The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
28001064 |
16 |
Recent Advances in Scaffold Hopping. |
Rheinische Friedrich-Wilhelms-Universit£T |
27876250 |
60 |
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH |
Jagiellonian University Medical College |
26988801 |
55 |
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents. |
Jagiellonian University Medical College |
26741855 |
65 |
Flexible analogues of WAY-267,464: Synthesis and pharmacology at the human oxytocin and vasopressin 1a receptors. |
The University of Sydney |
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 |
24881566 |
140 |
Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120). |
Glaxosmithkline |
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 |
21700453 |
56 |
Optimisation of pharmacokinetic properties to afford an orally bioavailable and selective V1A receptor antagonist. |
Msd |
21458261 |
55 |
The discovery of novel 8-azabicyclo[3.2.1]octan-3-yl)-3-(4-chlorophenyl) propanamides as vasopressin V1A receptor antagonists. |
Msd |
21146408 |
53 |
The characterization of a novel V1b antagonist lead series. |
Glaxosmithkline |
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 |
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 |
15857144 |
10 |
Design of benzophenone-containing photoactivatable linear vasopressin antagonists: pharmacological and photoreactive properties. |
University of Montpellier |
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 |
11585444 |
295 |
From hit to lead. Analyzing structure-profile relationships. |
Universities of Lille |
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 |
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 |
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 |
20591666 |
66 |
A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase. |
Università |
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 |
20172721 |
21 |
Identification of a urea bioisostere of a triazole oxytocin antagonist. |
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 |
7807119 |
5 |
Khusimol, a Non-Peptide Ligand for Vasopressin V1a Receptors |
TBA |
| 66 |
Non-peptide oxytocin antagonists: identification and synthesis of a potent camphor aminosuccinimide |
TBA |
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 |
17963373 |
36 |
Discovery of potent and selective adamantane-based small-molecule P2X(7) receptor antagonists/interleukin-1beta inhibitors. |
Astrazeneca R&D Charnwood |
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 |
17234419 |
79 |
Azetidinones as vasopressin V1a antagonists. |
Lehigh University |
16876401 |
48 |
Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: increased receptor specificity and in vivo activity. |
Jerini |
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 |
15125974 |
34 |
Synthesis and evaluation of spirobenzazepines as potent vasopressin receptor antagonists. |
Johnson and Johnson Pharmaceutical Research and Development |
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 |
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 |
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 |
11992787 |
37 |
Identification of potent and selective oxytocin antagonists. Part 2: further investigation of benzofuran derivatives. |
Glaxosmithkline |
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 |
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 |
30896946 |
36 |
Development of a Highly Potent Analogue and a Long-Acting Analogue of Oxytocin for the Treatment of Social Impairment-Like Behaviors. |
Tohoku University and Department of Pharmaceutical Sciences |
31229420 |
21 |
Synthesis of oxytocin derivatives lipidated via a carbonate or carbamate linkage as a long-acting therapeutic agent for social impairment-like behaviors. |
Kanazawa University |
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 |
31185168 |
144 |
Functionalized 6-(Piperidin-1-yl)-8,9-Diphenyl Purines as Peripherally Restricted Inverse Agonists of the CB1 Receptor. |
Rti International |
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 |
26565745 |
165 |
Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
Janssen Pharmaceutica |
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 |
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 |
30395477 |
26 |
Receptor-Ligand Interaction Measured by Inductively Coupled Plasma Mass Spectrometry and Selenium Labeling. |
University of Montpellier |
30199637 |
172 |
LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism. |
Umr7200 Cnrs/Universit£ |
29126725 |
95 |
Conformationally rigid derivatives of WAY-267,464: Synthesis and pharmacology at the human oxytocin and vasopressin-1a receptors. |
The University of Sydney |
28505537 |
35 |
Investigation of pyrazolo-sulfonamides as putative small molecule oxytocin receptor agonists. |
The University of Sydney |
29631962 |
252 |
Identification and biological evaluation of thiazole-based inverse agonists of ROR?t. |
Phenex Pharmaceuticals |
29602673 |
49 |
Building bridges for highly selective, potent and stable oxytocin and vasopressin analogs. |
Imperial College |
28438540 |
207 |
Potent and selective oxytocin receptor agonists without disulfide bridges. |
Takeda Pharmaceutical |
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 |
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 |
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 |
9223568 |
38 |
Pharmacological profile of YM087, a novel potent nonpeptide vasopressin V1A and V2 receptor antagonist, in vitro and in vivo. |
Yamanouchi Pharmaceutical |
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 |
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 |