中文名 | ARANIDIPINE |
英文名 | ARANIDIPINE |
别名 | 阿雷地平 2,6-二甲基-4-(2-硝基苯基)-1,4-二氢-3,5-吡啶二羧酸甲基2-氧丙基酯 2,6-二甲基-4-(2-硝基苯基)-1,4-二氢-3,5-吡啶二羧酸 3-甲基 2-氧代丙基酯 3-甲基 5-(2-氧丙基)2,6-二甲基-4-(2-硝基苯基)-1,4-二氢吡啶-3,5-二羧酸 |
英文别名 | MPC-1304 Sapresta ARANIDIPINE Asanidipine 3-Methyl 5-(2-oxopropyl) 2,6-diMethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate 1,4-Dihydro-2,6-dimethyl-4-(2-nitrophenyl)-3,5-pyridinedicarboxylic acid 3-methyl 5-(2-oxopropyl) ester 3,5-Pyridinedicarboxylicacid, 1,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)-, 3-methyl 5-(2-oxopropyl)ester |
CAS | 86780-90-7 |
化学式 | C19H20N2O7 |
分子量 | 388.37 |
密度 | 1.284±0.06 g/cm3(Predicted) |
熔点 | 155° |
沸点 | 530.0±50.0 °C(Predicted) |
酸度系数 | 2.56±0.70(Predicted) |
存储条件 | 2-8°C |
物化性质 | 从乙酸乙酯-己烷得黄色棱状结晶,熔点155℃。急性毒性LD50雄、雌小鼠,雄、雌大鼠(mg/kg):143,193,1982,1459口服。急性毒性LD50雄、雌小鼠(mg/kg):7.3,9.1腹腔注射。 |
体内研究 | Aranidipine (MPC-1304) is a new Ca 2+ channel antagonist in spontaneously hypertensive rats. Following oral administration of Aranidipine at doses of 3 and 10 mg/kg to spontaneously hypertensive rats (SHR), there are significant decreases in B max values for specific [ 3 H](+)-PN 200-110 binding to myocardial membranes compared to the control values. The B max values at 1 h (3 mg/kg), 1 and 6 h (10 mg/kg) are significantly decreased (47.7, 48.9 and 25.8%, respectively) compared to the control values. The effect is greatest at 1 h and decreases with time. The B max values at 6 h (3 mg/kg) and 12 or 24 h (10 mg/kg) after the oral administration of Aranidipine are not significantly different from the control values, suggesting the disappearance of the effect of Aranidipine. The K d values for myocardial [ 3 H](+)-PN 200-110 binding are unaltered by oral administration of Aranidipine. |
上游原料 | 反式丁烯酸 氨 氢化钠 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.575 ml | 12.874 ml | 25.749 ml |
5 mM | 0.515 ml | 2.575 ml | 5.15 ml |
10 mM | 0.257 ml | 1.287 ml | 2.575 ml |
5 mM | 0.051 ml | 0.257 ml | 0.515 ml |
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