阿雷地平

概述生物活性靶点体内研究阿雷地平试剂级价格

阿雷地平

CAS号:86780-90-7
英文名:ARANIDIPINE
中文名:阿雷地平
CBNumber:CB4386708
分子式:C19H20N2O7
分子量:388.37
MOL File:86780-90-7.mol

阿雷地平化学性质

熔点 :155°
沸点 :530.0±50.0 °C(Predicted)
密度 :1.284±0.06 g/cm3(Predicted)
储存条件 :2-8°C
溶解度 :DMSO : 125 mg/mL (321.86 mM)
酸度系数(pKa) :2.56±0.70(Predicted)

安全信息

毒性 :LD50 in male, female mice, rats (mg/kg): 143, 193, 1982, 1459 orally; LD50 in male, female mice (mg/kg): 7.3, 9.1 i.p. (Nakano)

阿雷地平性质、用途与生产工艺

概述阿雷地平(aranidipine)是日本Maruko Seiyaku公司研发的强效、长效钙拮抗剂，临床对原发性高血压有较好的疗效，能降低外周血管阻力，增强射血功能。此外，阿雷地平还能降低脑卒中、心脏纤维化、增生性纤维样小动脉炎以及恶性肾硬化的发生率。
生物活性 Aranidipine (MPC1304) 是一种钙离子 (Ca2+) 通道拮抗剂，具有强大而持久的抗高血压作用。
靶点

Ca ²⁺ Channel
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.
化学性质从乙酸乙酯-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。
用途钙拮抗剂。用于降压。
生产方法化合物(I)和3-氨基丁烯酸[2，2-(亚乙基二氧基)丙基]酯在乙醇中回流，缩合环合得到化合物(Ⅱ)，再酸性水解得到产物。