Mozavaptan (OPC-31260) is a competitive vasopressin receptor antagonist for both V1 and V2 receptors with IC50 of 1.2 μM and 14 nM, respectively.

Vasopressin receptor 1:1.2 μM, V2 receptor:14 nM

Mozavaptan (OPC-31260) 是一种非肽类、口服有效的竞争性抗利尿激素(AVP)抑制剂，具有25:1的V2至V1受体选择性比率，表明其相对于V2受体的选择性。[1] Mozavaptan (OPC-31260) 竞争性抑制AVP与V1和V2受体的结合。[2]

Mozavaptan (OPC-31260) 在水负荷、醉酒麻醉的大鼠中，以剂量依赖的方式抑制了外源性AVP的抗利尿作用。在常规清醒大鼠中，经口给予1至30 mg/kg剂量的OPC-31260，能剂量依赖性地增加尿流并降低尿渗透压。[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].