Calcium antagonists: mechanisms and therapeutic uses
Calcium antagonists: mechanisms and therapeutic uses
复制标题
钙拮抗剂：机制和治疗用途
DOI：
10.1016/0165-6147(84)90446-2
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发表时间：
1984
影响因子：
13.8
通讯作者：
A. Fleckenstein
中科院分区：
文献类型：
--
作者：
G. Fleckenstein;M. Frey;A. Fleckenstein
Nearly 20 years have passed since the appearance of the filSt report from our laboratory on a new compound (lsoptin, iproveratril, generic name: verapamil) which mimicked the cardiac effects of simple Ca withdrawalS-2: verapamil diminished Ca-dependent contractile force without a major change in the Nadependent action potential parameters. It also reduced Ca-dependent high energy phosphate utilization of the beating heart, and consequently lowered oxygen consumption in parallel with the depression of contractile activity" a'4. These inhibitory effects of verapamil could promptly be neutralized by additional Ca, 13-adrenergic catecholamines, or cardiac glycosides, ie by measures able to restore the Ca supply to the contractile system. Thus, verapamil represented the most interesting prototype of the new family of'Ca-antagonistic'substances. In fact, Ca-antagonism turned out to be a novel pharmacodynamic principle clearly distinguishable from [~-reeeptor blockade. These drugs should be subdivided into groups A and B, according to criteria unrelated to their chemical constitution, but corresponding to the strength and specificity of their Ca-antagonistic activities. According to this classification, group A comprises the most potent and specific Ca-antagonists such as nifedipine, niludipine, nimodipine, ryosidine, verapamil, gallopamil and diltiazem. These substances are capable of inhibiting Ca-dependent excitation-contraction coupling of the mammalian ventricular myocardium by at least 90% without affecting the fast Na influx associated with the rising phase of the action potential,
