Mozavaptan

Mozavaptan (OPC-31260) is a potent, selective nonpeptide vasopressin V2 receptor antagonist with IC50 of 14 nM; 100-fold less potent for VP1 (IC50=1.2 uM) ; dose-dependently increases urine flow and decreases urine osmolality in normal conscious rats; orally effective.Other Indication Approved (In Vitro) :Mozavaptan (OPC-31260) inhibits AVP binding to binding to rat liver (V1 receptor) and kidney (V2 receptor) plasma membranes in a competitive manner and that it is about 100 times more selective for V2 receptors. Kd value for [3H]-AVP in rat liver is 1.1 nM; in rat kidney is 1.38 nM. The Kd of [3H]-AVP is reduced significantly in both rat liver and kidney in the presence of Mozavaptan (Kd of 2.47 nM and 5.51 nM for V1 receptor at the doses of 0.3 μM and 1 μM.respectively; Kd of 2.4 nM and 4.03 nM for V2 receptor at the doses of 0.3 μM and 1 μM.respectively) . (In Vivo) :Mozavaptan (OPC-31260; 1-30 mg/kg; oral administration; hydrated conscious rats) treatment dose-dependently increases urine flow and decreased urine osmolality.Mozavaptan (OPC-31260; 10-100 μg/kg; intravenous injection; male Sprague-Dawley rats) treatment inhibits the antidiuretic action of exogenously administered arginine vasopressin (AVP) in water-loaded, alcohol-anaesthetized rats in a dose-dependent manner.