65 articles for thisTarget
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Article Title
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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
Optimisation of pharmacokinetic properties to afford an orally bioavailable and selective V1A receptor antagonist.
Msd
The discovery of novel 8-azabicyclo[3.2.1]octan-3-yl)-3-(4-chlorophenyl) propanamides as vasopressin V1A receptor antagonists.
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
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
Tetrahydroquinoline sulfonamides as vasopressin 1b receptor antagonists.
Schering-Plough Research Institute
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
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
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
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
Synthesis and SAR studies of novel 2-(6-aminomethylaryl-2-aryl-4-oxo-quinazolin-3(4H)-yl)acetamide 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
Identification and optimization of novel 2-(4-oxo-2-aryl-quinazolin-3(4H)-yl)acetamide vasopressin V3 (V1b) receptor antagonists.
Ligand Pharmaceuticals
Vasopressin trisulphide: synthesis, NMR study and affinity studies with V1 and V2 subtypes receptors
TBA
Triazole oxytocin antagonists: identification of aryl ether replacements for a biaryl substituent.
Pfizer
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
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
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
Hormone-like conopeptides - new tools for pharmaceutical design.
University of Queensland
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
Synthesis of oxytocin derivatives lipidated via a carbonate or carbamate linkage as a long-acting therapeutic agent for social impairment-like behaviors.
Kanazawa University
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
Engineering a Potent, Long-Acting, and Periphery-Restricted Oxytocin Receptor Agonist with Anorexigenic and Body Weight Reducing Effects.
Calibr At The Scripps Research Institute
Nanomolar-affinity, non-peptide oxytocin receptor antagonists.
Merck Research Laboratories
Novel, potent, selective and brain penetrant vasopressin 1b receptor antagonists.
Abbvie Deutschland
LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism.
Umr7200 Cnrs/Universit£
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
Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b.
University of Leipzig
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
The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C.
Laboratoires Glaxo