莫扎伐普坦盐酸盐
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- CAS号:
- 138470-70-9
- 英文名:
- Mozavaptan Hydrochloride
- 英文别名:
- Mozavaptan HCl;OPC 31260 hydrochloride;Mozavaptan Hydrochloride;MOROBKPIULFQDC-UHFFFAOYSA-N;OPC 31260 hydrochloride >=98% (HPLC);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;N-[4-[[5-(Dimethylamino)-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl]carbonyl]phenyl]-2-methylbenzamide hydrochloride;Benzamide,N-[4-[[5-(dimethylamino)-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl]carbonyl]phenyl]-2-methyl-,hydrochloride (1:1)
- 中文名:
- 莫扎伐普坦盐酸盐
- 中文别名:
- 溴十四烷酸乙酯;盐酸莫扎伐普坦;莫扎伐普坦盐酸盐;化合物 T21465;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
- CBNumber:
- CB11508553
- 分子式:
- C27H29N3O2.ClH
- 分子量:
- 464.006
- MOL File:
- 138470-70-9.mol
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莫扎伐普坦盐酸盐化学性质
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储存条件:
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2-8°C
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溶解度:
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DMSO: ≥15mg/mL
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形态:
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powder
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颜色:
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white to tan
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莫扎伐普坦盐酸盐性质、用途与生产工艺
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。
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.
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Animal Model:
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Hydrated conscious rats (300-350 g)
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Dosage:
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1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg
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Administration:
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Oral administration
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Result:
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Dose-dependently increased urine flow and decreased urine osmolality.
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莫扎伐普坦盐酸盐
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下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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| 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 |
138470-70-9, 莫扎伐普坦盐酸盐 相关搜索:
- 原料药
- 医药中间体
- C27H29N3O2HCl
- 化合物 T21465
- 溴十四烷酸乙酯
- 盐酸莫扎伐普坦
- 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
- 莫扎伐普坦盐酸盐
- 138470-70-9
- Mozavaptan Hydrochloride
- Benzamide,N-[4-[[5-(dimethylamino)-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl]carbonyl]phenyl]-2-methyl-,hydrochloride (1:1)
- OPC 31260 hydrochloride >=98% (HPLC)
- MOROBKPIULFQDC-UHFFFAOYSA-N
- Mozavaptan HCl
- OPC 31260 hydrochloride
- N-[4-(5-Dimethylamino-2,3,4,5-tetrahydro-1-benzazepine-1-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-1H-1-benzazepin-1-yl]carbonyl]phenyl]-2-methylbenzamide hydrochloride