Aranidipine 是一种钙通道拮抗剂,具有强效和持久的抗高血压作用。
产品描述
Aranidipine (MPC1304) is a calcium channel antagonist with potent and long-lasting antihypertensive effects.
体外活性
In myocytes, aranidipine (10 nmol/l to 1 micromol/l) concentration-dependently decreased T-type and L-type Ca(2+) currents. Aranidipine (1 micromol/l) had little effect on K(+) currents. In the sinoatrial node, 0.1 micromol/l aranidipine increased cycle length and decreased +V(max) and the slope of the phase 4 depolarization [1].
体内活性
At 1 and 6 h after oral administration of MPC-1304 (10 mg/kg) in spontaneously hypertensive rats (SHR), there was significant decrease (48%) in the number of [3H](+)-PN 200-110 binding sites (Bmax) in myocardial membranes compared to control values. The in vivo specific binding of [3H](+)-PN 200-110 in particulate fractions of aorta of SHR was significantly reduced (74.8 and 37.9%, respectively) at 1 and 6 after oral administration of MPC-1304 (3 mg/kg), while the myocardial [3H](+)-PN 200-110 binding was decreased only at 1 h later [2].
Cas No.
86780-90-7
分子式
C19H20N2O7
分子量
388.376
别名
阿雷地平;MPC1304;Aranidipine
储存和溶解度
DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years