The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 26390077 |
42 |
Tactical Approaches to Interconverting GPCR Agonists and Antagonists. |
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. |
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. |
F. Hoffmann-La Roche |
| 25642985 |
45 |
Selective nonpeptidic fluorescent ligands for oxytocin receptor: design, synthesis, and application to time-resolved FRET binding assay. |
University of Strasburg |
| 24874785 |
333 |
New, potent, and selective peptidic oxytocin receptor agonists. |
Ferring Research Institute |
| 16250654 |
41 |
2,5-diketopiperazines as potent, selective, and orally bioavailable oxytocin antagonists. 2. Synthesis, chirality, and pharmacokinetics. |
Glaxosmithkline |
| 23312470 |
3 |
A comparative protease stability study of synthetic macrocyclic peptides that mimic two endocrine hormones. |
The College of New Jersey |
| 23437772 |
35 |
Colloidal aggregation causes inhibition of G protein-coupled receptors. |
University of North Carolina At Chapel Hill |
| 21700453 |
56 |
Optimisation of pharmacokinetic properties to afford an orally bioavailable and selective V1A receptor antagonist. |
Msd |
| 20674355 |
58 |
Pyrrolo[1,2-a]pyrazine and pyrazolo[1,5-a]pyrazine: novel, potent, and selective series of Vasopressin 1b receptor antagonists. |
Glaxosmithkline |
| 19081251 |
38 |
Discovery and optimisation of a potent and selective tertiary sulfonamide oxytocin antagonist. |
Glaxosmithkline |
| 7752199 |
71 |
Effects of a D-Cys6/L-Cys6 interchange in nonselective and selective vasopressin and oxytocin antagonists. |
Medical College of Ohio |
| 22984902 |
59 |
Selective fluorescent nonpeptidic antagonists for vasopressin V2 GPCR: application to ligand screening and oligomerization assays. |
University of Strasburg |
| 22239250 |
59 |
Pyridyl-2,5-diketopiperazines as potent, selective, and orally bioavailable oxytocin antagonists: synthesis, pharmacokinetics, and in vivo potency. |
Glaxosmithkline |
| 22425346 |
28 |
Synthesis and evaluation of C-11, F-18 and I-125 small molecule radioligands for detecting oxytocin receptors. |
Emory University |
| 20104850 |
48 |
Subtlety of the structure-affinity and structure-efficacy relationships around a nonpeptide oxytocin receptor agonist. |
University of Strasburg |
| 19800231 |
92 |
Tetrahydroquinoline sulfonamides as vasopressin 1b receptor antagonists. |
Schering-Plough Research Institute |
| 19095447 |
28 |
Discovery and optimization of highly ligand-efficient oxytocin receptor antagonists using structure-based drug design. |
Glaxosmithkline |
| 18032036 |
17 |
The discovery of GSK221149A: a potent and selective oxytocin antagonist. |
Glaxosmithkline |
| 17850055 |
18 |
Toward efficient drug screening by homogeneous assays based on the development of new fluorescent vasopressin and oxytocin receptor ligands. |
Institute Genomics Functional (Igf) |
| 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. |
University of Montpellier |
| 16297621 |
17 |
Pyridobenzodiazepines: a novel class of orally active, vasopressin V2 receptor selective agonists. |
Wyeth Research |
| 16302826 |
129 |
Discovery and development of a new class of potent, selective, orally active oxytocin receptor antagonists. |
Serono Pharmaceutical Research Institute |
| 7241506 |
40 |
New analgesic drugs derived from phencyclidine. |
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. |
Medical College of Ohio |
| 12036367 |
46 |
Synthesis and characterization of fluorescent antagonists and agonists for human oxytocin and vasopressin V(1)(a) receptors. |
University of Montpellier |
| 7507528 |
23 |
Enhanced selectivity of oxytocin antagonists containing sarcosine in position 7. |
Max-Planck-Institut F£R Biophysik |
| 1331448 |
101 |
Development of a novel class of cyclic hexapeptide oxytocin antagonists based on a natural product. |
Merck Research Laboratories |
| 1732523 |
46 |
Preparation and biological activities of potential vasopressin photoaffinity labels. |
University of Sherbrooke |
| 2167976 |
33 |
Receptor ligands which bind the oxytocin receptor with selectivity and high affinity. Chemical modification of a Streptomyces silvensis derived cyclic hexapeptide. |
Merck |
| 15149662 |
71 |
Synthesis and evaluation of nonpeptide substituted spirobenzazepines as potent vasopressin antagonists. |
Johnson and Johnson Pharmaceutical Research and Development |
| 15125926 |
88 |
Potent nonpeptide vasopressin receptor antagonists based on oxazino- and thiazinobenzodiazepine templates. |
Johnson & Johnson Pharmaceutical Research & Development |
| 11755361 |
24 |
N-Methylbenzanilide derivatives as a novel class of selective V(1A) receptor antagonists. |
Yamanouchi Pharmaceutical |
| 10201826 |
24 |
Synthesis of oxytocin antagonists containing conformationally constrained amino acids in position 2. |
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. |
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. |
Pfizer |
| 21688787 |
295 |
New, potent, selective, and short-acting peptidic V1a receptor agonists. |
Ferring Research Institute |
| 21605973 |
69 |
Potent and selective oxindole-based vasopressin 1b receptor antagonists with improved pharmacokinetic properties. |
Abbott Laboratories |
| 21601454 |
26 |
Identification and optimisation of novel sulfonamide, selective vasopressin V1B receptor antagonists. |
Msd |
| 21428295 |
43 |
Design, synthesis, and pharmacological characterization of fluorescent peptides for imaging human V1b vasopressin or oxytocin receptors. |
University of Montpellier |
| 21353540 |
55 |
Synthesis and SAR studies of novel 2-(4-oxo-2-aryl-quinazolin-3(4H)-yl)acetamide vasopressin V1b receptor antagonists. |
Msd |
| 20550119 |
96 |
Oral oxytocin antagonists. |
Drugmoldesign |
| 20813948 |
63 |
Spiroindolones, a potent compound class for the treatment of malaria. |
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. |
Ligand Pharmaceuticals |
| 20471258 |
117 |
Synthesis and evaluation of azabicyclo[3.2.1]octane derivatives as potent mixed vasopressin antagonists. |
Pfizer |
| 20189387 |
46 |
Identification of amide bioisosteres of triazole oxytocin antagonists. |
Pfizer |
| 19963374 |
68 |
Triazole oxytocin antagonists: Identification of an aryloxyazetidine replacement for a biaryl substituent. |
Pfizer |
| 19376698 |
16 |
Aryloxypyrazines as highly selective antagonists of Oxytocin. |
Pfizer |
| | 4 |
Vasopressin trisulphide: synthesis, NMR study and affinity studies with V1 and V2 subtypes receptors |
TBA |
| | 66 |
Non-peptide oxytocin antagonists: identification and synthesis of a potent camphor aminosuccinimide |
TBA |
| | 9 |
Potent, non-peptidic oxytocin receptor antagonists from a natural source |
TBA |
| 19053774 |
56 |
New benzylureas as a novel series of potent, nonpeptidic vasopressin V2 receptor agonists. |
Vantia |
| 18778939 |
23 |
Triazole oxytocin antagonists: identification of aryl ether replacements for a biaryl substituent. |
Pfizer |
| 18639455 |
43 |
Design and optimization of potent, selective antagonists of Oxytocin. |
Pfizer |
| 17942308 |
62 |
Next-generation spirobenzazepines: identification of RWJ-676070 as a balanced vasopressin V1a/V2 receptor antagonist for human clinical studies. |
Johnson & Johnson Pharmaceutical Research & Development |
| 17855087 |
19 |
Identification and synthesis of major metabolites of Vasopressin V2-receptor agonist WAY-151932, and antagonist, Lixivaptan. |
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. |
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. |
Wyeth Research |
| 15357997 |
22 |
Non-peptide oxytocin agonists. |
Ferring Research |
| 15125974 |
34 |
Synthesis and evaluation of spirobenzazepines as potent vasopressin receptor antagonists. |
Johnson and Johnson Pharmaceutical Research and Development |
| 14695824 |
68 |
Synthesis and structure-activity relationships of 5,6,7,8-tetrahydro-4H-thieno[3,2-b]azepine derivatives: novel arginine vasopressin antagonists. |
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. |
Johnson & Johnson Pharmaceutical Research & Development |
| 12798333 |
56 |
Structure-activity study of novel tricyclic benzazepine arginine vasopressin antagonists. |
Wyeth Research |
| 12639574 |
21 |
Synthesis and biological evaluation of novel indoloazepine derivatives as non-peptide vasopressin V2 receptor antagonists. |
Johnson & Johnson Pharmaceutical Research & Development |
| 12502367 |
17 |
New benzo[h][1,6]naphthyridine and azepino[3,2-c]quinoline derivatives as selective antagonists of 5-HT4 receptors: binding profile and pharmacological characterization. |
Université |
| 12372506 |
41 |
Bridged bicyclic vasopressin receptor antagonists with V(2)-selective or dual V(1a)/V(2) activity. |
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. |
Otsuka Pharmaceutical |
| 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. |
Yamanouchi Pharmaceutical |
| 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. |
Otsuka Pharmaceutical |
| 10782686 |
13 |
The design, synthesis and physical chemical properties of novel human vasopressin V2-receptor antagonists optimized for parenteral delivery. |
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. |
Wyeth-Ayerst Research |
| 31022340 |
101 |
Discovery of Potent, Selective, and Short-Acting Peptidic V |
Ferring Research Institute |
| 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. |
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. |
Wyeth-Ayerst Research |
| 10340620 |
30 |
Nonpeptide oxytocin antagonists: analogs of L-371,257 with improved potency. |
Merck Research Laboratories |
| 10197974 |
22 |
Fluorescent pseudo-peptide linear vasopressin antagonists: design, synthesis, and applications. |
University of Montpellier |
| 31223461 |
56 |
Discovery of SHR1653, a Highly Potent and Selective OTR Antagonist with Improved Blood-Brain Barrier Penetration. |
Shanghai Hengrui Pharmaceutical |
| 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. |
Wyeth-Ayerst Research |
| 31850759 |
24 |
Engineering a Potent, Long-Acting, and Periphery-Restricted Oxytocin Receptor Agonist with Anorexigenic and Body Weight Reducing Effects. |
Calibr At The Scripps Research Institute |
| 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. |
Otsuka Pharmaceutical |
| 8393113 |
114 |
Orally active, nonpeptide vasopressin V1 antagonists. A novel series of 1-(1-substituted 4-piperidyl)-3,4-dihdyro-2(1H)-quinolinone. |
Otsuka Pharmaceutical |
| 8258821 |
491 |
Nanomolar-affinity, non-peptide oxytocin receptor antagonists. |
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. |
Merck Research Laboratories |
| 8021923 |
27 |
A new series of photoactivatable and iodinatable linear vasopressin antagonists. |
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. |
Merck Research Laboratories |
| 3397986 |
14 |
Dicarbavasopressin antagonist analogues exhibit reduced in vivo agonist activity. |
Smith Kline & French Laboratories |
| 30199637 |
172 |
LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism. |
Umr7200 Cnrs/Universit£ |
| 2965243 |
4 |
Design, synthesis, and biological activity of a peptide mimic of vasopressin. |
Smith Kline and French Laboratories |
| 2946863 |
4 |
Potent antagonists of vasopressin antidiuretic activity that lack the beta,beta-cyclopentamethylene-beta-mercaptopropionic acid substitution at position 1. |
TBA |
| 2940368 |
9 |
Potent vasopressin antagonists lacking the proline residue at position 7. |
TBA |
| 2933517 |
14 |
Novel vasopressin analogues that help define a minimum effective antagonist pharmacophore. |
TBA |
| 2522994 |
7 |
A minor modification of residue 1 in potent vasopressin antagonists dramatically reduces agonist activity. |
Smith Kline & French Laboratories |
| 2521519 |
26 |
Structure-activity relationships of novel vasopressin antagonists containing C-terminal diaminoalkanes and (aminoalkyl)guanidines. |
Smith Kline & French Laboratories |
| 2416923 |
40 |
Arginine-vasopressin analogues with high antidiuretic/vasopressor selectivity. Synthesis, biological activity, and receptor binding affinity of arginine-vasopressin analogues with substitutions in positions 1, 2, 4, 7, and 8. |
TBA |
| 2163451 |
45 |
Cyclic hexapeptide oxytocin antagonists. Potency-, selectivity-, and solubility-enhancing modifications. |
Merck Sharp & Dohme Research Laboratories |
| 29602673 |
49 |
Building bridges for highly selective, potent and stable oxytocin and vasopressin analogs. |
Imperial College |
| 1331449 |
268 |
Orally active, nonpeptide oxytocin antagonists. |
Merck Research Laboratories |
| 28475329 |
18 |
Tolvaptan-Type Vasopressin Receptor Ligands: Important Role of Axial Chirality in the Active Form. |
Teikyo University |
| 17221184 |
55 |
Synthesis and in vivo evaluation of a novel 5-HT1A receptor agonist radioligand [O-methyl- 11C]2-(4-(4-(2-methoxyphenyl)piperazin-1-yl)butyl)-4-methyl-1,2,4-triazine-3,5(2H,4H)dione in nonhuman primates. |
Columbia University |
| 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. |
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. |
Lcg Bioscience |
| 12649361 |
779 |
L-homocysteine sulfinic acid and other acidic homocysteine derivatives are potent and selective metabotropic glutamate receptor agonists. |
Case Western Reserve University |
| 12192085 |
52 |
Salvinorin A: a potent naturally occurring nonnitrogenous kappa opioid selective agonist. |
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. |
WestfÄLische Wilhelms-UniversitÄ |
| 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. |
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. |
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. |
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. |
Second Tokushima Institute of New Drug Research |
| 9454810 |
72 |
SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor. |
Sanofi Recherche |
| 9223568 |
38 |
Pharmacological profile of YM087, a novel potent nonpeptide vasopressin V1A and V2 receptor antagonist, in vitro and in vivo. |
Yamanouchi Pharmaceutical |
| 8012715 |
38 |
GR113808: a novel, selective antagonist with high affinity at the 5-HT4 receptor. |
Glaxo Group Research |
| 1988661 |
44 |
In vitro pharmacological profile of a novel structural class of oxytocin antagonists. |
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. |
Otsuka Pharmaceutical |
| 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. |
Astellas Pharma |
| 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. |
Astellas Pharma |
| 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. |
Astellas Pharma |
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