138 articles for thisTarget
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Article Title
Organization
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
Bifunctional Peptide-Based Opioid Agonist-Nociceptin Antagonist Ligands for Dual Treatment of Acute and Neuropathic Pain.
Vrije Universiteit Brussel
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
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
Tactical Approaches to Interconverting GPCR Agonists and Antagonists.
University of Minnesota
Tritium-labelled isovaleryl-RYYRIK-NH2 as potential antagonist probe for ORL1 nociceptin receptor.
Kyushu 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
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
A selective small molecule NOP (ORL-1 receptor) partial agonist for the treatment of anxiety.
West Chester University
Pyrrolo- and pyridomorphinans: non-selective opioid antagonists and delta opioid agonists/mu opioid partial agonists.
University of Bath
Selectively promiscuous opioid ligands: discovery of high affinity/low efficacy opioid ligands with substantial nociceptin opioid peptide receptor affinity.
University of Bath
Designing bifunctional NOP receptor-mu opioid receptor ligands from NOP-receptor selective scaffolds. Part II.
Astraea Therapeutics
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
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.
Institute of Organic Synthesis
Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.
University of Siena
Designing bifunctional NOP receptor-mu opioid receptor ligands from NOP receptor-selective scaffolds. Part I.
Astraea Therapeutics
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
Synthesis and biological activity of nociceptin/orphanin FQ analogues substituted in position 7 or 11 with Calpha,alpha-dialkylated amino acids.
University of Ferrara
Synthesis and evaluation of radioligands for imaging brain nociceptin/orphanin FQ peptide (NOP) receptors with positron emission tomography.
National Institute of Mental Health
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
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
Spare interactions of highly potent [Arg(14),Lys(15)]nociceptin for cooperative induction of ORL1 receptor activation.
Kyushu University
Synthesis and pharmacological evaluation of 6-naltrexamine analogs for alcohol cessation.
Human Biomolecular Research Institute
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
Synergistic effect of basic residues at positions 14-15 of nociceptin on binding affinity and receptor activation.
TBA
High affinity conformationally constrained nociceptin/orphanin FQ(1-13) amide analogues.
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
Designed modification of partial agonist of ORL1 nociceptin receptor for conversion into highly potent antagonist.
Kyushu University
Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1.
Schering-Plough Research Institute
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
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
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
Probing opioid receptor interactions with azacycloalkane amino acids. Synthesis of a potent and selective ORL1 antagonist.
University of Montreal
Novel, potent ORL-1 receptor agonist peptides containing alpha-Helix-promoting conformational constraints.
Purdue Pharma
High-affinity, non-peptide agonists for the ORL1 (orphanin FQ/nociceptin) receptor.
F. Hoffmann-La Roche
Synthesis and delta-opioid receptor antagonist activity of a naltrindole analogue with a regioisomeric indole moiety.
University of Minnesota
The design and synthesis of a novel quinolizidine template for potent opioid and opioid receptor-like (ORL1, NOP) receptor ligands.
Sri International
Synthesis and structure-activity relationships of aminoalkylazetidines as ORL1 receptor ligands.
Schering-Plough Research Institute
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
Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine.
University of Bath
Synthesis and pharmacological evaluation of bivalent antagonists of the nociceptin opioid receptor.
Istituto Superiore Di Sanit£
Novel Helix-Constrained Nociceptin Derivatives Are Potent Agonists and Antagonists of ERK Phosphorylation and Thermal Analgesia in Mice
TBA
A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.
Università
Rapid access towards follow-up NOP receptor agonists using a knowledge based approach.
Schering-Plough Research Institute
Synthesis and biological evaluation of imidazole derivatives as novel NOP/ORL1 receptor antagonists: exploration and optimization of alternative pyrazole structure.
Banyu Tsukuba Research Institute
Discriminatory synergistic effect of Trp-substitutions in superagonist [(Arg/Lys)(14), (Arg/Lys)(15)]nociceptin on ORL1 receptor binding and activation.
Kyushu 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
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
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
Structure-activity relationships of 3-substituted N-benzhydryl-nortropane analogs as nociceptin receptor ligands for the treatment of cough.
Schering-Plough Research Institute
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
Novel ORL1-selective antagonists with oral bioavailability and brain penetrability.
Banyu Tsukuba Research Institute
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
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
Synthesis and evaluation of N-3 substituted phenoxypropyl piperidine benzimidazol-2-one analogues as NOP receptor agonists with analgesic and sedative properties.
Organon Laboratories
Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: increased receptor specificity and in vivo activity.
Jerini
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
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
An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression.
Predix Pharmaceuticals
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
Design, synthesis, and biological evaluation of indole derivatives as novel nociceptin/orphanin FQ (N/OFQ) receptor antagonists.
Banyu Tsukuba Research Institute
Identification of a novel spiropiperidine opioid receptor-like 1 antagonist class by a focused library approach featuring 3D-pharmacophore similarity.
Banyu Tsukuba Research Institute
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
Preparation of 3-spirocyclic indolin-2-ones as ligands for the ORL-1 receptor.
Johnson & Johnson Pharmaceutical Research and Development
Novel 2-N,N-dimethylaminomethyl-2,3,3a,12b-tetrahydrodibenzo[b,f]furo[2,3-d]oxepin derivatives displaying combined norepinephrine reuptake inhibition and 5-HT2A/2C receptor antagonism.
Janssen-Cilag
Synthesis and SAR studies of 3-phenoxypropyl piperidine analogues as ORL1 (NOP) receptor agonists.
Organon Laboratories
Design and synthesis of 4-phenyl piperidine compounds targeting the mu receptor.
Purdue Pharma
Synthesis and biological evaluation of the major metabolite of atomoxetine: elucidation of a partial kappa-opioid agonist effect.
Johnson and Johnson Pharmaceutical
A novel series of piperidin-4-yl-1,3-dihydroindol-2-ones as agonist and antagonist ligands at the nociceptin receptor.
Sri International
Structure-activity study of the ORL1 antagonist Ac-Arg-D-Cha-Qaa-D-Arg-D-p-ClPhe-NH2.
Vrije Universiteit Brussel
Design and parallel synthesis of piperidine libraries targeting the nociceptin (N/OFQ) receptor.
Purdue Pharma
Neuropeptide FF and Its Receptors: Therapeutic Applications and Ligand Development.
Research Triangle Institute
Biased Agonism at Nociceptin/Orphanin FQ Receptors: A Structure Activity Study on N/OFQ(1-13)-NH
University of Ferrara
Structure-activity studies on nociceptin analogues: ORL1 receptor binding and biological activity of cyclic disulfide-containing analogues of nociceptin peptides.
Tohoku Pharmaceutical University
4-Aminoquinolines: novel nociceptin antagonists with analgesic activity.
Central Pharmaceutical Research Institute
Treatment of Pain with Spirocylic Cyclohexane Derivatives Having Dual Specificity for ORL-1 and μ-Opioid Receptors.
Dart Neuroscience
Nociceptin Opioid Receptor (NOP) as a Therapeutic Target: Progress in Translation from Preclinical Research to Clinical Utility.
Astraea Therapeutics
The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series.
University of Silesia In Katowice
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
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.
Shanghaitech University
Discovery and Structure-Activity Relationships of Nociceptin Receptor Partial Agonists That Afford Symptom Ablation in Parkinson's Disease Models.
Astraea Therapeutics
Synthesis and changes in affinity for NOP and opioid receptors of novel hexapeptides containing β(2)-tryptophan analogues.
Bulgarian Academy of Sciences
Structure-activity relationships and CoMFA of N-3 substituted phenoxypropyl piperidine benzimidazol-2-one analogues as NOP receptor agonists with analgesic properties.
Organon Laboratories
Synthesis and biological activity of nociceptin/orphanin FQ(1-13)NH2 analogues modified in 9 and/or 13 position.
University of Chemical Technology and Metallurgy
N- and C-terminal modifications of nociceptin/orphanin FQ generate highly potent NOP receptor ligands.
University of Ferrara
Novel hexahydrospiro[piperidine-4,1'-pyrrolo[3,4-c]pyrroles]: highly selective small-molecule nociceptin/orphanin FQ receptor agonists.
F. Hoffmann-La Roche
Structure-activity studies of the Phe(4) residue of nociceptin(1-13)-NH(2): identification of highly potent agonists of the nociceptin/orphanin FQ receptor.
University of Ferrara
Further studies on nociceptin-related peptides: discovery of a new chemical template with antagonist activity on the nociceptin receptor.
University of Ferrara
Identification and biological evaluation of thiazole-based inverse agonists of RORγt.
Phenex Pharmaceuticals
Hydrophilic, Potent, and Selective 7-Substituted 2-Aminoquinolines as Improved Human Neuronal Nitric Oxide Synthase Inhibitors.
Northwestern University
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
Aza-oxo-indoles for the treatment and prophylaxis of respiratory syncytial virus infection
Hoffmann-La Roche
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
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
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
Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer.
University of Texas Southwestern Medical Center
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