SR 49059 is a potent, selective, non-peptide, orally active AVP Receptor V1a (Vasopressin V1a) antagonist. Devoid of agonist activity SR 49059 shows high affinity and efficacy at both rat (Ki = 1.6 nM) and human (Ki = 1.1-6.3 nM) V1a receptors. Potently antagonizes arginine vasopressin-induced effects in vitro.
Serradeil-Le Gal et al (1993) Biochemical and pharmacological properties of SR 49059, a new, potent, nonpeptide antagonist of rat and human vasopressin V1a receptors. J.Clin.Invest. 92 224. Serradeil-Le Gal et al (1994) Binding of [3H]SR 49059, a potent nonpeptide vasopressin V1a antagonist, to rat and human liver membranes. Biochem.Biophys.Res.Comm. 199 353. Tahtaoui et al (2003) Identification of the binding sites of the SR 49059 nonpeptide antagonist into the V1a vasopressin receptor using sulfydryl-reactive ligands and cysteine mutants as chemical sensors. J.Biol.Chem. 278 40010.
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CenksoyCenksoy, C. et al. (PubMed 24405730) presented a potential novel strategy, inhibition of vasopressin-induced VEGF secretion by SR 49059, for decreasing the incidence of ovarian hyperstimulation syndrome in the hyperstimulated rat model. -SCBT Publication Review
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