Rakotoarisoa L, Leprêtre N, Mironneau J, Galiano A, Mironneau C
Laboratoire de Physiologie Cellulaire et Pharmacologie Moléculaire, URA CNRS 1489, Université de Bordeaux II, France.
Fundam Clin Pharmacol. 1994;8(6):546-52. doi: 10.1111/j.1472-8206.1994.tb00836.x.
We studied the effects of six dihydropyridines on the specific binding of (+)-[3H]-isradipine to vascular (portal vein) and cardiac isolated membranes to achieve the relative cardiovascular selectivity of these compounds. Elgodipine, (+)-oxodipine and nifedipine had a significantly higher affinity for the vascular L-type calcium channel than for the cardiac calcium channel while nicardipine showed opposite properties. The other dihydropyridines (nitrendipine and (+)-isradipine) had similar affinities for the cardiac and vascular calcium channels. As the membrane potential of isolated membranes is about 0 mV, these results suggest that the differences in binding of these dihydropyridines to L-type calcium channels in vascular and cardiac cells may be attributed to differences in the molecular structure of these calcium channels.
我们研究了六种二氢吡啶对(+)-[3H]-伊拉地平与血管（门静脉）和心脏分离膜特异性结合的影响，以实现这些化合物的相对心血管选择性。依福地平、(+)-氧代地平硝苯地平对血管L型钙通道的亲和力显著高于对心脏钙通道的亲和力，而尼卡地平则表现出相反的特性。其他二氢吡啶（尼群地平和(+)-伊拉地平）对心脏和血管钙通道具有相似的亲和力。由于分离膜的膜电位约为0 mV，这些结果表明，这些二氢吡啶与血管和心脏细胞中L型钙通道结合的差异可能归因于这些钙通道分子结构的差异。
