莫扎伐普坦盐酸盐

生物活性靶点体外研究体内研究莫扎伐普坦盐酸盐试剂级价格

莫扎伐普坦盐酸盐

CAS号:138470-70-9
英文名:Mozavaptan Hydrochloride
中文名:莫扎伐普坦盐酸盐
CBNumber:CB11508553
分子式:C27H29N3O2.ClH
分子量:464.006
MOL File:138470-70-9.mol

莫扎伐普坦盐酸盐化学性质

储存条件 :2-8°C
溶解度 :DMSO: ≥15mg/mL
形态 :powder
颜色 :white to tan

安全信息

危险品标志 :Xn
危险类别码 :22
WGK Germany :3

莫扎伐普坦盐酸盐性质、用途与生产工艺

生物活性 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。
靶点

IC50: 14 nM (Vasopressin V ₂ receptor); 1.2 μM (Vasopressin V ₁ receptor)
体外研究

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).

体内研究

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.

Animal Model:	Hydrated conscious rats (300-350 g)
Dosage:	1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg
Administration:	Oral administration
Result:	Dose-dependently increased urine flow and decreased urine osmolality.