131 articles for thisTarget
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Article Title
Organization
Tactical Approaches to Interconverting GPCR Agonists and Antagonists.
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.
Teikyo University
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
Selective nonpeptidic fluorescent ligands for oxytocin receptor: design, synthesis, and application to time-resolved FRET binding assay.
University of Strasburg
New, potent, and selective peptidic oxytocin receptor agonists.
Ferring Research Institute
2,5-diketopiperazines as potent, selective, and orally bioavailable oxytocin antagonists. 2. Synthesis, chirality, and pharmacokinetics.
Glaxosmithkline
A comparative protease stability study of synthetic macrocyclic peptides that mimic two endocrine hormones.
The College of New Jersey
Colloidal aggregation causes inhibition of G protein-coupled receptors.
University of North Carolina At Chapel Hill
Optimisation of pharmacokinetic properties to afford an orally bioavailable and selective V1A receptor antagonist.
Msd
Pyrrolo[1,2-a]pyrazine and pyrazolo[1,5-a]pyrazine: novel, potent, and selective series of Vasopressin 1b receptor antagonists.
Glaxosmithkline
Discovery and optimisation of a potent and selective tertiary sulfonamide oxytocin antagonist.
Glaxosmithkline
Effects of a D-Cys6/L-Cys6 interchange in nonselective and selective vasopressin and oxytocin antagonists.
Medical College of Ohio
Selective fluorescent nonpeptidic antagonists for vasopressin V2 GPCR: application to ligand screening and oligomerization assays.
University of Strasburg
Pyridyl-2,5-diketopiperazines as potent, selective, and orally bioavailable oxytocin antagonists: synthesis, pharmacokinetics, and in vivo potency.
Glaxosmithkline
Synthesis and evaluation of C-11, F-18 and I-125 small molecule radioligands for detecting oxytocin receptors.
Emory University
Subtlety of the structure-affinity and structure-efficacy relationships around a nonpeptide oxytocin receptor agonist.
University of Strasburg
Tetrahydroquinoline sulfonamides as vasopressin 1b receptor antagonists.
Schering-Plough Research Institute
Discovery and optimization of highly ligand-efficient oxytocin receptor antagonists using structure-based drug design.
Glaxosmithkline
The discovery of GSK221149A: a potent and selective oxytocin antagonist.
Glaxosmithkline
Toward efficient drug screening by homogeneous assays based on the development of new fluorescent vasopressin and oxytocin receptor ligands.
Institute Genomics Functional (Igf)
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
Pyridobenzodiazepines: a novel class of orally active, vasopressin V2 receptor selective agonists.
Wyeth Research
Discovery and development of a new class of potent, selective, orally active oxytocin receptor antagonists.
Serono Pharmaceutical Research Institute
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
Synthesis and characterization of fluorescent antagonists and agonists for human oxytocin and vasopressin V(1)(a) receptors.
University of Montpellier
Enhanced selectivity of oxytocin antagonists containing sarcosine in position 7.
Max-Planck-Institut F£R Biophysik
Development of a novel class of cyclic hexapeptide oxytocin antagonists based on a natural product.
Merck Research Laboratories
Preparation and biological activities of potential vasopressin photoaffinity labels.
University of Sherbrooke
Receptor ligands which bind the oxytocin receptor with selectivity and high affinity. Chemical modification of a Streptomyces silvensis derived cyclic hexapeptide.
Merck
Synthesis and evaluation of nonpeptide substituted spirobenzazepines as potent vasopressin antagonists.
Johnson and Johnson Pharmaceutical Research and Development
Potent nonpeptide vasopressin receptor antagonists based on oxazino- and thiazinobenzodiazepine templates.
Johnson & Johnson Pharmaceutical Research & Development
N-Methylbenzanilide derivatives as a novel class of selective V(1A) receptor antagonists.
Yamanouchi Pharmaceutical
Synthesis of oxytocin antagonists containing conformationally constrained amino acids in position 2.
Albert Szent-Gy£Rgyi Medical University
Synthesis and evaluation of potent and selective human V1a receptor antagonists as potential ligands for PET or SPECT imaging.
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.
Pfizer
New, potent, selective, and short-acting peptidic V1a receptor agonists.
Ferring Research Institute
Potent and selective oxindole-based vasopressin 1b receptor antagonists with improved pharmacokinetic properties.
Abbott Laboratories
Identification and optimisation of novel sulfonamide, selective vasopressin V1B receptor antagonists.
Msd
Design, synthesis, and pharmacological characterization of fluorescent peptides for imaging human V1b vasopressin or oxytocin receptors.
University of Montpellier
Synthesis and SAR studies of novel 2-(4-oxo-2-aryl-quinazolin-3(4H)-yl)acetamide vasopressin V1b receptor antagonists.
Msd
Spiroindolones, a potent compound class for the treatment of malaria.
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.
Ligand Pharmaceuticals
Synthesis and evaluation of azabicyclo[3.2.1]octane derivatives as potent mixed vasopressin antagonists.
Pfizer
Triazole oxytocin antagonists: Identification of an aryloxyazetidine replacement for a biaryl substituent.
Pfizer
Vasopressin trisulphide: synthesis, NMR study and affinity studies with V1 and V2 subtypes receptors
TBA
Non-peptide oxytocin antagonists: identification and synthesis of a potent camphor aminosuccinimide
TBA
New benzylureas as a novel series of potent, nonpeptidic vasopressin V2 receptor agonists.
Vantia
Triazole oxytocin antagonists: identification of aryl ether replacements for a biaryl substituent.
Pfizer
Next-generation spirobenzazepines: identification of RWJ-676070 as a balanced vasopressin V1a/V2 receptor antagonist for human clinical studies.
Johnson & Johnson Pharmaceutical Research & Development
Identification and synthesis of major metabolites of Vasopressin V2-receptor agonist WAY-151932, and antagonist, Lixivaptan.
Wyeth Research
Optical-Controlled Kinetic Switch: Fine-Tuning of the Residence Time of an Antagonist Binding to the Vasopressin V
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.
Columbia University College of Physicians and Surgeons
(4-Substituted-phenyl)-(5H-10,11-dihydro-pyrrolo [2,1-c][1,4] benzodiazepin-10-yl)-methanone derivatives as vasopressin receptor modulators.
Wyeth Research
Synthesis and evaluation of spirobenzazepines as potent vasopressin receptor antagonists.
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.
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.
Johnson & Johnson Pharmaceutical Research & Development
Structure-activity study of novel tricyclic benzazepine arginine vasopressin antagonists.
Wyeth Research
Synthesis and biological evaluation of novel indoloazepine derivatives as non-peptide vasopressin V2 receptor antagonists.
Johnson & Johnson Pharmaceutical Research & Development
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
Yohimbine as a Starting Point to Access Diverse Natural Product-Like Agents with Re-programmed Activities against Cancer-Relevant GPCR Targets.
University of Florida
Bridged bicyclic vasopressin receptor antagonists with V(2)-selective or dual V(1a)/V(2) activity.
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.
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.
Yamanouchi Pharmaceutical
New V1a receptor antagonist. Part 2. Identification and optimization of triazolobenzazepines.
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.
Otsuka Pharmaceutical
The design, synthesis and physical chemical properties of novel human vasopressin V2-receptor antagonists optimized for parenteral delivery.
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.
Wyeth-Ayerst Research
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
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
Nonpeptide oxytocin antagonists: analogs of L-371,257 with improved potency.
Merck Research Laboratories
Fluorescent pseudo-peptide linear vasopressin antagonists: design, synthesis, and applications.
University of Montpellier
Discovery of SHR1653, a Highly Potent and Selective OTR Antagonist with Improved Blood-Brain Barrier Penetration.
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.
Wyeth-Ayerst Research
Engineering a Potent, Long-Acting, and Periphery-Restricted Oxytocin Receptor Agonist with Anorexigenic and Body Weight Reducing Effects.
Calibr At The Scripps Research Institute
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
Orally active, nonpeptide vasopressin V1 antagonists. A novel series of 1-(1-substituted 4-piperidyl)-3,4-dihdyro-2(1H)-quinolinone.
Otsuka Pharmaceutical
Nanomolar-affinity, non-peptide oxytocin receptor antagonists.
Merck Research Laboratories
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
A new series of photoactivatable and iodinatable linear vasopressin antagonists.
Upr 9023 Cnrs
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
Dicarbavasopressin antagonist analogues exhibit reduced in vivo agonist activity.
Smith Kline & French Laboratories
LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism.
Umr7200 Cnrs/Universit£
Design, synthesis, and biological activity of a peptide mimic of vasopressin.
Smith Kline and French Laboratories
Potent antagonists of vasopressin antidiuretic activity that lack the beta,beta-cyclopentamethylene-beta-mercaptopropionic acid substitution at position 1.
TBA
Novel vasopressin analogues that help define a minimum effective antagonist pharmacophore.
TBA
A minor modification of residue 1 in potent vasopressin antagonists dramatically reduces agonist activity.
Smith Kline & French Laboratories
Structure-activity relationships of novel vasopressin antagonists containing C-terminal diaminoalkanes and (aminoalkyl)guanidines.
Smith Kline & French Laboratories
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
Cyclic hexapeptide oxytocin antagonists. Potency-, selectivity-, and solubility-enhancing modifications.
Merck Sharp & Dohme Research Laboratories
Building bridges for highly selective, potent and stable oxytocin and vasopressin analogs.
Imperial College
Tolvaptan-Type Vasopressin Receptor Ligands: Important Role of Axial Chirality in the Active Form.
Teikyo University
SPIROCYCLIC MODULATORS OF CHOLESTEROL BIOSYNTHESIS AND THEIR USE FOR PROMOTING REMYELINATION
Genentech
8-(piperazin-1-yl)-1,2,3,4-tetrahydro-isoquinoline derivatives
Idorsia Pharmaceuticals
Substituted 2,3,4,5,7,9,13,13a-octahydropyrido[1′,2′:4,5]pyrazino[2,1-b][1,3]OXAZEPINES and methods for treating viral infections
Gilead Sciences
C2-carbocyclic iminothiazine dioxides as BACE inhibitors, compositions, and their use
Merck Sharp & Dohme
Diamino-pyridine, pyrimidine, and pyridazine modulators of the histamine H4 receptor
Janssen Pharmaceutica
Synthesis of hybrid molecules of caffeine and eudistomin D and its effects on adenosine receptors.
Hokkaido University
Ligand discovery from a dopamine D3 receptor homology model and crystal structure.
University of California San Francisco
Selective Inhibition of DNA Replicase Assembly by a Non-natural Nucleotide: Exploiting the Structural Diversity of ATP-Binding Sites
Case Western Reserve University
Correlating solution binding and ESI-MS stabilities by incorporating solvation effects in a confined cucurbit[8]uril system.
University of Cambridge
Discovery of a series of acrylic acids and their derivatives as chemical leads for selective EP3 receptor antagonists.
Ono Pharmaceutical
Antagonists of the human A(2A) receptor. Part 6: Further optimization of pyrimidine-4-carboxamides.
Vernalis (R&D)
3,4-Dihydropyrimido(1,2-a)indol-10(2H)-ones as potent non-peptidic inhibitors of caspase-3.
Wyeth Research
Design, synthesis, and X-ray crystal structures of 2,4-diaminofuro[2,3-d]pyrimidines as multireceptor tyrosine kinase and dihydrofolate reductase inhibitors.
Duquesne University
Structure-activity relationship studies of phenanthridine-based Bcl-XL inhibitors.
A* Star
Carbonic anhydrase inhibitors: clash with Ala65 as a means for designing inhibitors with low affinity for the ubiquitous isozyme II, exemplified by the crystal structure of the topiramate sulfamide analogue.
Universite Montpellier Ii