Cellular action of calcium channel blocking drugs.
Cellular action of calcium channel blocking drugs.
复制标题
钙通道阻断药物的细胞作用。
DOI：
10.1146/annurev.me.35.020184.001545
复制
发表时间：
1984
影响因子：
10.5
通讯作者：
Triggle,DJ
中科院分区：
文献类型：
--
作者：
Schwartz,A;Triggle,DJ
钙拮抗剂是一个令人兴奋的“类”药物，已经在冠状动脉疾病的治疗中产生了重要影响。在美国，维拉帕米、硝苯地平和地尔硫卓这三种药物都是有效的冠状动脉扩张剂。此外，维拉帕米和地尔硫卓对某些室上性异常有抗心律失常作用。由于钙拮抗剂扩张外周阻力血管，它们也可用于高血压。也有报道称，它们可能对偏头痛有效，可能是因为它们在脑血管中的”解痉挛”活性。由于钙最终参与所有需要电刺激或化学刺激的过程，因此，其主要作用似乎是抑制钙穿过或穿过细胞膜的药物应该表现出广谱的治疗活性，这并不奇怪。二氢吡啶衍生物与膜制剂的立体特异性结合，以及这些和其他钙拮抗剂对结合过程的影响，应该产生关于钙拮抗剂作用机制的重要信息。
The calcium antagonists are an exciting" class" of drugs that are already making an important impact in the treatment of coronary artery disease. All three drugs in use in the US, verapamil, nifedipine, and diltiazem, are effective coronary vasodilators. In addition, verapamil and diltiazem have antiarrhythmic activity against certain supraventricular abnormalities. Since the calcium antagonists dilate peripheral resistance vessels, they may also be useful in hypertension. There are reports also that they may be effective in migraine headache, probably because of their" antispastic" activity in cerebral vessels. Since calcium is ultimately involved in all processes that require stimulation, either electrical or chemical, it is not surprising that drugs whose primary effect appears to be an inhibition of the entry of calcium across or through cell membranes should exhibit a wide spectrum of therapeutic activity. The stereospecific binding of dihydropyridine derivatives to membrane preparations, and the effects of those and other calcium antagonists on the binding process, should yield important information on the mechanisms of calcium antagonist action.