148 articles for thisTarget
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Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.
University of Kansas
N-Arylsulfonyl-a-amino carboxamides are potent and selective inhibitors of the chemokine receptor CCR10 that show efficacy in the murine DNFB model of contact hypersensitivity.
Boehringer Ingelheim Pharmaceuticals
Synthesis and evaluation of a 2-benzothiazolylphenylmethyl ether class of histamine H4 receptor antagonists.
Bioprojet-Biotech
Conformational Restriction and Enantioseparation Increase Potency and Selectivity of Cyanoguanidine-Type Histamine H4 Receptor Agonists.
University of Regensburg
2,4-Diaminopyrimidines as dual ligands at the histamine H1 and H4 receptor-H1/H4-receptor selectivity.
Friedrich-Alexander-Universit£T Erlangen-N£Rnberg
(2-Arylethenyl)-1,3,5-triazin-2-amines as a novel histamine H4 receptor ligands.
Jagiellonian University Medical College
Functional Profiling of 2-Aminopyrimidine Histamine H4 Receptor Modulators.
Janssen Research and Development
3,4-Diaza-bicyclo[4.1.0]hept-4-en-2-one phenoxypropylamine analogs of irdabisant (CEP-26401) as potent histamine-3 receptor inverse agonists with robust wake-promoting activity.
Teva Global R & D.
Diaminopyrimidines, diaminopyridines and diaminopyridazines as histamine H4 receptor modulators.
Janssen Research and Development
Biased ligand modulation of seven transmembrane receptors (7TMRs): functional implications for drug discovery.
Merck Research Laboratories
The effect of pK(a) on pyrimidine/pyridine-derived histamine H4 ligands.
Janssen Research and Development
Aryl-1,3,5-triazine derivatives as histamine H4 receptor ligands.
Jagiellonian University Medical College
Design and synthesis of systemically active metabotropic glutamate subtype-2 and -3 (mGlu2/3) receptor positive allosteric modulators (PAMs): pharmacological characterization and assessment in a rat model of cocaine dependence.
Sanford-Burnham Medical Research Institute
Discovery and SAR of 6-alkyl-2,4-diaminopyrimidines as histamine H4 receptor antagonists.
Janssen Research and Development
Non-imidazole histamine H3 receptor ligands incorporating antiepileptic moieties.
United Arab Emirates University
A novel series of histamine H4 receptor antagonists based on the pyrido[3,2-d]pyrimidine scaffold: comparison of hERG binding and target residence time with PF-3893787.
Griffin Discoveries
Bodilisant-a novel fluorescent, highly affine histamine h3 receptor ligand.
Goethe University
Synthesis and evaluation of novel ligands for the histamine H4 receptor based on a pyrrolo[2,3-d]pyrimidine scaffold.
Ku Leuven
Molecular determinants of ligand binding modes in the histamine H(4) receptor: linking ligand-based three-dimensional quantitative structure-activity relationship (3D-QSAR) models to in silico guided receptor mutagenesis studies.
Vu University Amsterdam
Mepyramine-JNJ7777120-hybrid compounds show high affinity to hH(1)R, but low affinity to hH(4)R.
University of Regensburg
Fragment library screening reveals remarkable similarities between the G protein-coupled receptor histamine H4 and the ion channel serotonin 5-HT3A.
Vu University Amsterdam
Triazole ligands reveal distinct molecular features that induce histamine H4 receptor affinity and subtly govern H4/H3 subtype selectivity.
Vu University Amsterdam
Chiral NG-acylated hetarylpropylguanidine-type histamine H2 receptor agonists do not show significant stereoselectivity.
University of Regensburg
Rigidified 2-aminopyrimidines as histamine H4 receptor antagonists: effects of substitution about the rigidifying ring.
Abbott Laboratories
Synthesis and structure-activity relationships of cyanoguanidine-type and structurally related histamine H4 receptor agonists.
University of Regensburg
Synthesis and QSAR of quinazoline sulfonamides as highly potent human histamine H4 receptor inverse agonists.
Griffin Discoveries
Diamine-based human histamine H3 receptor antagonists: (4-aminobutyn-1-yl)benzylamines.
Johnson & Johnson Pharmaceutical Research & Development
Clobenpropit analogs as dual activity ligands for the histamine H3 and H4 receptors: synthesis, pharmacological evaluation, and cross-target QSAR studies.
Vu University Amsterdam
N(G)-acylated imidazolylpropylguanidines as potent histamine H4 receptor agonists: selectivity by variation of the N(G)-substituent.
University of Regensburg
Discovery of quinazolines as histamine H4 receptor inverse agonists using a scaffold hopping approach.
Vrije Universiteit Amsterdam
Synthesis and structure-activity relationships for biphenyl H3 receptor antagonists with moderate anti-cholinesterase activity.
University of Parma
Synthesis and SAR of aminoalkoxy-biaryl-4-carboxamides: novel and selective histamine H3 receptor antagonists.
Abbott Laboratories
Novel azulene derivatives for the treatment of erectile dysfunction.
Friedrich-Alexander University
The bivalent ligand approach leads to highly potent and selective acylguanidine-type histamine H2 receptor agonists.
University of Regensburg
Detailed structure-activity relationship of indolecarboxamides as H4 receptor ligands.
Boehringer Ingelheim Rcv
Synthesis and evaluation of 4- and 5-pyridazin-3-one phenoxypropylamine analogues as histamine-3 receptor antagonists.
Cephalon
Radiosynthesis and evaluation of an (18)F-labeled positron emission tomography (PET) radioligand for brain histamine subtype-3 receptors based on a nonimidazole 2-aminoethylbenzofuran chemotype.
National Institute of Mental Health
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
Synthesis and structure-activity relationships of N-aryl-piperidine derivatives as potent (partial) agonists for human histamine H3 receptor.
Meiji Seika Kaisha
Identification and hit-to-lead exploration of a novel series of histamine H4 receptor inverse agonists.
Argenta Discovery
Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine.
Hunter College and The Graduate Center of The City University of New York
Acylguanidines as bioisosteres of guanidines: NG-acylated imidazolylpropylguanidines, a new class of histamine H2 receptor agonists.
University of Regensburg
Discovery of novel human histamine H4 receptor ligands by large-scale structure-based virtual screening.
Gedeon Richter
In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.
Abbott Laboratories
The first potent and selective non-imidazole human histamine H4 receptor antagonists.
Johnson & Johnson Pharmaceutical Research and Development
Ligand based design of novel histamine H4 receptor antagonists; fragment optimization and analysis of binding kinetics.
Griffin Discoveries
Synthesis and evaluation of 4-alkoxy-[1'-cyclobutyl-spiro(3,4-dihydrobenzopyran-2,4'-piperidine)] analogues as histamine-3 receptor antagonists.
Cephalon
Searching for the Multi-Target-Directed Ligands against Alzheimer's disease: discovery of quinoxaline-based hybrid compounds with AChE, H3R and BACE 1 inhibitory activities.
Zhejiang University
Synthesis and evaluation of pyridone-phenoxypropyl-R-2-methylpyrrolidine analogues as histamine H3 receptor antagonists.
Cephalon
Crystal structure-based virtual screening for fragment-like ligands of the human histamine H(1) receptor.
Vu University Amsterdam
Discovery of a series of potent and selective human H4 antagonists using ligand efficiency and libraries to explore structure-activity relationship (SAR).
Pfizer
Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.
Pfizer
Tricyclic aminopyrimidine histamine H4 receptor antagonists.
Johnson & Johnson Pharmaceutical Research & Development
N-Alkenyl and cycloalkyl carbamates as dual acting histamine H3 and H4 receptor ligands.
Jagiellonian University Medical College
Triamino pyrimidines and pyridines as histamine H(4) receptor modulators.
Johnson & Johnson Pharmaceutical Research & Development
Investigation of the histamine H3 receptor binding site. Design and synthesis of hybrid agonists with a lipophilic side chain.
Meiji Seika Kaisha
Discovery of substituted benzyl tetrazoles as histamine H3 receptor antagonists.
Evotec (Uk)
Agonist/antagonist modulation in a series of 2-aryl benzimidazole H4 receptor ligands.
Johnson & Johnson Pharmaceutical Research & Development
Role of hydrophobic substituents on the terminal nitrogen of histamine in receptor binding and agonist activity: development of an orally active histamine type 3 receptor agonist and evaluation of its antistress activity in mice.
Meiji Seika Kaisha
Histamine H3 and H4 receptor affinity of branched 3-(1H-imidazol-4-yl)propyl N-alkylcarbamates.
Jagiellonian University Medical College
Synthesis and structural and pharmacological properties of cyclopropane-based conformationally restricted analogs of 4-methylhistamine as histamine H3/H4 receptor ligands.
Hokkaido University
2,4-Diaminopyrimidines as histamine H4 receptor ligands--Scaffold optimization and pharmacological characterization.
Johann Wolfgang Goethe University
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
Discovery of novel phenethylpyridone derivatives as potent melanin-concentrating hormone 1 receptor antagonists.
Tsukuba Research Institute
Synthesis, structure-activity relationships, and biological profiles of a dihydrobenzoxathiin class of histamine H(3) receptor inverse agonists.
Tsukuba Research Institute
Development of a selective and potent radioactive ligand for histamine H(3) receptors: A compound potentially useful for receptor occupancy studies.
Tsukuba Research Institute
Development of novel 2-[4-(aminoalkoxy)phenyl]-4(3H)-quinazolinone derivatives as potent and selective histamine H3 receptor inverse agonists.
Tsukuba Research Institute
Synthesis and evaluation of structurally constrained quinazolinone derivatives as potent and selective histamine H3 receptor inverse agonists.
Tsukuba Research Institute
Synthesis and evaluation of a spiro-isobenzofuranone class of histamine H3 receptor inverse agonists.
Tsukuba Research Institute
Synthesis, structure-activity relationships, and biological profiles of a quinazolinone class of histamine H3 receptor inverse agonists.
Tsukuba Research Institute
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
Treatment of allergy: Overview of synthetic anti-allergy small molecules in medicinal chemistry.
Zhejiang Sci-Tech University
Stereochemical diversity-oriented conformational restriction strategy. Development of potent histamine H3 and/or H4 receptor antagonists with an imidazolylcyclopropane structure.
Hokkaido University
Characterization of the histamine H4 receptor binding site. Part 1. Synthesis and pharmacological evaluation of dibenzodiazepine derivatives.
Vrije Universiteit Amsterdam
Optimization of Peptide Linker-Based Fluorescent Ligands for the Histamine H
University of Nottingham Biodiscovery Institute
Synthesis, in vitro and in vivo evaluation of [O-methyl-11C] 2-{4-[4-(3-methoxyphenyl)piperazin-1-yl]-butyl}-4-methyl-2H-[1,2,4]-triazine-3,5-dione: a novel agonist 5-HT1A receptor PET ligand.
Columbia University College of Physicians and Surgeons
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
Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine h(4) antagonists.
Johnson & Johnson Pharmaceutical Research and Development
2-(4-alkylpiperazin-1-yl)quinolines as a new class of imidazole-free histamine H3 receptor antagonists.
Novo Nordisk
A Versatile Sub-Nanomolar Fluorescent Ligand Enables NanoBRET Binding Studies and Single-Molecule Microscopy at the Histamine H
University of Regensburg
Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 3: 5-Substituted 3-phenyl-1,2,4-oxadiazoles as potent antagonists.
Abbott Laboratories
Pharmacological characterization of a new series of carbamoylguanidines reveals potent agonism at the H
University of Regensburg
Structure-Activity Relationship of Heterocyclic P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Discovery of a Novel Highly Selective Histamine H4 Receptor Antagonist for the Treatment of Atopic Dermatitis.
Sungkyunkwan University
Cyclopropane-based conformational restriction of histamine. (1S,2S)-2-(2-aminoethyl)-1-(1H-imidazol-4-yl)cyclopropane, a highly selective agonist for the histamine H3 receptor, having a cis-cyclopropane structure.
Hokkaido University
Identification of N-phenyl-3-methoxy-4-pyridinones as orally bioavailable H
Zhejiang University
Structural modifications in the distal, regulatory region of histamine H
Jagiellonian University Medical College
Novel potent (dihydro)benzofuranyl piperazines as human histamine receptor ligands - Functional characterization and modeling studies on H
Universidade Federal De S£O Paulo
Isolation and Synthesis of Veranamine, an Antidepressant Lead from the Marine Sponge
University of Mississippi
UR-DEBa242: A Py-5-Labeled Fluorescent Multipurpose Probe for Investigations on the Histamine H
University of Regensburg
Alkyl derivatives of 1,3,5-triazine as histamine H
Jagiellonian University Medical College
Biphenyloxy-alkyl-piperidine and azepane derivatives as histamine H
Jagiellonian University Medical College
Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective D
National Institute of Neurological Disorders and Stroke
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.
Shanghaitech University
4-(3-Aminoazetidin-1-yl)pyrimidin-2-amines as High-Affinity Non-imidazole Histamine H
Vrije Universiteit Amsterdam
Nature-inspired pyrrolo[2,3-d]pyrimidines targeting the histamine H
Heinrich Heine University D£Sseldorf
3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HT
University of Minnesota Twin Cities
Anticonvulsant properties of histamine H3 receptor ligands belonging to N-substituted carbamates of imidazopropanol.
United Arab Emirates University
Bispyrimidines as potent histamine H(4) receptor ligands: delineation of structure-activity relationships and detailed H(4) receptor binding mode.
Boehringer Ingelheim Rcv
Synthesis and pharmacological properties of novel hydrophilic 5-HT4 receptor antagonists.
Drug Discovery Laboratory
Fragment based design of new H4 receptor-ligands with anti-inflammatory properties in vivo.
Vrije Universiteit Amsterdam
Discovery of S-(2-guanidylethyl)-isothiourea (VUF 8430) as a potent nonimidazole histamine H4 receptor agonist.
Vrije Universiteit Amsterdam
N-substituted piperidinyl alkyl imidazoles: discovery of methimepip as a potent and selective histamine H3 receptor agonist.
Vrije Universiteit Amsterdam
Synthesis and structure-activity relationships of conformationally constrained histamine H(3) receptor agonists.
Vrije Universiteit
A selective human H(4)-receptor agonist: (-)-2-cyano-1-methyl-3-[(2R,5R)-5- [1H-imidazol-4(5)-yl]tetrahydrofuran-2-y] methylguanidine.
Osaka University
1,3,5-Triazines: A promising scaffold for anticancer drugs development.
University of Palermo
Synthesis and biological activity of novel tert-butyl and tert-pentylphenoxyalkyl piperazine derivatives as histamine H
Jagiellonian University Medical College
Discovery of nanomolar ligands with novel scaffolds for the histamine H4 receptor by virtual screening.
Bioprojet-Biotech
Hydrophilic, Potent, and Selective 7-Substituted 2-Aminoquinolines as Improved Human Neuronal Nitric Oxide Synthase Inhibitors.
Northwestern University
SPIROCYCLIC MODULATORS OF CHOLESTEROL BIOSYNTHESIS AND THEIR USE FOR PROMOTING REMYELINATION
Genentech
Combination Alzheimer therapy using anti-N3pGlu Abeta antibodies + a BACE inhibitor
Eli Lilly
Crystal structure of 3-hydroxybenzoate 6-hydroxylase uncovers lipid-assisted flavoprotein strategy for regioselective aromatic hydroxylation.
Wageningen University
Synthetic compounds and derivatives as modulators of smoking or nicotine ingestion and lung cancer
Human Biomolecular Research Institute
Pharmacological characterization of AC-90179 [2-(4-methoxyphenyl)-N-(4-methyl-benzyl)-N-(1-methyl-piperidin-4-yl)-acetamide hydrochloride]: a selective serotonin 2A receptor inverse agonist.
Acadia Pharmaceuticals
Inhibitory effect on soybean lipoxygenase and docking studies of some secondary metabolites, isolated from Origanum vulgare L. ssp. hirtum.
University of Athens
Selective targeting of lysosomal cysteine proteases with radiolabeled electrophilic substrate analogs.
University of California San Francisco
Antibiotic sensitization using biphenyl tetrazoles as potent inhibitors of Bacteroides fragilis metallo-beta-lactamase.
Merck Research Laboratories
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
Thermodynamics of molecular recognition by cyclodextrins. 1. Calorimetric titration of inclusion complexation of naphthalenesulfonates with .alpha.-, .beta.-, and .gamma.-cyclodextrins: enthalpy-entropy compensation
Himeji Institute of Technology
Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase.
Shanghai Institutes For Biological Sciences
Identification of a Bis-guanylhydrazone [4,4'-Diacetyldiphenylurea-bis(guanylhydrazone); NSC 109555] as a novel chemotype for inhibition of Chk2 kinase.
Nih
Syntheses and anticholinesterase activities of (3aS)-N1, N8-bisnorphenserine, (3aS)-N1,N8-bisnorphysostigmine, their antipodal isomers, and other potential metabolites of phenserine.
University of North Carolina at Chapel Hill