- 英文名称
- Aranidipine
- 分子式
- C19H20N2O7
- 分子量
- 388.37
- 中文别名
- 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; 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; 3-O-methyl 5-O-(2-oxopropyl) 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate; MPC1304
- 用途
- - 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LD
50
雄、雌小鼠，雄、雌大鼠(mg/kg)：143，193，1982，1459口服。急性毒性LD
50
雄、雌小鼠(mg/kg)：7.3，9.1腹腔注射。
- 钙拮抗剂。用于降压。
