Mozavaptan-d6 is intended for use as an internal standard for the quantification of mozavaptan by GC- or LC-MS. Mozavaptan is an orally bioavailable antagonist of vasopressin V2 receptors (Ki = 9.42 nM in HeLa cells expressing the human receptor).1,2 It is selective for vasopressin V2 over V1 receptors (IC50s = 14 and 1,200 nM, respectively) in radioligand binding assays using rat kidney and rat liver membranes that endogenously express high levels of vasopressin V2 and V1 receptors, respectively.1 Mozavaptan (10-30 mg/kg, p.o.) increases urine volume and decreases urine osmolality, indicating aquaresis, in conscious rats. It reduces decreases in urine flow and increases in urine osmolality induced by arginine vasopressin in anesthetized rats when administered intravenously at doses ranging from 10 to 100 µg/kg.
1.Yamamura, Y., Ogawa, H., Yamashita, H., et al.Characterization of a novel aquaretic agent, OPC-31260, as an orally effective, nonpeptide vasopressin V2 receptor antagonistBr. J. Pharmacol.105(4)787-791(1992) 2.Nakamura, S., Itoh, S., Fujiki, H., et al.Binding affinities of mozavaptan hydrochloride (OPC-31260) for vasopressin receptorsJap. Pharmacol. Ther.34(7)827-834(2006)