Ishibashi A, Horii D
Jpn J Pharmacol. 1987 Feb;43(2):234-6. doi: 10.1254/jjp.43.234.
Calcium antagonistic activity of MCI-176, a new calcium antagonist, was compared with those of diltiazem and nifedipine in isolated depolarized porcine coronary arteries. MCI-176, diltiazem and nifedipine competitively inhibited calcium contraction of the large coronary arteries, and their pA2 values were 7.49, 6.89 and 9.55, respectively. Similar competitive inhibition by MCI-176, diltiazem and nifedipine of calcium contraction was also observed in the small coronary arteries, and their pA2 values were 7.38, 6.83 and 9.91, respectively. Although calcium antagonistic activity of nifedipine was several hundreds times more potent than MCI-176 and diltiazem, the action of nifedipine, unlike MCI-176 and diltiazem, favored the small coronary arteries rather than the large coronary arteries.
新型钙拮抗剂MCI - 176的钙拮抗活性在离体去极化猪冠状动脉中与地尔硫䓬和硝苯地平进行了比较。MCI - 176、地尔硫䓬和硝苯地平竞争性抑制大冠状动脉的钙收缩,其pA2值分别为7.49、6.89和9.55。在小冠状动脉中也观察到MCI - 176、地尔硫䓬和硝苯地平对钙收缩有类似的竞争性抑制作用,其pA2值分别为7.38、6.83和9.91。尽管硝苯地平的钙拮抗活性比MCI - 176和地尔硫䓬强数百倍,但与MCI - 176和地尔硫䓬不同,硝苯地平的作用更倾向于小冠状动脉而非大冠状动脉。