二氢吡啶衍生物可延长培养心肌细胞中钙通道的开放状态。
Dihydropyridine derivatives prolong the open state of Ca channels in cultured cardiac cells.
作者信息
Kokubun S, Reuter H
出版信息
Proc Natl Acad Sci U S A. 1984 Aug;81(15):4824-7. doi: 10.1073/pnas.81.15.4824.
Abstract
The dihydropyridine derivatives CGP 28392 and BAY K 8644 exert a strong positive inotropic effect in mammalian cardiac muscle, presumably by increasing Ca influx during the action potential. Analysis of the drug effects at the level of single Ca channels by means of the patch-clamp method revealed complicated changes in the kinetics of channel gating. The prevailing effect is a prolongation of the mean open time of Ca channels. In addition, the intervals between channel openings can be slightly prolonged. Ensemble averages of single-channel traces showed a concentration-dependent increase in the mean current amplitude by the drugs. In contrast to beta-adrenoceptor agonists, the increase in Ca current by the dihydropyridine derivatives is not associated with an increase in the intracellular cyclic AMP level.
摘要
二氢吡啶衍生物CGP 28392和BAY K 8644在哺乳动物心肌中发挥强烈的正性肌力作用，推测是通过增加动作电位期间的钙内流来实现的。运用膜片钳技术在单个钙通道水平分析药物效应，结果显示通道门控动力学发生了复杂变化。主要效应是钙通道平均开放时间延长。此外，通道开放之间的间隔也可稍有延长。单通道记录的总体平均值显示，这些药物可使平均电流幅度呈浓度依赖性增加。与β-肾上腺素能受体激动剂不同，二氢吡啶衍生物引起的钙电流增加与细胞内环磷酸腺苷水平升高无关。
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