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Mozavaptan hydrochloride

CAS No. : 138470-70-9

MCE 站：Mozavaptan hydrochloride

产品活性：Mozavaptan hydrochloride (OPC-31260 hydrochloride) 是一种 benzazepine 衍生物，也是一种有效，选择性，竞争性和口服活性的加压素 V₂ 受体拮抗剂，IC₅₀ 为 14 nM。Mozavaptan hydrochloride 对 V₂ 受体的选择性比 V₁ 受体 (IC₅₀ 为 1.2 μM) 高约 85 倍，并且可以在体内拮抗精氨酸加压素的抗利尿作用。Mozavaptan hydrochloride 可用于低钠血症，抗利尿激素不适当综合征 (SIADH) 和充血性心力衰竭的研究。

研究领域：GPCR/G Protein

作用靶点：Vasopressin Receptor

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. K_d value for [3H]-AVP in rat liver is 1.1 nM; in rat kidney is 1.38 nM. The K_d of [3H]-AVP is reduced significantly in both rat liver and kidney in the presence of Mozavaptan (K_d of 2.47 nM and 5.51 nM for V1 receptor at the doses of 0.3 μM and 1 μM.respectively; K_d 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.

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