99 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
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An evaluation of central penetration from a peripherally administered oxytocin receptor selective antagonist in nonhuman primates.
Emory University
Identification of potent and selective oxytocin antagonists. Part 1: indole and benzofuran derivatives.
Glaxosmithkline
Structure-activity relationship investigations of a potent and selective benzodiazepine oxytocin antagonist.
Glaxosmithkline
Systematic N-methylation of oxytocin: Impact on pharmacology and intramolecular hydrogen bonding network.
Pfizer
Flexible analogues of WAY-267,464: Synthesis and pharmacology at the human oxytocin and vasopressin 1a receptors.
The University of Sydney
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
Investigation of an F-18 oxytocin receptor selective ligand via PET imaging.
Emory University
Carbon-11 N-methyl alkylation of L-368,899 and in vivo PET imaging investigations for neural oxytocin receptors.
Yerkes National Primate Research Center
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
Peptide science: exploring the use of chemical principles and interdisciplinary collaboration for understanding life processes.
University of Arizona
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
Receptor ligands which bind the oxytocin receptor with selectivity and high affinity. Chemical modification of a Streptomyces silvensis derived cyclic hexapeptide.
Merck
Synthesis of oxytocin antagonists containing conformationally constrained amino acids in position 2.
Albert Szent-Gy£Rgyi Medical 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
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
Modulating oxytocin activity and plasma stability by disulfide bond engineering.
The University of Queensland
Identification and optimization of novel 2-(4-oxo-2-aryl-quinazolin-3(4H)-yl)acetamide vasopressin V3 (V1b) receptor antagonists.
Ligand Pharmaceuticals
Triazole oxytocin antagonists: Identification of an aryloxyazetidine replacement for a biaryl substituent.
Pfizer
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
Identification and synthesis of major metabolites of Vasopressin V2-receptor agonist WAY-151932, and antagonist, Lixivaptan.
Wyeth Research
Synthesis and biological activity of oxytocin analogues containing conformationally-restricted residues in position 7.
University of Patras
Structure-Based Design of Glycosylated Oxytocin Analogues with Improved Selectivity and Antinociceptive Activity.
The University of Arizona
2,5-diketopiperazines as potent, selective, and orally bioavailable oxytocin antagonists. 3. Synthesis, pharmacokinetics, and in vivo potency.
Cardiovascular and Urogenital Centre of Excellence For Drug Discovery
Yohimbine as a Starting Point to Access Diverse Natural Product-Like Agents with Re-programmed Activities against Cancer-Relevant GPCR Targets.
University of Florida
Identification of potent and selective oxytocin antagonists. Part 2: further investigation of benzofuran derivatives.
Glaxosmithkline
Design, synthesis and pharmacological characterization of a potent radioiodinated and photoactivatable peptidic oxytocin antagonist.
University of Montpellier
Identification of a potent and selective oxytocin antagonist, from screening a fully encoded differential release combinatorial chemical library.
Glaxosmithkline
Design and Characterization of Superpotent Bivalent Ligands Targeting Oxytocin Receptor Dimers via a Channel-Like Structure.
Institute of Neuroscience
A study of the relationship between biological activity and prolyl amide isomer geometry in oxytocin using 5-tert-butylproline to augment the Cys(6)-Pro(7) amide cis-isomer population.
Université
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
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
Nonpeptide oxytocin antagonists: potent, orally bioavailable analogs of L-371,257 containing a 1-R-(pyridyl)ethyl ether terminus.
Merck Research Laboratories
Discovery of SHR1653, a Highly Potent and Selective OTR Antagonist with Improved Blood-Brain Barrier Penetration.
Shanghai Hengrui Pharmaceutical
Peptidomimetic growth hormone secretagogues. Design considerations and therapeutic potential.
Merck Research Laboratories
Development of orally active oxytocin antagonists: studies on 1-(1-[4-[1-(2-methyl-1-oxidopyridin-3-ylmethyl)piperidin-4-yloxy]-2- methoxybenzoyl]piperidin-4-yl)-1,4-dihydrobenz[d][1,3]oxazin-2-one (L-372,662) and related pyridines.
Merck Research Laboratories
Engineering a Potent, Long-Acting, and Periphery-Restricted Oxytocin Receptor Agonist with Anorexigenic and Body Weight Reducing Effects.
Calibr At The Scripps Research Institute
Synthesis and pharmacology of novel analogues of oxytocin and deaminooxytocin: directed methods for the construction of disulfide and trisulfide bridges in peptides.
University of Minnesota
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
LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism.
Umr7200 Cnrs/Universit£
Discovery, Synthesis, Pharmacological Profiling, and Biological Characterization of Brintonamides A-E, Novel Dual Protease and GPCR Modulators from a Marine Cyanobacterium.
University of Florida
Conformationally rigid derivatives of WAY-267,464: Synthesis and pharmacology at the human oxytocin and vasopressin-1a receptors.
The University of Sydney
Investigation of pyrazolo-sulfonamides as putative small molecule oxytocin receptor agonists.
The University of Sydney
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
Targets for Drug Therapy for Autism Spectrum Disorder: Challenges and Future Directions.
Universit£
Potent and selective oxytocin receptor agonists without disulfide bridges.
Takeda Pharmaceutical
N-(4-tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide (BCTC), a novel, orally effective vanilloid receptor 1 antagonist with analgesic properties: I. in vitro characterization and pharmacokinetic properties.
Pudue Pharma Discovery Research
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
L-homocysteine sulfinic acid and other acidic homocysteine derivatives are potent and selective metabotropic glutamate receptor agonists.
Case Western Reserve University
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
Pharmacological profile of YM087, a novel potent nonpeptide vasopressin V1A and V2 receptor antagonist, in vitro and in vivo.
Yamanouchi Pharmaceutical