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98 articles for thisTarget

The following articles (labelled with PubMed ID or TBD) are for your review

Article Title
Tactical Approaches to Interconverting GPCR Agonists and Antagonists.EBI
University of Minnesota
N-benzoyl-1,5-benzothiazepine and its S-oxide as vasopressin receptor ligands: insight into the active stereochemistry around the seven-membered ring.EBI
Teikyo University
Discovery of highly selective brain-penetrant vasopressin 1a antagonists for the potential treatment of autism via a chemogenomic and scaffold hopping approach.EBI
F. Hoffmann-La Roche
Selective nonpeptidic fluorescent ligands for oxytocin receptor: design, synthesis, and application to time-resolved FRET binding assay.EBI
University of Strasburg
New, potent, and selective peptidic oxytocin receptor agonists.EBI
Ferring Research Institute
2,5-diketopiperazines as potent, selective, and orally bioavailable oxytocin antagonists. 2. Synthesis, chirality, and pharmacokinetics.EBI
A comparative protease stability study of synthetic macrocyclic peptides that mimic two endocrine hormones.EBI
The College of New Jersey
Colloidal aggregation causes inhibition of G protein-coupled receptors.EBI
University of North Carolina At Chapel Hill
Optimisation of pharmacokinetic properties to afford an orally bioavailable and selective V1A receptor antagonist.EBI
Pyrrolo[1,2-a]pyrazine and pyrazolo[1,5-a]pyrazine: novel, potent, and selective series of Vasopressin 1b receptor antagonists.EBI
Discovery and optimisation of a potent and selective tertiary sulfonamide oxytocin antagonist.EBI
Selective fluorescent nonpeptidic antagonists for vasopressin V2 GPCR: application to ligand screening and oligomerization assays.EBI
University of Strasburg
Pyridyl-2,5-diketopiperazines as potent, selective, and orally bioavailable oxytocin antagonists: synthesis, pharmacokinetics, and in vivo potency.EBI
Synthesis and evaluation of C-11, F-18 and I-125 small molecule radioligands for detecting oxytocin receptors.EBI
Emory University
Subtlety of the structure-affinity and structure-efficacy relationships around a nonpeptide oxytocin receptor agonist.EBI
University of Strasburg
Tetrahydroquinoline sulfonamides as vasopressin 1b receptor antagonists.EBI
Schering-Plough Research Institute
Discovery and optimization of highly ligand-efficient oxytocin receptor antagonists using structure-based drug design.EBI
The discovery of GSK221149A: a potent and selective oxytocin antagonist.EBI
Toward efficient drug screening by homogeneous assays based on the development of new fluorescent vasopressin and oxytocin receptor ligands.EBI
Institute Genomics Functional (Igf)
Pyridobenzodiazepines: a novel class of orally active, vasopressin V2 receptor selective agonists.EBI
Wyeth Research
Discovery and development of a new class of potent, selective, orally active oxytocin receptor antagonists.EBI
Serono Pharmaceutical Research Institute
New analgesic drugs derived from phencyclidine.EBI
Design of potent and selective agonists for the human vasopressin V1b receptor based on modifications of [deamino-cys1]arginine vasopressin at position 4.EBI
Medical College of Ohio
Synthesis and characterization of fluorescent antagonists and agonists for human oxytocin and vasopressin V(1)(a) receptors.EBI
University of Montpellier
Synthesis and evaluation of nonpeptide substituted spirobenzazepines as potent vasopressin antagonists.EBI
Johnson and Johnson Pharmaceutical Research and Development
Potent nonpeptide vasopressin receptor antagonists based on oxazino- and thiazinobenzodiazepine templates.EBI
Johnson & Johnson Pharmaceutical Research & Development
Synthesis and evaluation of potent and selective human V1a receptor antagonists as potential ligands for PET or SPECT imaging.EBI
Lehigh University
Discovery of PF-184563, a potent and selective V1a antagonist for the treatment of dysmenorrhoea. The influence of compound flexibility on microsomal stability.EBI
New, potent, selective, and short-acting peptidic V1a receptor agonists.EBI
Ferring Research Institute
Potent and selective oxindole-based vasopressin 1b receptor antagonists with improved pharmacokinetic properties.EBI
Abbott Laboratories
Identification and optimisation of novel sulfonamide, selective vasopressin V1B receptor antagonists.EBI
Design, synthesis, and pharmacological characterization of fluorescent peptides for imaging human V1b vasopressin or oxytocin receptors.EBI
University of Montpellier
Synthesis and SAR studies of novel 2-(4-oxo-2-aryl-quinazolin-3(4H)-yl)acetamide vasopressin V1b receptor antagonists.EBI
Oral oxytocin antagonists.EBI
Spiroindolones, a potent compound class for the treatment of malaria.EBI
Swiss Tropical and Public Health Institute
Identification and optimization of novel 2-(4-oxo-2-aryl-quinazolin-3(4H)-yl)acetamide vasopressin V3 (V1b) receptor antagonists.EBI
Ligand Pharmaceuticals
Synthesis and evaluation of azabicyclo[3.2.1]octane derivatives as potent mixed vasopressin antagonists.EBI
Identification of amide bioisosteres of triazole oxytocin antagonists.EBI
Triazole oxytocin antagonists: Identification of an aryloxyazetidine replacement for a biaryl substituent.EBI
Aryloxypyrazines as highly selective antagonists of Oxytocin.EBI
New benzylureas as a novel series of potent, nonpeptidic vasopressin V2 receptor agonists.EBI
Triazole oxytocin antagonists: identification of aryl ether replacements for a biaryl substituent.EBI
Design and optimization of potent, selective antagonists of Oxytocin.EBI
Next-generation spirobenzazepines: identification of RWJ-676070 as a balanced vasopressin V1a/V2 receptor antagonist for human clinical studies.EBI
Johnson & Johnson Pharmaceutical Research & Development
Identification and synthesis of major metabolites of Vasopressin V2-receptor agonist WAY-151932, and antagonist, Lixivaptan.EBI
Wyeth Research
Long Residence Time at the Vasopressin VEBI
Xuzhou Medical University
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.EBI
Columbia University College of Physicians and Surgeons
Benzodiazepine Derivatives as Potent Vasopressin VEBI
Xuzhou Medical University
(4-Substituted-phenyl)-(5H-10,11-dihydro-pyrrolo [2,1-c][1,4] benzodiazepin-10-yl)-methanone derivatives as vasopressin receptor modulators.EBI
Wyeth Research
Synthesis and Characterization of New VEBI
Gedeon Richter
Non-peptide oxytocin agonists.EBI
Ferring Research
Synthesis and evaluation of spirobenzazepines as potent vasopressin receptor antagonists.EBI
Johnson and Johnson Pharmaceutical Research and Development
Synthesis and structure-activity relationships of 5,6,7,8-tetrahydro-4H-thieno[3,2-b]azepine derivatives: novel arginine vasopressin antagonists.EBI
Central Pharmaceutical Research Institute
2,5-disubstituted 3,4-dihydro-2H-benzo[b][1,4]thiazepines as potent and selective V2 arginine vasopressin receptor antagonists.EBI
Johnson & Johnson Pharmaceutical Research & Development
Synthesis and biological evaluation of novel indoloazepine derivatives as non-peptide vasopressin V2 receptor antagonists.EBI
Johnson & Johnson Pharmaceutical Research & Development
Yohimbine as a Starting Point to Access Diverse Natural Product-Like Agents with Re-programmed Activities against Cancer-Relevant GPCR Targets.EBI
University of Florida
Bridged bicyclic vasopressin receptor antagonists with V(2)-selective or dual V(1a)/V(2) activity.EBI
Johnson and Johnson Pharmaceutical Research and Development
Characterization of orally active nonpeptide vasopressin V(2) receptor agonist. Synthesis and biological evaluation of both the (5R)- and (5S)-enantioisomers of 2-[1-(2-Chloro-4-pyrrolidin-1-yl-benzoyl)-2,3,4,5-tetrahydro-1H-1-benzazepin- 5-yl]-N-isopropylacetamide.EBI
Otsuka Pharmaceutical
Synthesis and pharmacological evaluation of 5-(4-biphenyl)-3-methyl-4-phenyl-1,2,4-triazole derivatives as a novel class of selective antagonists for the human vasopressin V(1A) receptor.EBI
Yamanouchi Pharmaceutical
New V1a receptor antagonist. Part 2. Identification and optimization of triazolobenzazepines.EBI
Gedeon Richter
Novel design of nonpeptide AVP V(2) receptor agonists: structural requirements for an agonist having 1-(4-aminobenzoyl)-2,3,4, 5-tetrahydro-1H-1-benzazepine as a template.EBI
Otsuka Pharmaceutical
The design, synthesis and physical chemical properties of novel human vasopressin V2-receptor antagonists optimized for parenteral delivery.EBI
Wyeth-Ayerst Research
The synthesis and vasopressin (AVP) antagonist activity of a novel series of N-aroyl-2,4,5,6-tetrahydropyrazolo[3,4-d]thieno[3,2-b]azepines.EBI
Wyeth-Ayerst Research
Discovery of Potent, Selective, and Short-Acting Peptidic VEBI
Ferring Research Institute
4,10-dihydro-5H-thieno[3,2-c][1]benzazepine derivatives and 9,10-dihydro-4H-thieno[2,3-c][1]benzazepine derivatives as orally active arginine vasopressin receptor antagonists.EBI
Wyeth-Ayerst Research
Nonpeptide oxytocin antagonists: analogs of L-371,257 with improved potency.EBI
Merck Research Laboratories
Fluorescent pseudo-peptide linear vasopressin antagonists: design, synthesis, and applications.EBI
University of Montpellier
Discovery of SHR1653, a Highly Potent and Selective OTR Antagonist with Improved Blood-Brain Barrier Penetration.EBI
Shanghai Hengrui Pharmaceutical
5-Fluoro-2-methyl-N-[4-(5H-pyrrolo[2,1-c]-[1, 4]benzodiazepin-10(11H)-ylcarbonyl)-3-chlorophenyl]benzamide (VPA-985): an orally active arginine vasopressin antagonist with selectivity for V2 receptors.EBI
Wyeth-Ayerst Research
Engineering a Potent, Long-Acting, and Periphery-Restricted Oxytocin Receptor Agonist with Anorexigenic and Body Weight Reducing Effects.EBI
Calibr At The Scripps Research Institute
1-(1-[4-[(N-acetyl-4-piperidinyl)oxy]-2-methoxybenzoyl]piperidin-4- yl)-4H-3,1-benzoxazin-2(1H)-one (L-371,257): a new, orally bioavailable, non-peptide oxytocin antagonist.EBI
Merck Research Laboratories
Dicarbavasopressin antagonist analogues exhibit reduced in vivo agonist activity.EBI
Smith Kline & French Laboratories
LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism.EBI
Umr7200 Cnrs/Universit£
A minor modification of residue 1 in potent vasopressin antagonists dramatically reduces agonist activity.EBI
Smith Kline & French Laboratories
Structure-activity relationships of novel vasopressin antagonists containing C-terminal diaminoalkanes and (aminoalkyl)guanidines.EBI
Smith Kline & French Laboratories
Building bridges for highly selective, potent and stable oxytocin and vasopressin analogs.EBI
Imperial College
Tolvaptan-Type Vasopressin Receptor Ligands: Important Role of Axial Chirality in the Active Form.EBI
Teikyo University
Synthesis, Biological Evaluation, and Molecular Docking of 8-imino-2-oxo-2H,8H-pyrano[2,3-f]chromene Analogs: New Dual AChE Inhibitors as Potential Drugs for the Treatment of Alzheimer's Disease.BDB
Yogi Vemana University
Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b.BDB
University of Leipzig
New natural cholinesterase inhibiting and calcium channel blocking quinoline alkaloids.BDB
University of Karachi
Benzofuran- and furan-2-yl-(phenyl)-3-pyridylmethanols: synthesis and inhibition of P450 aromatase.BDB
Cardiff University
The motilin pharmacophore in CHO cells expressing the human motilin receptor.BDB
Katholieke Universiteit Leuven
Functional selectivity of dopamine receptor agonists. II. Actions of dihydrexidine in D2L receptor-transfected MN9D cells and pituitary lactotrophs.BDB
University of North Carolina At Chapel Hill
Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity.BDB
Merck Frosst Centre For Therapeutic Research
Synthesis of novel, potent, diol-based HIV-1 protease inhibitors via intermolecular pinacol homocoupling of (2S)-2-benzyloxymethyl-4-phenylbutanal.BDB
Stockholm University