105 articles for thisTarget
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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
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
Flexible analogues of WAY-267,464: Synthesis and pharmacology at the human oxytocin and vasopressin 1a receptors.
The University of Sydney
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
Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).
Glaxosmithkline
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
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
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)
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 benzophenone-containing photoactivatable linear vasopressin antagonists: pharmacological and photoreactive properties.
University of Montpellier
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 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
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
A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.
Università
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
Triazole oxytocin antagonists: identification of aryl ether replacements for a biaryl substituent.
Pfizer
Discovery of potent and selective adamantane-based small-molecule P2X(7) receptor antagonists/interleukin-1beta inhibitors.
Astrazeneca R&D Charnwood
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
Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: increased receptor specificity and in vivo activity.
Jerini
(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
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
Synthesis and biological evaluation of novel indoloazepine derivatives as non-peptide vasopressin V2 receptor antagonists.
Johnson & Johnson Pharmaceutical Research & Development
New V1a receptor antagonist. Part 1. Synthesis and SAR development of urea derivatives.
Gedeon Richter
Bridged bicyclic vasopressin receptor antagonists with V(2)-selective or dual V(1a)/V(2) activity.
Johnson and Johnson Pharmaceutical Research and Development
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
Identification of potent and selective oxytocin antagonists. Part 2: further investigation of benzofuran derivatives.
Glaxosmithkline
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 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
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
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
Discovery of SHR1653, a Highly Potent and Selective OTR Antagonist with Improved Blood-Brain Barrier Penetration.
Shanghai Hengrui Pharmaceutical
Functionalized 6-(Piperidin-1-yl)-8,9-Diphenyl Purines as Peripherally Restricted Inverse Agonists of the CB1 Receptor.
Rti International
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
Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example.
Janssen Pharmaceutica
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
Receptor-Ligand Interaction Measured by Inductively Coupled Plasma Mass Spectrometry and Selenium Labeling.
University of Montpellier
LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism.
Umr7200 Cnrs/Universit£
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
Identification and biological evaluation of thiazole-based inverse agonists of ROR?t.
Phenex Pharmaceuticals
Building bridges for highly selective, potent and stable oxytocin and vasopressin analogs.
Imperial College
Potent and selective oxytocin receptor agonists without disulfide bridges.
Takeda Pharmaceutical
Tolvaptan-Type Vasopressin Receptor Ligands: Important Role of Axial Chirality in the Active Form.
Teikyo University
New natural cholinesterase inhibiting and calcium channel blocking quinoline alkaloids.
University of Karachi
The motilin pharmacophore in CHO cells expressing the human motilin receptor.
Katholieke Universiteit Leuven
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
Discovery of novel spirocyclopropyl hydroxamate and carboxylate compounds as TACE inhibitors.
Schering-Plough Research Institute
High-throughput screening for potent and selective inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase.
University of Texas Southwestern Medical Center