阿雷地平

中文名称:

阿雷地平

中文同义词:

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;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 3-甲基 2-氧代丙基酯

英文名称:

ARANIDIPINE

英文同义词:

ARANIDIPINE;2，6-Dimethyl-4-(2-nitrophenyl)-1，4-dihydro-3，5-pyridinedicarboxylic acid methyl 2-oxopropyl ester;MPC-1304;Sapresta;1,4-Dihydro-2,6-dimethyl-4-(2-nitrophenyl)-3,5-pyridinedicarboxylic acid 3-methyl 5-(2-oxopropyl) ester;Asanidipine;3,5-Pyridinedicarboxylicacid, 1,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)-, 3-methyl 5-(2-oxopropyl)ester;3-Methyl 5-(2-oxopropyl) 2,6-diMethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate

CAS号:

86780-90-7

分子式:

C19H20N2O7

分子量:

388.37

EINECS号:

相关类别:

抗心绞痛药;心脑血管药物;药物;对照品

Mol文件:

86780-90-7.mol

熔点 

155°

沸点 

530.0±50.0 °C(Predicted)

密度 

1.284±0.06 g/cm3(Predicted)

储存条件 

Sealed in dry,2-8°C

酸度系数(pKa)

2.56±0.70(Predicted)

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。

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)