Mozavaptan 是 benzazepine 衍生物，是一种竞争性加压素受体拮抗剂，作用于 V1 和 V2 受体，IC50 分别为 1.2 μM 和 14 nM。它可在体内拮抗精氨酸加压素的抗利尿作用，可用于低钠血症、抗利尿激素不适当综合征和充血性心力衰竭的研究。

Mozavaptan is a competitive vasopressin receptor antagonist for both V1 and V2 receptors with IC50 of 1.2 μM and 14 nM, respectively.

Mozavaptan (OPC-31260) is a nonpeptide, orally effective competitive inhibitor of AVP with a V2:V1 receptor selectivity ratio of 25:1 indicating relative V2 receptor selectivity. [1] Mozavaptan (OPC-31260) inhibits AVP binding to V1 and V2 receptors in a competitive manner. [2]

Mozavaptan (OPC-31260) inhibits the antidiuretic action of exogenously administered AVP in water-loaded, alcohol-anaesthetized rats in a dose-dependent manner. OPC-31260 dose-dependently increases urine flow and decreased urine osmolality after oral administration at doses of 1 to 30 mg/kg in normal conscious rats. [2]

To determine binding kinetic constants, liver or kidney plasma membranes are incubated with increasing concentrations of [3H]-AVP with or without excess (1 μM) unlabelled AVP to obtain a saturation curve. To investigate whether mozavaptan interacts competitively or noncompetitively, the saturation binding of [3H]-AVP is examined in the absence and presence of mozavaptan at concentrations of 0.3 μM and 1 μM in liver membranes and 3 nM, and 10 nM in kidney membranes. Data on the saturation curve are plotted according to the method of Scatchard and fitted by a regression analysis[1].

137975-06-5

C27H29N3O2

427.548

OPC-31260;莫扎伐坦;OPC31260l

DMSO:10mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years