138470-70-9
138470-70-9 結構式
基本信息
鹽酸莫扎伐普坦
莫扎伐普坦鹽酸鹽
5-(二甲基氨基)-1-[4-(2-甲基苯甲酰胺基)苯甲酰]-2,3,4,5-四氫-1H-苯并氮雜卓鹽酸鹽
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)
常見問題列表
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. |