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103 articles for thisTarget

The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
26390077 42 Tactical Approaches to Interconverting GPCR Agonists and Antagonists.EBI University of Minnesota
25774991 23 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
25654260 49 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 Ltd.
25642985 45 Selective nonpeptidic fluorescent ligands for oxytocin receptor: design, synthesis, and application to time-resolved FRET binding assay.EBI UMR7200 CNRS/Universit£ de Strasbourg
24874785 333 New, potent, and selective peptidic oxytocin receptor agonists.EBI Ferring Research Institute Inc.
16250654 41 2,5-diketopiperazines as potent, selective, and orally bioavailable oxytocin antagonists. 2. Synthesis, chirality, and pharmacokinetics.EBI GlaxoSmithKline Research and Development
23312470 3 A comparative protease stability study of synthetic macrocyclic peptides that mimic two endocrine hormones.EBI The College of New Jersey
23437772 35 Colloidal aggregation causes inhibition of G protein-coupled receptors.EBI University of North Carolina Chapel Hill School of Medicine
21700453 56 Optimisation of pharmacokinetic properties to afford an orally bioavailable and selective V1A receptor antagonist.EBI MSD
20674355 58 Pyrrolo[1,2-a]pyrazine and pyrazolo[1,5-a]pyrazine: novel, potent, and selective series of Vasopressin 1b receptor antagonists.EBI GlaxoSmithKline
19081251 38 Discovery and optimisation of a potent and selective tertiary sulfonamide oxytocin antagonist.EBI GlaxoSmithKline Pharmaceuticals
7752199 71 Effects of a D-Cys6/L-Cys6 interchange in nonselective and selective vasopressin and oxytocin antagonists.EBI Medical College of Ohio
2231609 13 Design of potent and selective linear antagonists of vasopressor (V1-receptor) responses to vasopressin.EBI Medical College of Ohio
22984902 59 Selective fluorescent nonpeptidic antagonists for vasopressin V2 GPCR: application to ligand screening and oligomerization assays.EBI UMR7200 CNRS/Universit£ de Strasbourg
22239250 59 Pyridyl-2,5-diketopiperazines as potent, selective, and orally bioavailable oxytocin antagonists: synthesis, pharmacokinetics, and in vivo potency.EBI GlaxoSmithKline Research and Development
22425346 28 Synthesis and evaluation of C-11, F-18 and I-125 small molecule radioligands for detecting oxytocin receptors.EBI Emory University
20104850 48 Subtlety of the structure-affinity and structure-efficacy relationships around a nonpeptide oxytocin receptor agonist.EBI UMR 7200 CNRS/Universit£ de Strasbourg
19800231 92 Tetrahydroquinoline sulfonamides as vasopressin 1b receptor antagonists.EBI Schering-Plough Research Institute
19095447 28 Discovery and optimization of highly ligand-efficient oxytocin receptor antagonists using structure-based drug design.EBI GlaxoSmithKline Pharmaceuticals
18032036 17 The discovery of GSK221149A: a potent and selective oxytocin antagonist.EBI GlaxoSmithKline Research and Development
17850055 18 Toward efficient drug screening by homogeneous assays based on the development of new fluorescent vasopressin and oxytocin receptor ligands.EBI INSERM
17300166 88 Design and synthesis of the first selective agonists for the rat vasopressin V(1b) receptor: based on modifications of deamino-[Cys1]arginine vasopressin at positions 4 and 8.EBI INSERM
16297621 17 Pyridobenzodiazepines: a novel class of orally active, vasopressin V2 receptor selective agonists.EBI Wyeth Research
16302826 129 Discovery and development of a new class of potent, selective, orally active oxytocin receptor antagonists.EBI Serono Pharmaceutical Research Institute
7241506 40 New analgesic drugs derived from phencyclidine.EBI TBA
15084136 96 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
12036367 46 Synthesis and characterization of fluorescent antagonists and agonists for human oxytocin and vasopressin V(1)(a) receptors.EBI INSERM
1331448 101 Development of a novel class of cyclic hexapeptide oxytocin antagonists based on a natural product.EBI Merck Research Laboratories
2167976 33 Receptor ligands which bind the oxytocin receptor with selectivity and high affinity. Chemical modification of a Streptomyces silvensis derived cyclic hexapeptide.EBI Merck
15149662 71 Synthesis and evaluation of nonpeptide substituted spirobenzazepines as potent vasopressin antagonists.EBI Johnson and Johnson Pharmaceutical Research and Development
15125926 88 Potent nonpeptide vasopressin receptor antagonists based on oxazino- and thiazinobenzodiazepine templates.EBI Johnson& Johnson Pharmaceutical Research& Development
11755361 24 N-Methylbenzanilide derivatives as a novel class of selective V(1A) receptor antagonists.EBI Yamanouchi Pharmaceutical Co. Ltd.
10201826 16 Synthesis of oxytocin antagonists containing conformationally constrained amino acids in position 2.EBI Albert Szent-Gy£rgyi Medical University
22249122 9 Synthesis and evaluation of potent and selective human V1a receptor antagonists as potential ligands for PET or SPECT imaging.EBI Lehigh University
21885275 65 Discovery of PF-184563, a potent and selective V1a antagonist for the treatment of dysmenorrhoea. The influence of compound flexibility on microsomal stability.EBI Pfizer Inc.
21688787 295 New, potent, selective, and short-acting peptidic V1a receptor agonists.EBI Ferring Research Institute Inc.
21605973 69 Potent and selective oxindole-based vasopressin 1b receptor antagonists with improved pharmacokinetic properties.EBI Abbott
21601454 26 Identification and optimisation of novel sulfonamide, selective vasopressin V1B receptor antagonists.EBI MSD
21428295 43 Design, synthesis, and pharmacological characterization of fluorescent peptides for imaging human V1b vasopressin or oxytocin receptors.EBI INSERM
21353540 55 Synthesis and SAR studies of novel 2-(4-oxo-2-aryl-quinazolin-3(4H)-yl)acetamide vasopressin V1b receptor antagonists.EBI MSD
20550119 96 Oral oxytocin antagonists.EBI DrugMolDesign
20813948 63 Spiroindolones, a potent compound class for the treatment of malaria.EBI Swiss Tropical and Public Health Institute
20719508 26 Identification and optimization of novel 2-(4-oxo-2-aryl-quinazolin-3(4H)-yl)acetamide vasopressin V3 (V1b) receptor antagonists.EBI Ligand Pharmaceuticals, Inc.
20471258 117 Synthesis and evaluation of azabicyclo[3.2.1]octane derivatives as potent mixed vasopressin antagonists.EBI Pfizer Global Research and Development
20189387 46 Identification of amide bioisosteres of triazole oxytocin antagonists.EBI Pfizer Global Research and Development
19963374 68 Triazole oxytocin antagonists: Identification of an aryloxyazetidine replacement for a biaryl substituent.EBI Pfizer Global Research and Development
19376698 16 Aryloxypyrazines as highly selective antagonists of Oxytocin.EBI Pfizer Global Research and Development
 66 Non-peptide oxytocin antagonists: identification and synthesis of a potent camphor aminosuccinimideEBI TBA
19053774 56 New benzylureas as a novel series of potent, nonpeptidic vasopressin V2 receptor agonists.EBI Vantia Ltd
18778939 23 Triazole oxytocin antagonists: identification of aryl ether replacements for a biaryl substituent.EBI Pfizer Global Research and Development
18639455 43 Design and optimization of potent, selective antagonists of Oxytocin.EBI Pfizer Global Research and Development
17942308 62 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
17855087 19 Identification and synthesis of major metabolites of Vasopressin V2-receptor agonist WAY-151932, and antagonist, Lixivaptan.EBI Wyeth Research
16392798 46 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
16153837 21 (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
15357997 22 Non-peptide oxytocin agonists.EBI Ferring Research Ltd
15125974 34 Synthesis and evaluation of spirobenzazepines as potent vasopressin receptor antagonists.EBI Johnson and Johnson Pharmaceutical Research and Development
14695824 31 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
14592501 33 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 L.L.C.
12798333 56 Structure-activity study of novel tricyclic benzazepine arginine vasopressin antagonists.EBI Wyeth Research
12639574 21 Synthesis and biological evaluation of novel indoloazepine derivatives as non-peptide vasopressin V2 receptor antagonists.EBI Johnson & Johnson Pharmaceutical Research & Development
12372506 41 Bridged bicyclic vasopressin receptor antagonists with V(2)-selective or dual V(1a)/V(2) activity.EBI Johnson and Johnson Pharmaceutical Research and Development
12166952 6 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 Company
12036368 59 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 Co. Ltd.
11087564 30 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 Company
10782686 13 The design, synthesis and physical chemical properties of novel human vasopressin V2-receptor antagonists optimized for parenteral delivery.EBI Wyeth-Ayerst Research
10782666 46 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
10406633 32 5-fluoro-2-methyl-N-[5-(5H-pyrrolo[2,1-c][1,4]benzodiazepine-10(11H)-yl carbonyl)-2-pyridinyl]benzamide (CL-385004) and analogs as orally active arginine vasopressin receptor antagonists.EBI Wyeth-Ayerst Research
10406632 11 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
10340620 30 Nonpeptide oxytocin antagonists: analogs of L-371,257 with improved potency.EBI Merck Research Laboratories
10197974 22 Fluorescent pseudo-peptide linear vasopressin antagonists: design, synthesis, and applications.EBI INSERM
9651149 54 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
8784453 134 Orally active, nonpeptide vasopressin V2 receptor antagonists: a novel series of 1-[4-(benzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H-benzazepines and related compounds.EBI Otsuka Pharmaceutical Co.
8393113 114 Orally active, nonpeptide vasopressin V1 antagonists. A novel series of 1-(1-substituted 4-piperidyl)-3,4-dihdyro-2(1H)-quinolinone.EBI Otsuka Pharmaceutical Co.
8258821 326 Nanomolar-affinity, non-peptide oxytocin receptor antagonists.EBI Merck Research Laboratories
8126695 35 1-((7,7-Dimethyl-2(S)-(2(S)-amino-4-(methylsulfonyl)butyramido)bicyclo [2.2.1]-heptan-1(S)-yl)methyl)sulfonyl)-4-(2-methylphenyl)piperaz ine (L-368,899): an orally bioavailable, non-peptide oxytocin antagonist with potential utility for managing preterm labor.EBI Merck Research Laboratories
8021923 27 A new series of photoactivatable and iodinatable linear vasopressin antagonists.EBI UPR 9023 CNRS
7473590 37 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
3397986 13 Dicarbavasopressin antagonist analogues exhibit reduced in vivo agonist activity.EBI Smith Kline & French Laboratories
2522994 7 A minor modification of residue 1 in potent vasopressin antagonists dramatically reduces agonist activity.EBI Smith Kline & French Laboratories
2521519 26 Structure-activity relationships of novel vasopressin antagonists containing C-terminal diaminoalkanes and (aminoalkyl)guanidines.EBI Smith Kline & French Laboratories
2163451 30 Cyclic hexapeptide oxytocin antagonists. Potency-, selectivity-, and solubility-enhancing modifications.EBI Merck Sharp & Dohme Research Laboratories
1331449 101 Orally active, nonpeptide oxytocin antagonists.EBI Merck Research Laboratories
15131245 86 SR147778 [5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(1-piperidinyl)-1H-pyrazole-3-carboxamide], a new potent and selective antagonist of the CB1 cannabinoid receptor: biochemical and pharmacological characterization.BDB Sanofi-Synthelabo Recherche
12660315 17 Pharmacology of (2S,4Z)-N-[(2S)-2-hydroxy-2-phenylethyl]-4-(methoxyimino) -1-[(2'-methyl[1,1'-biphenyl]-4-yl)carbonyl]-2-pyrrolidinecarboxamide, a new potent and selective nonpeptide antagonist of the oxytocin receptor.BDB LCG Bioscience
12649361 779 L-homocysteine sulfinic acid and other acidic homocysteine derivatives are potent and selective metabotropic glutamate receptor agonists.BDB Case Western Reserve University
12192085 52 Salvinorin A: a potent naturally occurring nonnitrogenous kappa opioid selective agonist.BDB Case Western Reserve University
12110997 380 In vitro receptor screening of pure constituents of St. John's wort reveals novel interactions with a number of GPCRs.BDB Westfälische Wilhelms-Universitä Muenster,
11861823 10 Characterization of (2S,4R)-1-[5-chloro-1-[(2,4-dimethoxyphenyl)sulfonyl]-3-(2-methoxy-phenyl)-2-oxo-2,3-dihydro-1H-indol-3-yl]-4-hydroxy-N,N-dimethyl-2-pyrrolidine carboxamide (SSR149415), a selective and orally active vasopressin V1b receptor antagonist.BDB Sanofi-Synthelabo Recherche
11512051 80 The in vitro pharmacology of the beta-adrenergic receptor pet ligand (s)-fluorocarazolol reveals high affinity for cloned beta-adrenergic receptors and moderate affinity for the human 5-HT1A receptor.BDB Case Western Reserve University
11082453 77 ABT-702 (4-amino-5-(3-bromophenyl)-7-(6-morpholinopyridin-3-yl)pyrido[2, 3-d]pyrimidine), a novel orally effective adenosine kinase inhibitor with analgesic and anti-inflammatory properties: I. In vitro characterization and acute antinociceptive effects in the mouse.BDB Abbott Laboratories
9864265 14 OPC-41061, a highly potent human vasopressin V2-receptor antagonist: pharmacological profile and aquaretic effect by single and multiple oral dosing in rats.BDB Second Tokushima Institute of New Drug Research
9454810 72 SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor.BDB Sanofi Recherche
9223568 38 Pharmacological profile of YM087, a novel potent nonpeptide vasopressin V1A and V2 receptor antagonist, in vitro and in vivo.BDB Yamanouchi Pharmaceutical Co., Ltd.
8012715 38 GR113808: a novel, selective antagonist with high affinity at the 5-HT4 receptor.BDB Glaxo Group Research Ltd.
1988661 44 In vitro pharmacological profile of a novel structural class of oxytocin antagonists.BDB Merck Sharp & Dohme Research Laboratories
10482466 32 7-Chloro-5-hydroxy-1-[2-methyl-4-(2-methylbenzoyl-amino)benzoyl ]-2,3,4,5-tetrahydro-1H-1-benzazepine (OPC-41061): a potent, orally active nonpeptide arginine vasopressin V2 receptor antagonist.BDB Otsuka Pharmaceutical Co., Ltd
18835174 17 Preparation of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepin-5-ylidene)acetamide derivatives as novel arginine vasopressin V(2) receptor agonists.BDB Astellas Pharma Inc.
19321349 46 Synthesis and structure-activity relationships of amide derivatives of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepin-5-ylidene)acetic acid as selective arginine vasopressin V2 receptor agonists.BDB Astellas Pharma Inc.
19900813 12 Optimization of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepine-5-ylidene)acetamide derivatives as arginine vasopressin V2 receptor agonists and discussion of their binding modes.BDB Astellas Pharma Inc.