莫扎伐普坦盐酸盐
| 中文名称 | 莫扎伐普坦盐酸盐 |
|---|---|
| 中文同义词 | 莫扎伐普坦盐酸盐;5-(二甲基氨基)-1-[4-(2-甲基苯甲酰胺基)苯甲酰]-2,3,4,5-四氢-1H-苯并氮杂卓盐酸盐;盐酸莫扎伐普坦;溴十四烷酸乙酯;化合物 T21465 |
| 英文名称 | Mozavaptan Hydrochloride |
| 英文同义词 | N-[4-[[5-(Dimethylamino)-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl]carbonyl]phenyl]-2-methylbenzamide hydrochloride;5-(Dimethylamino)-1-[4-(2-methylbenzamido)benzoyl]-2,3,4,5-tetrahydro-1H-benzazepine hydrochloride;N-[4-(5-Dimethylamino-2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl)phenyl]-2-methylbenzamide hydrochloride;OPC 31260 hydrochloride;Mozavaptan HCl;MOROBKPIULFQDC-UHFFFAOYSA-N;OPC 31260 hydrochloride >=98% (HPLC);Benzamide,N-[4-[[5-(dimethylamino)-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl]carbonyl]phenyl]-2-methyl-,hydrochloride (1:1) |
| CAS号 | 138470-70-9 |
| 分子式 | C27H29N3O2.ClH |
| 分子量 | 464.006 |
| EINECS号 | |
| 相关类别 | 医药中间体;原料药 |
| Mol文件 | 138470-70-9.mol |
| 结构式 |  |
莫扎伐普坦盐酸盐 性质
| 储存条件 | 2-8°C |
|---|---|
| 溶解度 | 在DMSO中的溶解度≥15mg/mL |
| 形态 | 粉末 |
| 颜色 | 白色至棕褐色 |
IC50: 14 nM (Vasopressin V 2 receptor); 1.2 μM (Vasopressin V 1 receptor)
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).
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. |
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-123593 | Mozavaptan hydrochloride | 5 mg | 350元 | |
| 2024/04/30 | HY-123593 | 莫扎伐普坦盐酸盐 Mozavaptan hydrochloride | 138470-70-9 | 10mM * 1mLin DMSO | 360元 |