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 |
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) |
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 |
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 |
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 |
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 |
12639574 |
21 |
Synthesis and biological evaluation of novel indoloazepine derivatives as non-peptide vasopressin V2 receptor antagonists. |
Johnson & Johnson Pharmaceutical Research & Development |
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 |
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 |
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£ |
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 |
29602673 |
49 |
Building bridges for highly selective, potent and stable oxytocin and vasopressin analogs. |
Imperial College |
28475329 |
18 |
Tolvaptan-Type Vasopressin Receptor Ligands: Important Role of Axial Chirality in the Active Form. |
Teikyo University |
26833890 |
18 |
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. |
Yogi Vemana University |
26469307 |
7 |
Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b. |
University of Leipzig |
17252943 |
10 |
New natural cholinesterase inhibiting and calcium channel blocking quinoline alkaloids. |
University of Karachi |
15968818 |
10 |
Benzofuran- and furan-2-yl-(phenyl)-3-pyridylmethanols: synthesis and inhibition of P450 aromatase. |
Cardiff University |
12054506 |
26 |
The motilin pharmacophore in CHO cells expressing the human motilin receptor. |
Katholieke Universiteit Leuven |
12023553 |
5 |
Functional selectivity of dopamine receptor agonists. II. Actions of dihydrexidine in D2L receptor-transfected MN9D cells and pituitary lactotrophs. |
University of North Carolina At Chapel Hill |
16302795 |
36 |
Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity. |
Merck Frosst Centre For Therapeutic Research |
11585446 |
6 |
Synthesis of novel, potent, diol-based HIV-1 protease inhibitors via intermolecular pinacol homocoupling of (2S)-2-benzyloxymethyl-4-phenylbutanal. |
Stockholm University |