Institute of Mental Health
Investigation of Beckett-Casy model 1: synthesis of novel 16,17-seco-naltrexone derivatives and their pharmacology.
Kitasato University
Design, synthesis and SAR analysis of novel selective sigma1 ligands (Part 2).
University of Pavia
Probes for narcotic receptor mediated phenomena. 40. N-substituted cis-4a-ethyl-1,2,3,4,4a,9a-hexahydrobenzofuro[2,3-c]pyridin-8-ols.
Nida
Highly selective and potent mu opioid ligands by unexpected substituent on morphine skeleton.
Fudan University
The biological activity and metabolic stability of peptidic bifunctional compounds that are opioid receptor agonists and neurokinin-1 receptor antagonists with a cystine moiety.
University of Arizona
Novel delta opioid receptor agonists exhibit differential stimulation of signaling pathways.
University of Medicine and Dentistry of New Jersey-Robert Wood Johnson Medical School and The Informatics Institute of Umdnj
Synthesis and characterizations of novel quinoline derivatives having mixed ligand activities at the kappa and mu receptors: Potential therapeutic efficacy against morphine dependence.
Institute of Chemical Biology
Synthesis and opioid activity of enantiomeric N-substituted 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolines.
National Taiwan University
Design, synthesis, biological properties, and molecular modeling investigations of novel tacrine derivatives with a combination of acetylcholinesterase inhibition and cannabinoid CB1 receptor antagonism.
Solvay Pharma
Synthesis and opioid receptor binding affinities of 2-substituted and 3-aminomorphinans: ligands for mu, kappa, and delta opioid receptors.
Harvard Medical School
N,N-Diethyl-4-[(3-hydroxyphenyl)(piperidin-4-yl)amino] benzamide derivatives: the development of diaryl amino piperidines as potent delta opioid receptor agonists with in vivo anti-nociceptive activity in rodent models.
Astrazeneca R & D Montr£Al
Molecular modeling studies to predict the possible binding modes of endomorphin analogs in mu opioid receptor.
Lanzhou University
Discovery of novel phenethylpyridone derivatives as potent melanin-concentrating hormone 1 receptor antagonists.
Tsukuba Research Institute
Synthesis and investigations of double-pharmacophore ligands for treatment of chronic and neuropathic pain.
University of Arizona
Synthesis and evaluation of a full-agonist orvinol for PET-imaging of opioid receptors: [11C]PEO.
Biomedizinische Forschungsreagenzien
Univalent and bivalent ligands of butorphan: characteristics of the linking chain determine the affinity and potency of such opioid ligands.
Harvard Medical School
Probes for narcotic receptor mediated phenomena. 39. Enantiomeric N-substituted benzofuro[2,3-c]pyridin-6-ols: synthesis and topological relationship to oxide-bridged phenylmorphans.
National Institute On Drug Abuse and The National Institute On Alcohol Abuse and Alcoholi
Discovery of dermorphin-based affinity labels with subnanomolar affinity for mu opioid receptors.
The University of Kansas
14beta-Arylpropiolylamino-17-cyclopropylmethyl-7,8-dihydronormorphinones and related opioids. Further examples of pseudoirreversible mu opioid receptor antagonists.
University of Bristol
Design, synthesis and biological evaluation of a bivalent micro opiate and adenosine A1 receptor antagonist.
Aix-Marseille Universit£
Agonist vs antagonist behavior of delta opioid peptides containing novel phenylalanine analogues in place of Tyr(1).
Clinical Research Institute of Montreal
The effects of C-terminal modifications on the opioid activity of [N-benzylTyr(1)]dynorphin A-(1-11) analogues.
University of Kansas
Delta agonist hydroxy bioisosteres: the discovery of 3-((1-benzylpiperidin-4-yl){4-[(diethylamino)carbonyl]phenyl}amino)benzamide with improved delta agonist activity and in vitro metabolic stability.
Astrazeneca R & D Montr£Al
Evaluation of spirocyclic 3-(3-fluoropropyl)-2-benzofurans as sigma1 receptor ligands for neuroimaging with positron emission tomography.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Westf£Lischen Wilhelms-Universit£T M£Nster
Pentapeptides displaying mu opioid receptor agonist and delta opioid receptor partial agonist/antagonist properties.
University of Michigan
Identification, structure-activity relationships and molecular modeling of potent triamine and piperazine opioid ligands.
Institute For Molecular Studies
Design, synthesis, and characterization of 6beta-naltrexol analogs, and their selectivity for in vitro opioid receptor subtypes.
University of New England
Design, synthesis, and pharmacological activities of dynorphin A analogues cyclized by ring-closing metathesis.
The University of Kansas
Spirocyclic delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-3-hydroxy-4-(spiro[chromene-2,4'-piperidine]-4-yl) benzamide (ADL5747).
Adolor
Influence of the side chain next to C-terminal benzimidazole in opioid pseudopeptides containing the Dmt-Tic pharmacophore.
University of Cagliari
Aerobic oxidation of indolomorphinan without the 4,5-epoxy bridge and subsequent rearrangement of the oxidation product to spiroindolinonyl-C-normorphinan derivative.
Kitasato University
Identification of MK-1925: a selective, orally active and brain-penetrable opioid receptor-like 1 (ORL1) antagonist.
Tsukuba Research Institute
Discovery of orally active 3-pyridinyl-tropane as a potent nociceptin receptor agonist for the management of cough.
Schering-Plough Research Institute
Synthesis and evaluation of new endomorphin analogues modified at the Pro(2) residue.
Sapienza University of Rome
Identification of an orally active opioid receptor-like 1 (ORL1) receptor antagonist 4-{3-[(2R)-2,3-dihydroxypropyl]-2-oxo-2,3-dihydro-1H-benzimidazol-1-yl}-1-[(1S,3S,4R)-spiro[bicyclo[2.2.1]heptane-2,1'-cyclopropan]-3-ylmethyl]piperidine as clinical candidate.
Tsukuba Research Institute
Akuammine and Dihydroakuammine, Two Indolomonoterpene Alkaloids Displaying Affinity for Opioid Receptors
TBA
Structure-activity relationships of novel endomorphin-2 analogues with N-O turns induced by alpha-aminoxy acids.
TBA
trans N-Methyl-N-[2-(1-pyrrolidinyl)cyclohexyl] cycloprop-2-ene-1-carboxamides: Novel lipophilic kappa opioid agonists
TBA
6N-Cinnamoyl-β-naltrexamine and its p-nitro derivative. High efficacy κ-opioid agonists with weak antagonist actions
TBA
Synthesis and opioid binding properties of 2-chloroacrylamido derivatives of 7,8-dihydromorphinans
TBA
Suppression of morphine and cocaine self-administration in rats by a mixed mu antagonist-kappa agonist (N-CBM-TAMO) and a long-acting selective D1 antagonist (AS-300)
TBA
Stereoselective synthesis and evaluation of all stereoisomers of Z4349, a novel and selective μ-opioid analgesic
TBA
Morphinan cyclic imines and pyrrolidines containing a constrained phenyl group: High affinity opioid agonists
TBA
N-Methyl and N-cyclopropylmethyl-14α,14′β-[dithiobis[(2-oxo-2,1-ethanediyl)imino]]bis(7,8-dihydro-5β-methyl-morphinone) MET-TAMO and N-CPM-MET-TAMO: Synthesis and opioid binding properties
TBA
Specific affinity labeling of μ opioid receptors in rat brain by S-activated sulfhydryldihydromorphine analogs
TBA
The discovery of CP-96,021 and CP-96,486, balanced, combined, potent and orally active leukotriene D4 (LTD4)/platelet activating factor (PAF) receptor antagonists.
TBA
Octahydro-1,2,3,4,4a,5,11,11a-pyrido[3,4-c][1,5]benzoxazepines: conformationally restricted fentanyl analogs
TBA
Synthesis and biological properties of quaternized N-methylation analogs of D-Arg-2-dermorphin tetrapeptide
TBA
A new approach to enhance bioavailability of biologically active peptides: conjugation of a δ opioid agonist to β-cyclodextrin
TBA
The use of synthetic peptide combinatorial libraries for the determination of peptide ligands in radio-receptor assays: Opioid peptides
TBA
Topographical requirements for delta opioid ligands: The synthesis and biological properties of a cyclic analogue of deltorphin I
TBA
Biological activity of endomorphin and [Dmt1]endomorphin analogs with six-membered proline surrogates in position 2.
Medical University of Lodz
The discovery of tropane derivatives as nociceptin receptor ligands for the management of cough and anxiety.
Schering-Plough Research Institute
Identification of 3-substituted N-benzhydryl-nortropane analogs as nociceptin receptor ligands for the management of cough and anxiety.
Schering-Plough Research Institute
Synthesis and in vitro affinities of various MDL 100907 derivatives as potential 18F-radioligands for 5-HT2A receptor imaging with PET.
Institute of Nuclear Chemistry Johannes Gutenberg-University Mainz
2,4-Diaminopyridine delta-opioid receptor agonists and their associated hERG pharmacology.
Pfizer
Discovery of mu-opioid selective ligands derived from 1-aminotetralin scaffolds made via metal-catalyzed ring-opening reactions.
University of Toronto
Modification of the furan ring of salvinorin A: identification of a selective partial agonist at the kappa opioid receptor.
Mclean Hospital
Induced association of mu opioid (MOP) and type 2 cholecystokinin (CCK2) receptors by novel bivalent ligands.
University of Minnesota
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 7: syntheses and opioid receptor properties of cyclic variants of cyclazocine.
Rensselaer Polytechnic Institute
Conformationally constrained opioid ligands: the Dmt-Aba and Dmt-Aia versus Dmt-Tic scaffold.
Vrije Universiteit Brussel
Probes for narcotic receptor mediated phenomena. 37. Synthesis and opioid binding affinity of the final pair of oxide-bridged phenylmorphans, the ortho- and para-b-isomers and their N-phenethyl analogues, and the synthesis of the N-phenethyl analogues of the ortho- and para-d-isomers.
National Institute On Drug Abuse
Structure-activity relationships of 3-substituted N-benzhydryl-nortropane analogs as nociceptin receptor ligands for the treatment of cough.
Schering-Plough Research Institute
The importance of micelle-bound states for the bioactivities of bifunctional peptide derivatives for delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.
University of Arizona
Novel opioid peptide derived antagonists containing (2S)-2-methyl-3-(2,6-dimethyl-4-carbamoylphenyl)propanoic acid [(2S)-Mdcp].
National University of Singapore
Synthesis and evaluation of [N-methyl-11C]N-desmethyl-loperamide as a new and improved PET radiotracer for imaging P-gp function.
National Institute of Mental Health
Highly functionalized 7-azaindoles as selective PPAR gamma modulators.
Merck Research Laboratories
Further studies on lead compounds containing the opioid pharmacophore Dmt-Tic.
University of Cagliari
Synthesis and pharmacological evaluation of hydrophobic esters and ethers of butorphanol at opioid receptors.
Harvard Medical School
Structural modifications of N-arylamide oxadiazoles: Identification of N-arylpiperidine oxadiazoles as potent and selective agonists of CB2.
Amgen
New endomorphin analogues containing alicyclic beta-amino acids: influence on bioactive conformation and pharmacological profile.
Hungarian Academy of Sciences
A novel class of cycloalkano[b]pyridines as potent and orally active opioid receptor-like 1 antagonists with minimal binding affinity to the hERG K+ channel.
Tsukuba Research Institute
Design, synthesis, and structure-activity relationship study of a novel class of ORL1 receptor antagonists based on N-biarylmethyl spiropiperidine.
Tsukuba Research Institute
1,4-Diazepanes derived from (S)-serine--homopiperazines with improved sigma(1) (sigma) receptor affinity and selectivity.
Institut FüR Pharmazeutische Und Medizinische Chemie
Structure-activity study of endomorphin-2 analogs with C-terminal modifications by NMR spectroscopy and molecular modeling.
Lanzhou University
Synthesis and in vitro evaluation of a library of modified endomorphin 1 peptides.
University of Queensland
Novel ORL1-selective antagonists with oral bioavailability and brain penetrability.
Banyu Tsukuba Research Institute
Internalisation of the mu-opioid receptor by endomorphin-1 and leu-enkephalin is dependant on aromatic amino acid residues.
University of Queensland
Nitrile analogs of meperidine as high affinity and selective sigma-1 receptor ligands.
University of Maryland
Novel highly potent mu-opioid receptor antagonist based on endomorphin-2 structure.
Medical University of Lodz
A new opioid designed multiple ligand derived from the micro opioid agonist endomorphin-2 and the delta opioid antagonist pharmacophore Dmt-Tic.
University of Ferrara
Design and synthesis of opioidmimetics containing 2',6'-dimethyl-L-tyrosine and a pyrazinone-ring platform.
Kobe Gakuin University
Structure-activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 1.
Eli Lilly
Probes for narcotic receptor mediated phenomena. 34. Synthesis and structure-activity relationships of a potent mu-agonist delta-antagonist and an exceedingly potent antinociceptive in the enantiomeric C9-substituted 5-(3-hydroxyphenyl)-N-phenylethylmorphan series.
National Institute On Drug Abuse
Functionalization of the 6,14-bridge of the orvinols. Part 3: preparation and pharmacological evaluation of 18- and 19-hydroxyl substituted orvinols.
University of Maryland
Synthesis and simple 18F-labeling of 3-fluoro-5-(2-(2-(fluoromethyl)thiazol-4-yl)ethynyl)benzonitrile as a high affinity radioligand for imaging monkey brain metabotropic glutamate subtype-5 receptors with positron emission tomography.
National Institute of Mental Health
4-Amino-5-vinyl-3(2H)-pyridazinones and analogues as potent antinociceptive agents: Synthesis, SARs, and preliminary studies on the mechanism of action.
Dipartimento Di Scienze Farmaceutiche
4-Phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives as non-peptidic selective delta-opioid agonists with potential anxiolytic/antidepressant properties. Part 2.
Johnson & Johnson Pharmaceutical Research & Development
Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands.
Kobe Gakuin University
Synthesis and pharmacological evaluation of 6,7-indolo/thiazolo-morphinans--further SAR of levorphanol.
Chinese Academy of Sciences
Pharmacological and Physicochemical Properties Optimization for Dual-Target Dopamine D
National Institute On Drug Abuse?Intramural Research Program
In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.
Harvard Medical School
A systematic review on the kappa opioid receptor and its ligands: New directions for the treatment of pain, anxiety, depression, and drug abuse.
University of Mississippi
Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Schering-Plough Research Institute
Benzo[b]thiophene-2-carboxamides as novel opioid receptor agonists with potent analgesic effect and reduced constipation.
National Health Research Institutes
Further studies on the effect of lysine at the C-terminus of the Dmt-Tic opioid pharmacophore.
University of Cagliari
A Molecular Toolbox of Positron Emission Tomography Tracers for General Anesthesia Mechanism Research.
Xiamen University
Understanding the structural requirements of 4-anilidopiperidine analogues for biological activities at mu and delta opioid receptors.
University of Arizona
Model of P-Glycoprotein Ligand Binding and Validation with Efflux Substrate Matched Pairs.
University of California
Dicarba analogues of the cyclic enkephalin peptides H-Tyr-c[D-Cys-Gly-Phe-D(or L)-Cys]NH(2) retain high opioid activity.
Clinical Research Institute of Montreal
Structure-Activity Relationship Study of Cannabidiol-Based Analogs as Negative Allosteric Modulators of the μ-Opioid Receptor.
Indiana University
Synthesis and structure-activity relationships of N-substituted spiropiperidines as nociceptin receptor ligands.
Schering-Plough Research Institute
Discovery and structure-activity relationships (SAR) of a novel class of 2-substituted N-piperidinyl indole-based nociceptin opioid receptor ligands.
Astraea Therapeutics
Studies on diketopiperazine and dipeptide analogs as opioid receptor ligands.
Texas Tech University Health Sciences Center
Synthesis and characterization of potent and selective mu-opioid receptor antagonists, [Dmt(1), D-2-Nal(4)]endomorphin-1 (Antanal-1) and [Dmt(1), D-2-Nal(4)]endomorphin-2 (Antanal-2).
Medical University
What We Have Gained from Ibogaine: α3β4 Nicotinic Acetylcholine Receptor Inhibitors as Treatments for Substance Use Disorders.
University of Illinois At Chicago
Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder.
High Point University
Structure-activity relationships of novel piperazines as antagonists for the melanocortin-4 receptor.
Taisho Pharmaceutical
Beta-methyl substitution of cyclohexylalanine in Dmt-Tic-Cha-Phe peptides results in highly potent delta opioid antagonists.
Hungarian Academy of Sciences
Structural Alterations of the "Address" Moiety of NAN Leading to the Discovery of a Novel Opioid Receptor Modulator with Reduced hERG Toxicity.
Virginia Commonwealth University
Benzomorphan skeleton, a versatile scaffold for different targets: A comprehensive review.
University of Catania
Partial retro-inverso, retro, and inverso modifications of hydrazide linked bifunctional peptides for opioid and cholecystokinin (CCK) receptors.
University of Arizona
Endomorphin-1 analogs with enhanced metabolic stability and systemic analgesic activity: design, synthesis, and pharmacological characterization.
Lanzhou University
Side Chain Cyclized Aromatic Amino Acids: Great Tools as Local Constraints in Peptide and Peptidomimetic Design.
Vrije Universiteit Brussel
Synthesis and evaluation of N-3 substituted phenoxypropyl piperidine benzimidazol-2-one analogues as NOP receptor agonists with analgesic and sedative properties.
Organon Laboratories
Transformation of mu-opioid receptor agonists into biologically potent mu-opioid receptor antagonists.
Kobe Gakuin University
Modified Akuamma Alkaloids with Increased Potency at the Mu-opioid Receptor.
University of Illinois Chicago
Oxidative Metabolism as a Modulator of Kratom's Biological Actions.
University of Health Sciences & Pharmacy and Washington University School of Medicine
Expanding the repertoire of methanocarba nucleosides from purinergic signaling to diverse targets.
National Institute of Diabetes & Digestive & Kidney Diseases
Synthesis of 3,6-bis[H-Tyr/H-Dmt-NH(CH2)m,n]-2(1H)pyrazinone derivatives: function of alkyl chain length on opioid activity.
Kobe Gakuin University
New opioid designed multiple ligand from Dmt-Tic and morphinan pharmacophores.
Harvard Medical School
Replacement of the N-terminal tyrosine residue in opioid peptides with 3-(2,6-dimethyl-4-carbamoylphenyl)propanoic acid (Dcp) results in novel opioid antagonists.
National University of Singapore
Discovery, Structure-Activity Relationship, and Mechanistic Studies of 1-((3
Fudan University
Synthesis and evaluation of 3-aminopropionyl substituted fentanyl analogues for opioid activity.
University of Arizona
Recent Scaffold Hopping Applications in Central Nervous System Drug Discovery.
The University of Sydney
Design and synthesis of 4-substituted-8-(2-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-one as a novel class of GlyT1 inhibitors: achieving selectivity against the mu opioid and nociceptin/orphanin FQ peptide (NOP) receptors.
F. Hoffmann-La Roche
6-N,N-dimethylamino-2,3-naphthalimide: a new environment-sensitive fluorescent probe in delta- and mu-selective opioid peptides.
Universidad De Santiago De Compostela
Discovery of 4-substituted-8-(2-hydroxy-2-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-one as a novel class of highly selective GlyT1 inhibitors with improved metabolic stability.
F. Hoffmann-La Roche
Identification of potent and highly selective chiral tri-amine and tetra-amine mu opioid receptors ligands: an example of lead optimization using mixture-based libraries.
Institute For Molecular Studies
Discovery of a novel, orally active, small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist.
Pfizer
Opioid receptor binding and antinociceptive activity of the analogues of endomorphin-2 and morphiceptin with phenylalanine mimics in the position 3 or 4.
Lanzhou University
3-(4-Piperidinyl)indoles and 3-(4-piperidinyl)pyrrolo-[2,3-b]pyridines as ligands for the ORL-1 receptor.
Johnson & Johnson Pharmaceutical Research and Development
Synthetic studies of neoclerodane diterpenes from Salvia divinorum: selective modification of the furan ring.
The University of Iowa
Synthesis of 8-aminomorphans with high KOR affinity.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Identification of potent phenyl imidazoles as opioid receptor agonists.
Johnson & Johnson Pharmaceutical Research & Development
The Repertoire of Small-Molecule PET Probes for Neuroinflammation Imaging: Challenges and Opportunities beyond TSPO.
Massachusetts General Hospital
Identification of a novel spiropiperidine opioid receptor-like 1 antagonist class by a focused library approach featuring 3D-pharmacophore similarity.
Banyu Tsukuba Research Institute
Synthesis and in vivo validation of [O-methyl-11C]2-{4-[4-(7-methoxynaphthalen-1-yl)piperazin- 1-yl]butyl}-4-methyl-2H-[1,2,4]triazine-3,5-dione: a novel 5-HT1A receptor agonist positron emission tomography ligand.
Columbia University College of Physicians and Surgeons
Conversion of the potent delta-opioid agonist H-Dmt-Tic-NH-CH(2)-bid into delta-opioid antagonists by N(1)-benzimidazole alkylation(1).
University of Cagliari
Synthesis and biological evaluation of novel hexahydro-pyrido[3',2':4,5]pyrrolo[1,2-a]pyrazines as potent and selective 5-HT(2C) receptor agonists.
F. Hoffmann-La Roche
Potent Dmt-Tic pharmacophoric delta- and mu-opioid receptor antagonists.
Kobe Gakuin University
Syntheses, biological evaluation, and molecular modeling of 18F-labeled 4-anilidopiperidines as mu-opioid receptor imaging agents.
Technische UniversitäT MüNchen
The Design and Optimization of Monomeric Multitarget Peptides for the Treatment of Multifactorial Diseases.
China Pharmaceutical University
Synthesis and structure-activity relationships of a new series of 2alpha-substituted trans-4,5-dimethyl-4-(3-hydroxyphenyl)piperidine as mu-selective opioid antagonists.
Adolor
Morphinan derivatives with an oxabicyclo[3.2.1]octane structure as dual agonists toward δ and κ opioid receptors.
Kitasato University
Synthesis and biological activity of the first cyclic biphalin analogues.
University of Arizona
Novel phenylamino acetamide derivatives as potent and selective kappa opioid receptor agonists.
Adolor
Is a Highly Selective and Potent κ Opioid Receptor (KOR) Agonist with an Unexpected Nonreduction in Locomotor Activity.
Fudan University
Discovery of N-(2-hydroxy-2-aryl-cyclohexyl) substituted spiropiperidines as GlyT1 antagonists with improved pharmacological profile.
F. Hoffmann-La Roche
Discovery of N-(2-aryl-cyclohexyl) substituted spiropiperidines as a novel class of GlyT1 inhibitors.
F. Hoffmann-La Roche
4-Phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives, a novel class of selective delta-opioid agonists.
Johnson and Johnson Pharmaceutical Research and Development
Potent and highly selective kappa opioid receptor agonists incorporating chroman- and 2,3-dihydrobenzofuran-based constraints.
Adolor
New series of potent delta-opioid antagonists containing the H-Dmt-Tic-NH-hexyl-NH-R motif.
Kobe Gakuin University
Preparation of 3-spirocyclic indolin-2-ones as ligands for the ORL-1 receptor.
Johnson & Johnson Pharmaceutical Research and Development
Synthesis of potent and selective serotonin 5-HT1B receptor ligands.
Columbia University College of Physicians and Surgeons
From the potent and selective mu opioid receptor agonist H-Dmt-d-Arg-Phe-Lys-NH(2) to the potent delta antagonist H-Dmt-Tic-Phe-Lys(Z)-OH.
University of Cagliari
Dual Sigma-1 receptor antagonists and hydrogen sulfide-releasing compounds for pain treatment: Design, synthesis, and pharmacological evaluation.
University of Catania
Effect of removal of the 14-hydroxy group on the affinity of the 4,5-epoxymorphinan derivatives for orexin and opioid receptors.
University of Tsukuba
Neoclerodane diterpenes as a novel scaffold for mu opioid receptor ligands.
The University of Iowa
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
TBA
Arylacetamide kappa opioid receptor agonists with reduced cytochrome P450 2D6 inhibitory activity.
Adolor
6-Hydroxy-1,2,3,4-tetrahydro-isoquinoline-3-carboxylic acid mimics active conformation of tyrosine in opioid peptides.
University of Catania
Ligand-based prediction of active conformation by 3D-QSAR flexibility descriptors and their application in 3+3D-QSAR models.
University of Szeged
Morphiceptin analogues containing a dipeptide mimetic structure: an investigation on the bioactive topology at the mu-receptor.
Università
Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands.
University of Trieste
Structure-activity relationship of the novel bivalent and C-terminal modified analogues of endomorphin-2.
Lanzhou University
Benzylaminofentanyl derivates: Discovery of bifunctional μ opioid and σ
Jiangsu Ocean University
Modulating β-arrestin 2 recruitment at the δ- and μ-opioid receptors using peptidomimetic ligands.
The Ohio State University
Structure-Activity Studies of 1
National Institute of Diabetes and Digestive and Kidney Diseases
Studies on the structure-activity relationship of 2',6'-dimethyl-l-tyrosine (Dmt) derivatives: bioactivity profile of H-Dmt-NH-CH(3).
Kobe Gakuin University
Synthesis and SAR studies of 3-phenoxypropyl piperidine analogues as ORL1 (NOP) receptor agonists.
Organon Laboratories
Development of potent mu-opioid receptor ligands using unique tyrosine analogues of endomorphin-2.
Kobe Gakuin University
Highly selective fluorescent analogue of the potent delta-opioid receptor antagonist Dmt-Tic.
University of Cagliary
Conformational Constraint between Aromatic Residue Side Chains in the "Message" Sequence of the Peptide Arodyn Using Ring Closing Metathesis Results in a Potent and Selective Kappa Opioid Receptor Antagonist.
The University of Kansas
C-terminal modified Enkephalin-like tetrapeptides with enhanced affinities at the kappa opioid receptor and monoamine transporters.
University of The Punjab
Design, Synthesis, and Biological Evaluation of NAP Isosteres: A Switch from Peripheral to Central Nervous System Acting Mu-Opioid Receptor Antagonists.
Virginia Commonwealth University
Rational Design, Chemical Syntheses, and Biological Evaluations of Peripherally Selective Mu Opioid Receptor Ligands as Potential Opioid Induced Constipation Treatment.
Virginia Commonwealth University
Azepinone as a conformational constraint in the design of kappa-opioid receptor agonists.
Adolor
Synthesis and Evaluation of Novel Tetrahydronaphthyridine CXCR4 Antagonists with Improved Drug-like Profiles.
Emory University
Parallel methods for the preparation and SAR exploration of N-ethyl-4-[(8-alkyl-8-aza-bicyclo[3.2.1]oct-3-ylidene)-aryl-methyl]-benzamides, powerful mu and delta opioid agonists.
Johnson and Johnson Pharmaceutical Research and Development
Novel Dual-Target μ-Opioid Receptor and Dopamine D
National Institute On Drug Abuse-Intramural Research Program
Rationale, design, and synthesis of novel phenyl imidazoles as opioid receptor agonists for gastrointestinal disorders.
Johnson & Johnson Pharmaceutical Research & Development
Design and synthesis of 4-phenyl piperidine compounds targeting the mu receptor.
Purdue Pharma
Synthesis, biological, and structural explorations of a series of μ-opioid receptor (MOR) agonists with high G protein signaling bias.
Yantai University
Structure-Based Design and Development of Chemical Probes Targeting Putative MOR-CCR5 Heterodimers to Inhibit Opioid Exacerbated HIV-1 Infectivity.
Virginia Commonwealth University
A novel cyclic enkephalin analogue with potent opioid antagonist activity.
Clinical Research Institute of Montreal
Direct influence of C-terminally substituted amino acids in the Dmt-Tic pharmacophore on delta-opioid receptor selectivity and antagonism.
University of Cagliary
Optimization of bifunctional piperidinamide derivatives as σ
Huazhong University of Science and Technology
Development of Multifunctional and Orally Active Cyclic Peptide Agonists of Opioid/Neuropeptide FF Receptors that Produce Potent, Long-Lasting, and Peripherally Restricted Antinociception with Diminished Side Effects.
Lanzhou University
Development of potent bifunctional endomorphin-2 analogues with mixed mu-/delta-opioid agonist and delta-opioid antagonist properties.
Kobe Gakuin University
Propionamide Derivatives as Dual μ-Opioid Receptor Agonists and σ
Esteve Pharmaceuticals
Design of a Stable Cyclic Peptide Analgesic Derived from Sunflower Seeds that Targets the κ-Opioid Receptor for the Treatment of Chronic Abdominal Pain.
Medical University of Vienna
Synthesis and biological evaluation of 14-alkoxymorphinans. 21. Novel 4-alkoxy and 14-phenylpropoxy derivatives of the mu opioid receptor antagonist cyprodime.
University of Innsbruck
A Novel Mitragynine Analog with Low-Efficacy Mu Opioid Receptor Agonism Displays Antinociception with Attenuated Adverse Effects.
University of Health Sciences & Pharmacy At St. Louis
A novel series of piperidin-4-yl-1,3-dihydroindol-2-ones as agonist and antagonist ligands at the nociceptin receptor.
Sri International
Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects.
Harbin Institute of Technology
Structure-Based Design and Optimization of FPPQ, a Dual-Acting 5-HT
Jagiellonian University Medical College
N-alkyl-4-[(8-azabicyclo[3.2.1]-oct-3-ylidene)phenylmethyl]benzamides, micro and delta opioid agonists: a micro address.
Johnson and Johnson Pharmaceutical Research and Development
N,N-dialkyl-4-[(8-azabicyclo[3.2.1]-oct-3-ylidene)phenylmethyl]benzamides, potent, selective delta opioid agonists.
Johnson and Johnson Pharmaceutical Research and Development
Pharmacological Analysis of the Anti-inflammatory and Antiallodynic Effects of Zinagrandinolide E from
Universidad Nacional Aut£Noma De M£Xico
Discovery, Structure-Activity Relationships, and In Vivo Evaluation of Novel Aryl Amides as Brain Penetrant Adaptor Protein 2-Associated Kinase 1 (AAK1) Inhibitors for the Treatment of Neuropathic Pain.
Bristol Myers Squibb
Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues.
Biological Research Center of The Hungarian Academy of Sciences
Synthesis and opioid activity of side-chain-to-side-chain cyclic dynorphin A-(1-11) amide analogues cyclized between positions 2 and 5. 1. Substitutions in position 3.
University of Maryland
Fentanyl derivatives bearing aliphatic alkaneguanidinium moieties: a new series of hybrid molecules with significant binding affinity for mu-opioid receptors and I2-imidazoline binding sites.
Instituto De QuíMica MéDica
10-Ketomorphinan and 3-substituted-3-desoxymorphinan analogues as mixed kappa and micro opioid ligands: synthesis and biological evaluation of their binding affinity at opioid receptors.
Harvard Medical School
Piperazinyl Bicyclic Derivatives as Selective Ligands of the α2δ-1 Subunit of Voltage-Gated Calcium Channels.
Welab Barcelona
Structure activity relationship of 3-nitro-2-(trifluoromethyl)-2H-chromene derivatives as P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Exploring naltrexamine derivatives featuring azaindole moiety via nitrogen-walk approach to investigate their in vitro pharmacological profiles at the mu opioid receptor.
Virginia Commonwealth University
Isolation and Pharmacological Characterization of Six Opioidergic
University of Illinois At Chicago
Effects of the substitution of Phe4 in the opioid peptide [D-Ala8]dynorphin A-(1-11)NH2.
University of Maryland
Design and parallel synthesis of piperidine libraries targeting the nociceptin (N/OFQ) receptor.
Purdue Pharma
Unique high-affinity synthetic mu-opioid receptor agonists with central- and systemic-mediated analgesia.
Kobe Gakuin University
Neuropeptide FF and Its Receptors: Therapeutic Applications and Ligand Development.
Research Triangle Institute
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 2: 8-formamidocyclazocine analogues.
Rensselaer Polytechnic Institute
Piperidine propionamide as a scaffold for potent sigma-1 receptor antagonists and mu opioid receptor agonists for treating neuropathic pain.
Huazhong University of Science and Technology
New scaffolds in the development of mu opioid-receptor ligands.
Astrazeneca R&D Montreal
A novel [5.2.1]bicyclic amine is a potent analgesic without µ opioid activity.
Daiichi Sankyo
Mechanism of action of the diazabicyclononanone-type kappa-agonists.
UniversitäT WüRzburg
A novel N-terminal cyclic dynorphin A analogue cyclo(N,5)[Trp(3),Trp(4),Glu(5)] dynorphin A-(1-11)NH(2) that lacks the basic N-terminus.
University of Maryland
Dermorphin tetrapeptide analogues with 2',6'-dimethylphenylalanine (Dmp) substituted for aromatic amino acids have high mu opioid receptor binding and biological activities.
Tohoku Pharmaceutical University
Synthesis and Biological activity of kappa opioid receptor agonists. Part 2: preparation of 3-aryl-2-pyridone analogues generated by solution- and solid-phase parallel synthesis methods.
Astrazeneca R&D
Amide Bond Bioisosteres: Strategies, Synthesis, and Successes.
University of Nebraska Medical Center
Bivalent Ligand Aiming Putative Mu Opioid Receptor and Chemokine Receptor CXCR4 Dimers in Opioid Enhanced HIV-1 Entry.
Virginia Commonwealth University
Discovery of SHR0687, a Highly Potent and Peripheral Nervous System-Restricted KOR Agonist.
Shanghai Hengrui Pharmaceutical
Exception That Proves the Rule: Investigation of Privileged Stereochemistry in Designing Dopamine D
National Institute On Drug Abuse-Intramural Research Program
Syntheses and opioid receptor binding affinities of 8-amino-2,6-methano-3-benzazocines.
Rensselaer Polytechnic Institute
Identification of arodyn, a novel acetylated dynorphin A-(1-11) analogue, as a kappa opioid receptor antagonist.
University of Maryland
Crystal structures of dipeptides containing the Dmt-Tic pharmacophore.
National Institute of Environmental Health Sciences
Small Molecules Selectively Targeting Sigma-1 Receptor for the Treatment of Neurological Diseases.
Soochow University
Synthetic Studies of Neoclerodane Diterpenes from Salvia divinorum: Identification of a Potent and Centrally Acting μ Opioid Analgesic with Reduced Abuse Liability.
The University of Kansas
Structure-Based Optimization of Multifunctional Agonists for Opioid and Neuropeptide FF Receptors with Potent Nontolerance Forming Analgesic Activities.
Lanzhou University
Synthesis and structure-activity relationships of an orally available and long-acting analgesic peptide, N(alpha)-amidino-Tyr-D-Arg-Phe-MebetaAla-OH (ADAMB).
Daiichi Fine Chemical
Exploration of bivalent ligands targeting putative mu opioid receptor and chemokine receptor CCR5 dimerization.
Virginia Commonwealth University
Opioid activity of 4-imidazolidinone positional analogues of Leu-Enkephalin.
Institute For Molecular Studies
Synthesis and structure--activity relationship of novel aminotetralin derivatives with high micro selective opioid affinity.
Shire Biochem
Solid phase synthesis and evaluation of Tyr-Tic-Phe-Phe(p-NHCOCH(2)Br) ([Phe(p-bromoacetamide)(4)]TIPP), a potent affinity label for delta opioid receptors.
University of Maryland
Synthesis and biological activities of cyclic lanthionine enkephalin analogues: delta-opioid receptor selective ligands.
University of California
Synthesis and Biological Characterization of Cyclic Disulfide-Containing Peptide Analogs of the Multifunctional Opioid/Neuropeptide FF Receptor Agonists That Produce Long-Lasting and Nontolerant Antinociception.
Lanzhou University
Synthesis and Pharmacology of a Novel μ-δ Opioid Receptor Heteromer-Selective Agonist Based on the Carfentanyl Template.
St Louis College of Pharmacy and Washington University
Optimized Opioid-Neurotensin Multitarget Peptides: From Design to Structure-Activity Relationship Studies.
Vrije Universiteit Brussel
Design and synthesis of a bivalent probe targeting the putative mu opioid receptor and chemokine receptor CXCR4 heterodimer.
Virginia Commonwealth University
Dermorphin and deltorphin heptapeptide analogues: replacement of Phe residue by Dmp greatly improves opioid receptor affinity and selectivity.
Tohoku Pharmaceutical University
Synthesis, biochemical, pharmacological characterization and in silico profile modelling of highly potent opioid orvinol and thevinol derivatives.
University of Szeged
Discovery of 3-((dimethylamino)methyl)-4-hydroxy-4-(3-methoxyphenyl)-N-phenylpiperidine-1-carboxamide as novel potent analgesic.
Fudan University
3-Aryl pyridone derivatives. Potent and selective kappa opioid receptor agonists.
Astrazeneca R&D MöLndal
Synthesis and biological activity of 8beta-substituted hydrocodone indole and hydromorphone indole derivatives.
Niddk
Synthesis, Biological, and Structural Explorations of New Zwitterionic Derivatives of 14- O-Methyloxymorphone, as Potent μ/δ Opioid Agonists and Peripherally Selective Antinociceptives.
TBA
Biased Agonism at Nociceptin/Orphanin FQ Receptors: A Structure Activity Study on N/OFQ(1-13)-NH
University of Ferrara
Discovery of DS34942424: An orally potent analgesic without mu opioid receptor agonist activity.
Daiichi Sankyo
Synthesis and Structure-Activity Relationships of 5'-Aryl-14-alkoxypyridomorphinans: Identification of a μ Opioid Receptor Agonist/δ Opioid Receptor Antagonist Ligand with Systemic Antinociceptive Activity and Diminished Opioid Side Effects.
University of Alabama At Birmingham
Discovery of δ opioid receptor full agonists lacking a basic nitrogen atom and their antidepressant-like effects.
Kitasato University
Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications.
Lanzhou University
Identification and Optimization of Pyrrolidine Derivatives as Highly Potent Ghrelin Receptor Full Agonists.
Astrazeneca
Novel C-terminus modifications of the Dmt-Tic motif: a new class of dipeptide analogues showing altered pharmacological profiles toward the opioid receptors.
Astrazeneca R&D Montreal
Synthesis of potent and selective dopamine D(4) antagonists as candidate radioligands.
Columbia University College of Physicians and Surgeons
Stepwise modulation of neurokinin-3 and neurokinin-2 receptor affinity and selectivity in quinoline tachykinin receptor antagonists.
Smithkline Beecham Pharmaceuticals
Design, synthesis and biological evaluation of N-hydroxy-aminobenzyloxyarylamide analogues as novel selective κ opioid receptor antagonists.
China Pharmaceutical University
8-Carboxamidocyclazocine analogues: redefining the structure-activity relationships of 2,6-methano-3-benzazocines.
Rensselaer Polytechnic Institute
Developing Cyclic Opioid Analogues: Fluorescently Labeled Bioconjugates of Biphalin.
D'Annunzio University of Chieti���Pescara
Enkephalin analogues with 2',6'-dimethylphenylalanine replacing phenylalanine in position 4.
Tohoku Pharmaceutical University
Stereospecific synthesis of (2S)-2-methyl-3-(2',6'-dimethyl-4'-hydroxyphenyl)-propionic acid (Mdp) and its incorporation into an opioid peptide.
Clinical Research Institute of Montreal
Extended TIP(P) analogues as precursors for labeled delta-opioid receptor ligands.
University of Maryland
Synthesis and evaluation of isothiocyanate-containing derivatives of the delta-opioid receptor antagonist Tyr-Tic-Phe-Phe (TIPP) as potential affinity labels for delta-opioid receptors.
University of Maryland
Synthesis and in vitro and in vivo activity of (-)-(1R,5R,9R)- and (+)-(1S,5S,9S)-N-alkenyl-, -N-alkynyl-, and -N-cyanoalkyl-5, 9-dimethyl-2'-hydroxy-6,7-benzomorphan homologues.
Virginia Commonwealth University
Isolation and Synthesis of Veranamine, an Antidepressant Lead from the Marine Sponge
University of Mississippi
4-Aminoquinolines: novel nociceptin antagonists with analgesic activity.
Central Pharmaceutical Research Institute
N,N-Diethyl-4-(phenylpiperidin-4-ylidenemethyl)benzamide: a novel, exceptionally selective, potent delta opioid receptor agonist with oral bioavailability and its analogues.
Astrazeneca R&D Montreal
New diarylmethylpiperazines as potent and selective nonpeptidic delta opioid receptor agonists with increased In vitro metabolic stability.
Astrazeneca R&D Montreal
Novel Cyclic Biphalin Analogues by Ruthenium-Catalyzed Ring Closing Metathesis:
D'Annunzio University of Chieti���Pescara
Dual Pharmacophores Explored via Structure-Activity Relationship (SAR) Matrix: Insights into Potent, Bifunctional Opioid Ligand Design.
TBA
Treatment of Pain with Spirocylic Cyclohexane Derivatives Having Dual Specificity for ORL-1 and μ-Opioid Receptors.
Dart Neuroscience
Potent and selective indolomorphinan antagonists of the kappa-opioid receptor.
University of Minnesota
An LP1 analogue, selective MOR agonist with a peculiar pharmacological profile, used to scrutiny the ligand binding domain.
University of Catania
Versatile Picklocks To Access All Opioid Receptors: Tuning the Selectivity and Functional Profile of the Cyclotetrapeptide c[Phe-d-Pro-Phe-Trp] (CJ-15,208).
University of Bologna
Mitragynine/Corynantheidine Pseudoindoxyls As Opioid Analgesics with Mu Agonism and Delta Antagonism, Which Do Not Recruit β-Arrestin-2.
Memorial Sloan Kettering Cancer Center
4-[(8-Alkyl-8-azabicyclo[3.2.1]octyl-3-yl)-3-arylanilino]-N,N-diethylbenzamides: high affinity, selective ligands for the delta opioid receptor illustrate factors important to antagonist activity.
Research Triangle Institute
Nociceptin Opioid Receptor (NOP) as a Therapeutic Target: Progress in Translation from Preclinical Research to Clinical Utility.
Astraea Therapeutics
Synthesis and binding affinities of 4-diarylaminotropanes, a new class of delta opioid agonists.
R. W. Johnson Pharmaceutical Research Institute
Synthesis, molecular modeling, and opioid receptor affinity of 9, 10-diazatricyclo[4.2.1.1(2,5)]decanes and 2,7-diazatricyclo[4.4.0. 0(3,8)]decanes structurally related to 3,8-diazabicyclo[3.2. 1]octanes.
Istituto Di Chimica Farmaceutica E Tossicologica
Design and Synthesis of a Novel and Selective Kappa Opioid Receptor (KOR) Antagonist (BTRX-335140).
The Scripps Research Institute
Synthesis of spiro-2,6-dioxopiperazine and spiro-2,6-dioxopyrazine scaffolds using amino acids in a three-component reaction to generate potential Sigma-1 (σ
Memorial Sloan Kettering Cancer Center
Deltorphin II analogues with 6-hydroxy-2-aminotetralin-2-carboxylic acid in position 1.
Hungarian Academy of Sciences
Design, synthesis and biological evaluation of 3-amino-3-phenylpropionamide derivatives as novel mu opioid receptor ligands.
Pfizer
Opiate aromatic pharmacophore structure-activity relationships in CTAP analogues determined by topographical bias, two-dimensional NMR, and biological activity assays.
University of Arizona
Novel Dmt-Tic dipeptide analogues as selective delta-opioid receptor antagonists.
Astrazeneca R&D MontréAl
Discovery of Axelopran (TD-1211): A Peripherally Restricted μ-Opioid Receptor Antagonist.
Theravance Biopharma Us
Synthesis and μ-Opioid Activity of the Primary Metabolites of Carfentanil.
United States Army Ccdc Chemical Biological Center
Exploring the structure-activity relationships of [1-(4-tert-butyl-3'-hydroxy)benzhydryl-4-benzylpiperazine] (SL-3111), a high-affinity and selective delta-opioid receptor nonpeptide agonist ligand.
The University of Arizona
Discovery of a novel bicyclic compound, DS54360155, as an orally potent analgesic without mu-opioid receptor agonist activity.
Daiichi Sankyo
Synthesis and biological activities of position one and three transposed analogs of the opioid peptide YKFA.
University of Louisville
Progress in the development of more effective and safer analgesics for pain management.
University of Catania
Synthesis and opiate receptor binding properties of 17-methyl-6,7-dehydro-3,14-dihydroxy-4,5alpha-epoxy-6,7:4',5'-pyrimidin omorphinans.
University of Illinois At Chicago
Discovery of dual-acting opioid ligand and TRPV1 antagonists as novel therapeutic agents for pain.
Seoul National University
Discovery of the first potent and selective small molecule opioid receptor-like (ORL1) antagonist: 1-[(3R,4R)-1-cyclooctylmethyl-3- hydroxymethyl-4-piperidyl]-3-ethyl-1, 3-dihydro-2H-benzimidazol-2-one (J-113397).
Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories
Further studies on the Dmt-Tic pharmacophore: hydrophobic substituents at the C-terminus endow delta antagonists to manifest mu agonism or mu antagonism.
University of Ferrara
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 3. Approaches to eliminate opioid agonist metabolites by using substituted phenylpiperazine side chains.
Synaptic Pharmaceutical
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.
Synaptic Pharmaceutical
Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective D
National Institute of Neurological Disorders and Stroke
Potent, Efficacious, and Stable Cyclic Opioid Peptides with Long Lasting Antinociceptive Effect after Peripheral Administration.
D'Annunzio University of Chieti���Pescara
Biological activity of fragments and analogues of the potent dimeric opioid peptide, biphalin.
University of Arizona
The opioid mu agonist/delta antagonist DIPP-NH(2)[Psi] produces a potent analgesic effect, no physical dependence, and less tolerance than morphine in rats.
Clinical Research Institute of Montreal
Endomorphin-2 analogs containing modified tyrosines: Biological and theoretical investigation of the influence on conformation and pharmacological profile.
Medical University of Lodz
Tetrahydro-3-benzazepines with fluorinated side chains as NMDA and σ
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
A novel acetylated analogue of dynorphin A-(1-11) amide as a kappa-opioid receptor antagonist.
TBA
Defining Structure-Functional Selectivity Relationships (SFSR) for a Class of Non-Catechol Dopamine D
University of North Carolina At Chapel Hill
The in vivo antinociceptive and μ-opioid receptor activating effects of the combination of N-phenyl-2',4'-dimethyl-4,5'-bi-1,3-thiazol-2-amines and naloxone.
National Health Research Institutes
Discovery of conolidine derivative DS39201083 as a potent novel analgesic without mu opioid agonist activity.
Daiichi Sankyo
Synthesis of novel analogues of the delta opioid ligand SNC-80 using AlCl3-promoted aminolysis.
Organon Laboratories
Synthesis and Structure-Affinity Relationships of Spirocyclic Benzopyrans with Exocyclic Amino Moiety.
Universit£T M£Nster
Structural Simplification of a Tetrahydroquinoline-Core Peptidomimetic μ-Opioid Receptor (MOR) Agonist/δ-Opioid Receptor (DOR) Antagonist Produces Improved Metabolic Stability.
University of Michigan
Aromatic-Amine Pendants Produce Highly Potent and Efficacious Mixed Efficacy μ-Opioid Receptor (MOR)/δ-Opioid Receptor (DOR) Peptidomimetics with Enhanced Metabolic Stability.
University of Michigan
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
University of Florida
Dermorphin and deltorphin glycosylated analogues: synthesis and antinociceptive activity after systemic administration.
Sapienza University of Rome
Development of Novel Quinoxaline-Based κ-Opioid Receptor Agonists for the Treatment of Neuroinflammation.
Universit£T M£Nster
N-substituted octahydro-4a-(3-hydroxyphenyl)-10a-methyl-benzo[g]isoquinolines are opioid receptor pure antagonists.
Research Triangle Institute
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.
Shanghaitech University
Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design.
Bristol-Myers Squibb
Functionalized 6-(Piperidin-1-yl)-8,9-Diphenyl Purines as Peripherally Restricted Inverse Agonists of the CB1 Receptor.
Rti International
C-alkylated spiro[benzofuran-3(2H),4'-1'-methyl-piperidine-7-ols] as potent opioids: a conformation-activity study.
National Taiwan University
Preparation of bivalent agonists for targeting the mu opioid and cannabinoid receptors.
Biological Research Centre of The Hungarian Academy of Sciences
Discovery of a Thiadiazole-Pyridazine-Based Allosteric Glutaminase 1 Inhibitor Series That Demonstrates Oral Bioavailability and Activity in Tumor Xenograft Models.
Astrazeneca
Discovery and Structure-Activity Relationships of Nociceptin Receptor Partial Agonists That Afford Symptom Ablation in Parkinson's Disease Models.
Astraea Therapeutics
Modifications of the 4,4'-residues and SAR studies of Biphalin, a highly potent opioid receptor active peptide.
University of Arizona
4-Aryl-1-oxa-4,9-diazaspiro[5.5]undecane Derivatives as Dual μ-Opioid Receptor Agonists and σ
Esteve Pharmaceuticals
De novo design, synthesis, and biological activities of high-affinity and selective non-peptide agonists of the delta-opioid receptor.
The University of Arizona
N-Substituted 9beta-methyl-5-(3-hydroxyphenyl)morphans are opioid receptor pure antagonists.
Research Triangle Institute
Investigation of Inactive-State κ Opioid Receptor Homodimerization via Single-Molecule Microscopy Using New Antagonistic Fluorescent Probes.
Julius Maximilian University of W£Rzburg
Investigation of the N-substituent conformation governing potency and mu receptor subtype-selectivity in (+)-(3R, 4R)-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonists.
Research Triangle Institute
(2S)-N-2-methoxy-2-phenylethyl-6,7-benzomorphan compound (2S-LP2): Discovery of a biased mu/delta opioid receptor agonist.
University of Catania
Discovery of Benzamidine- and 1-Aminoisoquinoline-Based Human MAS-Related G-Protein-Coupled Receptor X1 (MRGPRX1) Agonists.
Eisai
Multi-target-directed-ligands acting as enzyme inhibitors and receptor ligands.
Julius Maximilian University of W£Rzburg
Discovery of two novel branched peptidomimetics containing endomorphin-2 and RF9 pharmacophores: Synthesis and neuropharmacological evaluation.
Lanzhou University
Design, Synthesis, and Biological Evaluation of the Third Generation 17-Cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-[(4'-pyridyl)carboxamido]morphinan (NAP) Derivatives as μ/κ Opioid Receptor Dual Selective Ligands.
Virginia Commonwealth University
7-spirobenzocyclohexyl derivatives of naltrexone, oxymorphone, and hydromorphone as selective opioid receptor ligands.
University of Minnesota
Synthesis and structure-activity relationships of 6,7-benzomorphan derivatives as antagonists of the NMDA receptor-channel complex.
Boehringer Ingelheim Pharmaceuticals
Synthesis and opioid activity of [D-Pro10]dynorphin A-(1-11) analogues with N-terminal alkyl substitution.
Oregon State University
Helix-inducing alpha-aminoisobutyric acid in opioid mimetic deltorphin C analogues.
National Institute of Environmental Health Sciences
Application of Bivalent Bioisostere Concept on Design and Discovery of Potent Opioid Receptor Modulators.
Virginia Commonwealth University
Discovery of a Highly Selective and Potent κ Opioid Receptor Agonist from
Fudan University
Benzyl Phenylsemicarbazides: A Chemistry-Driven Approach Leading to G Protein-Biased Dopamine D
Friedrich-Alexander-Universit£T Erlangen-N£Rnberg
Synthesis and opioid activity of conformationally constrained dynorphin A analogues. 2. Conformational constraint in the"address" sequence.
Oregon State University
Conformationally constrained deltorphin analogs with 2-aminotetralin-2-carboxylic acid in position 3.
Hungarian Academy of Sciences
Aspartic acid conjugates of 2-(3,4-dichlorophenyl)-N-methyl-N-[(1S)-1(3-aminophenyl)-2-(1-pyrrolidi nyl) ethyl]acetamide: kappa opioid receptor agonists with limited access to the central nervous system.
University of Minnesota
Discovery of naldemedine: A potent and orally available opioid receptor antagonist for treatment of opioid-induced adverse effects.
Shionogi
3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HT
University of Minnesota Twin Cities
Effects of modifications of residues in position 3 of dynorphin A(1-11)-NH2 on kappa receptor selectivity and potency.
University of Arizona
Design, synthesis, and biological activities of cyclic lactam peptide analogues of dynorphine A(1-11)-NH2.
University of Arizona
Asymmetric syntheses, opioid receptor affinities, and antinociceptive effects of 8-amino-5,9-methanobenzocyclooctenes, a new class of structural analogues of the morphine alkaloids.
Institute
Enkephalin analogues with N-phenyl-N-(piperidin-2-ylmethyl)propionamide derivatives: Synthesis and biological evaluations.
University of Arizona
Synthesis, biological evaluation, and quantitative receptor docking simulations of 2-[(acylamino)ethyl]-1,4-benzodiazepines as novel tifluadom-like ligands with high affinity and selectivity for kappa-opioid receptors.
Universitá
Design and synthesis of 1-aminocycloalkane-1-carboxylic acid-substituted deltorphin analogues: unique delta and mu opioid activity in modified peptides.
University of Ferrara
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
Hoechst-Roussel Pharmaceuticals
Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example.
Janssen Pharmaceutica
Discovery of Novel Multifunctional Ligands with μ/δ Opioid Agonist/Neurokinin-1 (NK1) Antagonist Activities for the Treatment of Pain.
University of Arizona
Discovery of tripeptide-derived multifunctional ligands possessing delta/mu opioid receptor agonist and neurokinin 1 receptor antagonist activities.
University of Arizona
Synthesis of tripeptides containing D-Trp substituted at the indole ring, assessment of opioid receptor binding and in vivo central antinociception.
University of Bologna
3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity.
Eli Lilly
Structure-activity relationships of trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine antagonists for mu- and kappa-opioid receptors.
Eli Lilly
A Bivalent Ligand Targeting the Putative Mu Opioid Receptor and Chemokine Receptor CCR5 Heterodimers: Binding Affinity versus Functional Activities.
Virginia Commonwealth University
Synthesis and binding properties of MK-801 isothiocyanates; (+)-3-isothiocyanato-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten- 5,10-imine hydrochloride: a new, potent and selective electrophilic affinity ligand for the NMDA receptor-coupled phencyclidine binding site.
National Institute of Diabetes and Digestive and Kidney Diseases
Potential Drug Abuse Therapeutics Derived from the Hallucinogenic Natural Product Salvinorin A.
University of Kansas
Design of cyclic deltorphins and dermenkephalins with a disulfide bridge leads to analogues with high selectivity for delta-opioid receptors.
University of Arizona
Phe3-substituted analogues of deltorphin C. Spatial conformation and topography of the aromatic ring in peptide recognition by delta opioid receptors.
University of Ferrara
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
Solvay Duphar
Synthesis and evaluation of 4-substituted piperidines and piperazines as balanced affinity μ opioid receptor (MOR) agonist/δ opioid receptor (DOR) antagonist ligands.
University of Michigan
2-(3,4-Dichlorophenyl)-N-methyl-N-[(1S)-1-(3-isothiocyanatophenyl)-2-(1-pyrrolidinyl)ethyl]acetamide: an opioid receptor affinity label that produces selective and long-lasting kappa antagonism in mice.
University of Minnesota
The most effective influence of 17-(3-ethoxypropyl) substituent on the binding affinity and the agonistic activity in KNT-127 derivatives, δ opioid receptor agonists.
Kitasato University
Novel glycosylated endomorphin-2 analog produces potent centrally-mediated antinociception in mice after peripheral administration.
Medical University of Lodz
Design, synthesis, and biological evaluation of 14-heteroaromatic-substituted naltrexone derivatives: pharmacological profile switch from mu opioid receptor selectivity to mu/kappa opioid receptor dual selectivity.
Virginia Commonwealth University
Synthesis and pharmacological evaluation of aminothiazolomorphinans at the mu and kappa opioid receptors.
Harvard Medical School
4β-Methyl-5-(3-hydroxyphenyl)morphan opioid agonist and partial agonist derived from a 4β-methyl-5-(3-hydroxyphenyl)morphan pure antagonist.
Research Triangle Institute
N-Alkyl dien- and trienamides from the roots of Otanthus maritimus with binding affinity for opioid and cannabinoid receptors.
Uos of Cagliari
Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain.
Trevena
Synthesis and opioid activity of dynorphin A-(1-13)NH2 analogues containing cis- and trans-4-aminocyclohexanecarboxylic acid.
Oregon State University
Binding mode characterization of 6α- and 6β-N-heterocyclic substituted naltrexamine derivatives via docking in opioid receptor crystal structures and site-directed mutagenesis studies: application of the 'message-address' concept in development of mu opioid receptor selective antagonists.
Virginia Commonwealth University
Design and synthesis of highly potent and selective cyclic dynorphin A analogs. 2. New analogs.
University of Arizona
Synthesis and biological evaluation of novel delta (δ) opioid receptor ligands with diazatricyclodecane skeletons.
C.N.R. Istituto Di Farmacologia Traslazionale
Discovery of a potent, peripherally selective trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonist for the treatment of gastrointestinal motility disorders.
Eli Lilly
Hybrid peptides endomorphin-2/DAMGO: design, synthesis and biological evaluation.
D'Annunzio University of Chieti���Pescara
Structure activity relationship studies of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3'-carboxamido)morphinan (NAQ) analogues as potent opioid receptor ligands: preliminary results on the role of electronic characteristics for affinity and function.
Virginia Commonwealth University
N-terminal guanidinylation of TIPP (Tyr-Tic-Phe-Phe) peptides results in major changes of the opioid activity profile.
Clinical Research Institute of Montreal
Access to 7β-analogs of codeine with mixed μ/δ agonist activity via 6,7-α-epoxide opening.
University of Texas At Austin
Probes for narcotic receptor mediated phenomena. 48. C7- and C8-substituted 5-phenylmorphan opioids from diastereoselective alkylation.
National Institute On Drug Abuse and The National Institute On Alcohol Abuse and Alcoholism
Development of a model for the delta opioid receptor pharmacophore. 2. Conformationally restricted Phe3 replacements in the cyclic delta receptor selective tetrapeptide Tyr-c[D-Cys-Phe-D-Pen]OH (JOM-13).
University of Michigan
Development of a model for the delta opioid receptor pharmacophore. 1. Conformationally restricted Tyr1 replacements in the cyclic delta receptor selective tetrapeptide Tyr-c[D-Cys-Phe-D-Pen]OH (JOM-13).
University of Michigan
Effect of ring-constrained phenylpropyloxyethylamines on sigma receptors.
University of Maryland
Design, synthesis, and biological properties of highly potent cyclic dynorphin A analogues. Analogues cyclized between positions 5 and 11.
University of Arizona
Sandmeyer reaction repurposed for the site-selective, non-oxidizing radioiodination of fully-deprotected peptides: studies on the endogenous opioid peptide α-neoendorphin.
Memorial Sloan-Kettering Cancer Center
Structural and biological exploration of phe(3)-phe(4)-modified endomorphin-2 peptidomimetics.
University of Milan
Cyclic enkephalins with a diversely substituted guanidine bridge or a thiourea bridge: synthesis, biological and structural evaluations.
University of Montpellier
Synthesis and changes in affinity for NOP and opioid receptors of novel hexapeptides containing β(2)-tryptophan analogues.
Bulgarian Academy of Sciences
Selective kappa-opioid agonists: synthesis and structure-activity relationships of piperidines incorporating on oxo-containing acyl group.
Smithkline Beecham Farmaceutici
Opioid receptor selectivity profile change via isosterism for 14-O-substituted naltrexone derivatives.
Virginia Commonwealth University
A marked change of receptor affinity of the 2-methyl-5-(3-hydroxyphenyl)morphans upon attachment of an (E)-8-benzylidene moiety: synthesis and evaluation of a new class of sigma receptor ligands.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and opioid activity of 7-oxygenated 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolin-9-ols.
National Taiwan University
Enkephalin analogs as systemically active antinociceptive agents: O- and N-alkylated derivatives of the dipeptide amide L-2,6-dimethyltyrosyl-N-(3-phenylpropyl)-D-alaninamide.
Searle
Design and synthesis of novel opioid ligands with an azabicyclo[2.2.2]octane skeleton having a 7-amide side chain and their pharmacologies.
Kitasato University
Probes for narcotic receptor mediated phenomena. 47. Novel C4a- and N-substituted-1,2,3,4,4a,9a-hexahydrobenzofuro[2,3-c]pyridin-6-ols.
National Institute On Drug Abuse and The National Institute On Alcohol Abuse and Alcoholism
Highly kappa receptor-selective dynorphin A analogues with modifications in position 3 of dynorphin A(1-11)-NH2.
University of Arizona
Kappa-opioid receptor-selective dicarboxylic ester-derived salvinorin A ligands.
University of Mississippi
kappa Opioid receptor selective affinity labels: electrophilic benzeneacetamides as kappa-selective opioid antagonists.
University of Minnesota
Electrophilic N-benzylnaltrindoles as delta opioid receptor-selective antagonists.
University of Minnesota
Opioid receptor binding requirements for the delta-selective peptide deltorphin. I: Phe3 replacement with ring-substituted and heterocyclic amino acids.
Eastern Michigan University
14 beta-[(p-nitrocinnamoyl)amino]morphinones, 14 beta-[(p-nitrocinnamoyl)amino]-7,8-dihydromorphinones, and their codeinone analogues: synthesis and receptor activity.
Institute
Stereoisomers of N-[1-hydroxy-(2-phenylethyl)-3-methyl-4-piperidyl]- N-phenylpropanamide: synthesis, stereochemistry, analgesic activity, and opioid receptor binding characteristics.
Institute of Materia Medica
Synthesis using a Fmoc-based strategy and biological activities of some reduced peptide bond pseudopeptide analogues of dynorphin A1.
University of Arizona
Synthesis and opioid activity of conformationally constrained dynorphin A analogues. 1. Conformational constraint in the"message" sequence.
Oregon State University
Novel deltorphin heptapeptide analogs with potent delta agonist, delta antagonist, or mixed mu antagonist/delta agonist properties.
Tohoku College of Pharmacy
(E)-8-benzylidene derivatives of 2-methyl-5-(3-hydroxyphenyl)morphans: highly selective ligands for the sigma 2 receptor subtype.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and pharmacological properties of novel hydrophilic 5-HT4 receptor antagonists.
Drug Discovery Laboratory
Structure-activity relationships and CoMFA of N-3 substituted phenoxypropyl piperidine benzimidazol-2-one analogues as NOP receptor agonists with analgesic properties.
Organon Laboratories
o-Naphthalenedicarboxaldehyde derivative of 7'-aminonaltrindole as a selective delta-opioid receptor affinity label.
University of Minnesota
Synthesis and pharmacological characterization of (+/-)-5,9 alpha-dimethyl-2-[2-(4-fluorophenyl)ethyl]-2'-hydroxy-6,7-benzomorphan (fluorophen), a ligand suitable for visualization of opiate receptors in vivo.
TBA
Major effect of pyrrolic N-benzylation in norbinaltorphimine, the selective kappa-opioid receptor antagonist.
University of Bath
Novel hexahydrospiro[piperidine-4,1'-pyrrolo[3,4-c]pyrroles]: highly selective small-molecule nociceptin/orphanin FQ receptor agonists.
F. Hoffmann-La Roche
Studies on the synthesis and opioid agonistic activities of mitragynine-related indole alkaloids: discovery of opioid agonists structurally different from other opioid ligands.
Chiba University
Design and synthesis of naltrexone-derived affinity labels with nonequilibrium opioid agonist and antagonist activities. Evidence for the existence of different mu receptor subtypes in different tissues.
TBA
Biodegradable Amphipathic Peptide Hydrogels as Extended-Release System for Opioid Peptides.
Vrije Universiteit Brussel
Analogs of penfluridol as chemotherapeutic agents with reduced central nervous system activity.
Texas Tech University Health Sciences Center
Selective kappa opioid antagonists for treatment of addiction, are we there yet?
University of Science and Technology
7β-Methyl substituent is a structural locus associated with activity cliff for nepenthone analogues.
Fudan University
Optimization of a Series of Mu Opioid Receptor (MOR) Agonists with High G Protein Signaling Bias.
The Scripps Research Institute
Benzomorphan scaffold for opioid analgesics and pharmacological tools development: A comprehensive review.
University of Catania
Opioid agonist and antagonist bivalent ligands. The relationship between spacer length and selectivity at multiple opioid receptors.
TBA
Cyclic Biphalin Analogues Incorporating a Xylene Bridge: Synthesis, Characterization, and Biological Profile.
D'Annunzio University of Chieti���Pescara
Design, synthesis, and opioid activity of arodyn analogs cyclized by ring-closing metathesis involving Tyr(allyl).
University of Kansas
Original endomorphin-1 analogues exhibit good analgesic effects.
The First Hospital of Lanzhou University
Design and synthesis of somatostatin analogues with topographical properties that lead to highly potent and specific mu opioid receptor antagonists with greatly reduced binding at somatostatin receptors.
University of Arizona
Synthesis and biological activities of dynorphin A analogues with opioid antagonist properties.
TBA
Development of conformationally constrained linear peptides exhibiting a high affinity and pronounced selectivity for delta opioid receptors.
Ua 498 Cnrs
Synthesis, Receptor Affinity, and Antiallodynic Activity of Spirocyclic σ Receptor Ligands with Exocyclic Amino Moiety.
Universit£T M£Nster
Structure-activity relationships of cyclic opioid peptide analogues containing a phenylalanine residue in the 3-position.
Clinical Research Institute of Montreal
Synthesis of 7β-hydroxy-8-ketone opioid derivatives with antagonist activity at mu- and delta-opioid receptors.
University of Helsinki
Constraining Endomorphin-1 by β,α-Hybrid Dipeptide/Heterocycle Scaffolds: Identification of a Novel κ-Opioid Receptor Selective Partial Agonist.
University of Bologna
New 4-(heteroanilido)piperidines, structurally related to the pure opioid agonist fentanyl, with agonist and/or antagonist properties.
Boc Technical Center
Dermorphin analogues carrying an increased positive net charge in their"message" domain display extremely high mu opioid receptor selectivity.
Clinical Research Institute of Montreal
Synthesis and Evaluation of a Novel Bivalent Selective Antagonist for the Mu-Delta Opioid Receptor Heterodimer that Reduces Morphine Withdrawal in Mice.
TBA
Selectivity Challenges in Docking Screens for GPCR Targets and Antitargets.
University of California San Francisco
Identification and Pharmacological Profile of an Indane Based Series of Ghrelin Receptor Full Agonists.
Astrazeneca
χ-Space Screening of Dermorphin-Based Tetrapeptides through Use of Constrained Arylazepinone and Quinolinone Scaffolds.
Vrije Universiteit Brussel
Cyclic biphalin analogues with a novel linker lead to potent agonist activities at mu, delta, and kappa opioid receptors.
University of Arizona
Synthesis and pharmacological evaluation of a series of new 3-methyl-1,4-disubstituted-piperidine analgesics.
Anaquest Pharmaceuticals
Identification and biological evaluation of thiazole-based inverse agonists of RORγt.
Phenex Pharmaceuticals
Development of novel LP1-based analogues with enhanced delta opioid receptor profile.
University of Catania
Discovery of highly selectiveκ-opioid receptor agonists: 10α-Hydroxy TRK-820 derivatives.
Toray Industries
Design, synthesis and biological evaluation of aminobenzyloxyarylamide derivatives as selectiveκ opioid receptor antagonists.
China Pharmaceutical University
Design and synthesis of highly potent and selective cyclic dynorphin A analogues.
University of Arizona
Synthesis and structure-activity relationships of dynorphin A-(1-8) amide analogues.
Eisai
Modification of the enkephalin"message" with an artificial polycationic C-terminus.
Case Western Reserve University
Antitrichomonal activity ofδ opioid receptor antagonists, 7-benzylidenenaltrexone derivatives.
University of Tsukuba
New 1-(heterocyclylalkyl)-4-(propionanilido)-4-piperidinyl methyl ester and methylene methyl ether analgesics.
Anaquest
(2S)-1-(arylacetyl)-2-(aminomethyl)piperidine derivatives: novel, highly selective kappa opioid analgesics.
Zambeletti Research Laboratories
Hydrophilic, Potent, and Selective 7-Substituted 2-Aminoquinolines as Improved Human Neuronal Nitric Oxide Synthase Inhibitors.
Northwestern University
Original endomorphin-1 analogues exhibit good analgesic effects with minimal implications for human sperm motility.
The Reproductive Medicine Special Hospital of The First Hospital of Lanzhou University
Design and characterization of opioid ligands based on cycle-in-macrocycle scaffold.
Medical University of Lodz
Modulation of opioid receptor affinity and efficacy via N-substitution of 9β-hydroxy-5-(3-hydroxyphenyl)morphan: Synthesis and computer simulation study.
National Institute On Drug Abuse and The National Institute On Alcohol Abuse
Pseudopeptide analogues of substance P and leucine enkephalinamide containing the psi (CH2O) modification: synthesis and biological activity.
Hebrew University of Jerusalem
Separation of alpha 1 adrenergic and N-methyl-D-aspartate antagonist activity in a series of ifenprodil compounds.
Pfizer
Design and synthesis of novelδ opioid receptor agonists with an azatricyclodecane skeleton for improving blood-brain barrier penetration.
Nippon Chemiphar
Common stereospecificity of opioid and dopamine systems for N-butyrophenone prodine-like compounds.
Istituto Superiore Di Sanità
Conformational restriction of the phenylalanine residue in a cyclic opioid peptide analogue: effects on receptor selectivity and stereospecificity.
Clinical Research Institute of Montreal
(1S)-1-(aminomethyl)-2-(arylacetyl)-1,2,3,4-tetrahydroisoquinoline and heterocycle-condensed tetrahydropyridine derivatives: members of a novel class of very potent kappa opioid analgesics.
Zambeletti Research Laboratories
Novel delta opioid receptor agonists with oxazatricyclodecane structure showing potent agonistic activities.
Kitasato University
Naphtho and benzo analogues of the kappa opioid agonist trans-(+/-)-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl] benzeneacetamide.
University of Notre Dame
Synthesis, Pharmacology, and Molecular Docking Studies on 6-Desoxo-N-methylmorphinans as Potentμ-Opioid Receptor Agonists.
University of Innsbruck
The Necessary Nitrogen Atom: A Versatile High-Impact Design Element for Multiparameter Optimization.
Alkermes
Structure-Activity Relationships and Computational Investigations into the Development of Potent and Balanced Dual-Acting Butyrylcholinesterase Inhibitors and Human Cannabinoid Receptor 2 Ligands with Pro-Cognitive in Vivo Profiles.
Julius Maximilian University of W£Rzburg
Discovery of N-substituted-endo-3-(8-aza-bicyclo[3.2.1]oct-3-yl)-phenol and -phenyl carboxamide series ofμ-opioid receptor antagonists.
Theravance Biopharma Us
Effect of modification of the basic residues of dynorphin A-(1-13) amide on kappa opioid receptor selectivity and opioid activity.
Oregon State University
Preparation and opioid activity of analogues of the analgesic dipeptide 2,6-dimethyl-L-tyrosyl-N-(3-phenylpropyl)-D-alaninamide.
G.D. Searle And
Highly Potent and Selective New Diphenethylamines Interacting with theκ-Opioid Receptor: Synthesis, Pharmacology, and Structure-Activity Relationships.
University of Innsbruck
Discovery and Characterization of (R)-6-Neopentyl-2-(pyridin-2-ylmethoxy)-6,7-dihydropyrimido[2,1-c][1,4]oxazin-4(9H)-one (PF-06462894), an Alkyne-Lacking Metabotropic Glutamate Receptor 5 Negative Allosteric Modulator Profiled in both Rat and Nonhuman Primates.
Pfizer
Para-substituted Phe3 deltorphin analogues: enhanced selectivity of halogenated derivatives for delta opioid receptor sites.
University of Ferrara
Conformationally restricted deltorphin analogues.
Clinical Research Institute of Montreal
Ring substituted and other conformationally constrained tyrosine analogues of [D-Pen2,D-Pen5]enkephalin with delta opioid receptor selectivity.
University of Arizona
Phenylmorphans and analogues: opioid receptor subtype selectivity and effect of conformation on activity.
Harvard Medical School
Stereospecificity of amino acid side chains in deltorphin defines binding to opioid receptors.
National Institute of Environmental Health Sciences
Synthesis and evaluation of a ligand targeting theμ andδ opioid receptors for drug delivery to lung cancer.
Purdue University
SPIROCYCLIC MODULATORS OF CHOLESTEROL BIOSYNTHESIS AND THEIR USE FOR PROMOTING REMYELINATION
Genentech
SELECTIVE MODULATORS OF ATAXIA TELANGIECTASIA MUTATED (ATM) KINASE AND USES THEREOF
Suzhou Zanrong Pharma
Nitrogen Containing 2,3-Dihydroquinazolinone Compounds as Nav1.8 Inhibitors
Glaxosmithkline Intellectual Property Development
THYROID HORMONE RECEPTOR b SELECTIVE AGONIST COMPOUND, PHARMACEUTICAL COMPOSITION AND USE THEREOF
Shanghai Institute of Materia Medica
Substituted nicotinimide inhibitors of BTK for treating cancer
Guangzhou Innocare Pharma Tech Co.
Small molecule inhibition of transcription factor SALL4 and uses thereof
Dana-Farber Cancer Institute
Substituted pyrazolopyrimidines and substituted purines and their use as ubiquitin-specific-processing protease 1 (USP1) inhibitors
Ksq Therapeutics
Treatment of relapsed and/or refractory solid tumors and non-Hodgkin's lymphomas
Celgene Quanticel Research
Isoidide derivatives and methods of making and using same
Rutgers, The State University of New Jersey
Thiazolidinedione derivative and use thereof
Industry-Academic Cooperation Foundation Chosun University
Substituted bicycle heterocyclic derivatives useful as ROMK channel inhibitors
Bristol-Myers Squibb
Compounds and methods for the enhanced degradation of targeted proteins
Arvinas Operations
C5-C6-oxacyclic fused iminothiazine dioxide compounds bearing an ether linker as BACE inhibitors, compositions, and their use
Merck Sharp & Dohme
Tetrazole containing apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
Enanta Pharmaceuticals
Identification of Antiviral Drug Candidates against SARS-CoV-2 from FDA-Approved Drugs.
Institut Pasteur Korea
Substituted bicyclic fused ring compounds as indoleamine-2,3-dioxygenase inhibitors
Iomet Pharma
1-[2-(aminomethyl)benzyl]-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-ones as inhibitors of myeloperoxidase
Astrazeneca
Aminoindane-, aminotetrahydronaphthalene- and aminobenzocyclobutane-derived PRMT5-inhibitors
Ctxt
Indazolecarboxamides, processes for their preparation, pharmaceutical preparations comprising them and their use for producing medicaments
Bayer Pharma Aktiengesellschaft
8-(piperazin-1-yl)-1,2,3,4-tetrahydro-isoquinoline derivatives
Idorsia Pharmaceuticals
Substituted indazole compounds as RORgammaT inhibitors and uses thereof
Merck Sharp & Dohme
Substituted phenyl alkanoic acid compounds as GPR120 agonists and uses thereof
Piramal Enterprises
Methyl- and trifluoromethyl-substituted pyrrolopyridine modulators of RORC2 and methods of use therof
Pfizer
Methods of treating a cancer using substituted pyrrolopyrimidine compounds, compositions thereof
Signal Pharmaceuticals
OCT3 activity inhibitor containing imidazopyridine derivative as active component, and OCT3 detection agent
Shin Nippon Biomedical Laboratories
Imidazopyridine macrocycles as inhibitors of human immunodeficiency virus replication
Viiv Healthcare UK (NO.5)
Antileishmanial activity evaluation of bis-lawsone analogs and DNA topoisomerase-I inhibition studies.
Karunya University
A screening assay for neuraminidase inhibitors using neuraminidases N1 and N3 from a baculovirus expression system.
Chulalongkorn University
Tetracyclic heterocycle compounds and methods of use thereof for the treatment of viral diseases
Merck Sharp & Dohme
Design, synthesis, and preliminary bioactivity evaluation of N(1) -hydroxyterephthalamide derivatives with indole cap as novel histone deacetylase inhibitors.
Shandong University
N2,N4-bis(4-(piperazine-1-yl)phenyl)pirimidine-2,4-diamine derivative or pharmaceutically acceptable salt thereof, and composition containing same as active ingredient for preventing or treating cancer
Korea Research Institute of Chemical Technology
Inhibitors of Glycogen Synthase Kinase 3 with Exquisite Kinome-Wide Selectivity and Their Functional Effects.
Harvard Medical School
Pyridone and pyridazinone derivatives as anti-obesity agents
Boehringer Ingelheim International
Effects of novel diarylpentanoid analogues of curcumin on secretory phospholipase A2 , cyclooxygenases, lipo-oxygenase, and microsomal prostaglandin E synthase-1.
Universiti Kebangsaan Malaysia, Jalan Raja Muda Abdul Aziz, 50300, Kuala Lumpur, Malaysia
Epiminocycloalkyl[b] indole derivatives as serotonin sub-type 6 (5-HT6) modulators and uses thereof
Albany Molecular Research
Insights from selective non-phosphinic inhibitors of MMP-12 tailored to fit with an S1' loop canonical conformation.
French Alternative Energies and Atomic Energy Commission
Thioether metabolites of 3,4-methylenedioxyamphetamine and 3,4-methylenedioxymethamphetamine inhibit human serotonin transporter (hSERT) function and simultaneously stimulate dopamine uptake into hSERT-expressing SK-N-MC cells.
University of Texas At Austin
SCH 206272: a potent, orally active tachykinin NK(1), NK(2), and NK(3) receptor antagonist.
Schering-Plough Research Institute
Native gamma-aminobutyric acid type A receptors from rat hippocampus, containing both alpha 1 and alpha 5 subunits, exhibit a single benzodiazepine binding site with alpha 5 pharmacological properties.
Universidad De Sevilla
A new series of S-adenosyl-L-methionine synthetase inhibitors.
Laboratoire De Chimie Bioorganique
Optimization of 3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines as potent, orally active CCK-A agonists.
Glaxo Wellcome Research and Development
The putative 5-HT1A receptor antagonist DU125530 blocks the discriminative stimulus of the 5-HT1A receptor agonist flesinoxan in pigeons.
Cns-Pharmacology
Cloning and characterization of a mammalian melatonin receptor that mediates reproductive and circadian responses.
Massachusetts General Hospital
Molecular characterization of a second melatonin receptor expressed in human retina and brain: the Mel1b melatonin receptor.
Massachusetts General Hospital
The binding of [3H]nitrendipine to receptors for calcium channel antagonists in the heart, cerebral cortex, and ileum of rats.
University of Arizona
The binding of [3H]-prostacyclin to membranes of a neuronal somatic hybrid.
Royal Postgraduate Medical School
(-)-[3H] desmethoxyverapamil labels multiple calcium channel modulator receptors in brain and skeletal muscle membranes: differentiation by temperature and dihydropyridines.
Johns Hopkins University
Structural basis for engineering of retinoic acid receptor isotype-selective agonists and antagonists.
Institute of Genetics and Molecular and Cellular Biology (Igbmc)
A high-affinity subtype-selective agonist ligand for the thyroid hormone receptor.
University of California San Francisco
Structure-activity studies of rapamycin analogs: evidence that the C-7 methoxy group is part of the effector domain and positioned at the FKBP12-FRAP interface.
Smithkline Beecham Pharmaceuticals
Site-specific orthogonal labeling of the carboxy terminus of alpha-tubulin.
Binghamton University
Ultrasensitive in situ visualization of active glucocerebrosidase molecules.
Leiden University
Transition state analogs of 5'-methylthioadenosine nucleosidase disrupt quorum sensing.
Albert Einstein College of Medicine
Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer.
University of Texas Southwestern Medical Center
Anchored plasticity opens doors for selective inhibitor design in nitric oxide synthase.
The Scripps Research Institute
Correlating solution binding and ESI-MS stabilities by incorporating solvation effects in a confined cucurbit[8]uril system.
University of Cambridge
Complexation and chiral recognition thermodynamics of 6-amino-6-deoxy-beta-cyclodextrin with anionic, cationic, and neutral chiral guests: counterbalance between van der Waals and coulombic interactions.
Japan Science and Technology Agency
Thermodynamic and Nuclear Magnetic Resonance Study of the Interactions of alpha-and beta-Cyclodextrin with Model Substances: Phenethylamine, Ephedrines, and Related Substances
Nist
Discovery of a series of acrylic acids and their derivatives as chemical leads for selective EP3 receptor antagonists.
Ono Pharmaceutical
Antagonists of the human A(2A) receptor. Part 6: Further optimization of pyrimidine-4-carboxamides.
Vernalis (R&D)
Design, synthesis, and SAR of cis-1,2-diaminocyclohexane derivatives as potent factor Xa inhibitors. Part II: exploration of 6-6 fused rings as alternative S1 moieties.
Daiichi Sankyo
Glycogen phosphorylase inhibitory effects of 2-oxo-1,2-dihydropyridin-3-yl amide derivatives.
Griffith University
3,4-Dihydropyrimido(1,2-a)indol-10(2H)-ones as potent non-peptidic inhibitors of caspase-3.
Wyeth Research
Discovery of 3-(1H-indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrole-2,5-dione (AEB071), a potent and selective inhibitor of protein kinase C isotypes.
Novartis
Design, synthesis, and X-ray crystal structures of 2,4-diaminofuro[2,3-d]pyrimidines as multireceptor tyrosine kinase and dihydrofolate reductase inhibitors.
Duquesne University
Identification of PDE4B Over 4D subtype-selective inhibitors revealing an unprecedented binding mode.
Gsk
Enhanced pharmacokinetic properties of 1,4-benzodiazepine-2,5-dione antagonists of the HDM2-p53 protein-protein interaction through structure-based drug design.
Johnson & Johnson Pharmaceutical
Discovery and cocrystal structure of benzodiazepinedione HDM2 antagonists that activate p53 in cells.
Johnson & Johnson Pharmaceutical
Second generation of BACE-1 inhibitors part 3: Towards non hydroxyethylamine transition state mimetics.
Gsk
N-aryl-oxazolidin-2-imine muscle selective androgen receptor modulators enhance potency through pharmacophore reorientation.
Bristol-Myers Squibb
Carbonic anhydrase inhibitors. Cloning, characterization, and inhibition studies of a new beta-carbonic anhydrase from Mycobacterium tuberculosis.
Kochi Medical School
Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's disease.
Wyeth Research
Identification and structure-activity relationships of substituted pyridones as inhibitors of Pim-1 kinase.
Valeant Pharmaceuticals Research and Development
Selectivity determinants of inhibitor binding to human 20alpha-hydroxysteroid dehydrogenase: crystal structure of the enzyme in ternary complex with coenzyme and the potent inhibitor 3,5-dichlorosalicylic acid.
Monash University
Design and synthesis of 2-amino-pyrazolopyridines as Polo-like kinase 1 inhibitors.
Sunesis Pharmaceuticals
Inhibitors of the tyrosine kinase EphB4. Part 1: Structure-based design and optimization of a series of 2,4-bis-anilinopyrimidines.
Astrazeneca
NAD+-dependent DNA ligase (Rv3014c) from Mycobacterium tuberculosis: novel structure-function relationship and identification of a specific inhibitor.
India Central Drug Research Institute
Synthesis of Stable and Potent delta/mu Opioid Peptides: Analogues of H-Tyr-c[d-Cys-Gly-Phe-d-Cys]-OH by Ring-Closing Metathesis.
Universita Degli Studi
Synthesis and SAR of 2-Aryloxy-4-alkoxy-pyridines as Potent Orally Active Corticotropin-Releasing Factor 1 Receptor Antagonists.
Pfizer
Structural Modification of the P2' Position of 2,7-Dialkyl-Substituted 5(S)-Amino-4(S)-hydroxy-8-phenyl-octanecarboxamides: The Discovery of Aliskiren, a Potent Nonpeptide Human Renin Inhibitor Active after Once Daily Dosing in Marmosets.
Novartis Pharmaceuticals