Beeler G W
Fed Proc. 1977 Aug;36(9):2209-13.
This paper briefly reviews the current state of understanding of cardiac excitation--contraction coupling and its relation to glycoside action. Evidence that inotropic action of glycosides might result from increased influx of Ca2+ during action potential is reviewed. Recent voltage clamp studies that show little if any direct effect on Ca2+ influx during the action potential are cited. It is suggested that the primary inotropic effects derive from altered ionic exchange mechanisms secondary to inhibition of Na+,K+-ATPase. The role of ionic currents in glycoside toxicity is considered, with discussion of a dynamic, depolarizing current that appears shortly after action potential. This current is apparently an inward movement of positive ions that is strongly mediated by extracellular Ca2+ levels. It is noted that such spontaneous depolarizations of the membrane have been observed in several other circumstances where strong positive inotropism has been induced. The conclusion is reached that membrane ionic currents probably play only a secondary role in glycoside inotropism and in many of the toxic effects.
本文简要回顾了目前对心脏兴奋 - 收缩偶联及其与糖苷作用关系的理解现状。综述了关于糖苷的正性肌力作用可能源于动作电位期间Ca2+内流增加的证据。引用了近期的电压钳研究,这些研究表明在动作电位期间对Ca2+内流几乎没有直接影响。有人提出,主要的正性肌力作用源于继发于Na+,K+-ATP酶抑制的离子交换机制改变。文中考虑了离子电流在糖苷毒性中的作用,并讨论了动作电位后不久出现的一种动态去极化电流。这种电流显然是由细胞外Ca2+水平强烈介导的正离子向内移动。值得注意的是,在其他几种诱导出强正性肌力作用的情况下也观察到了这种膜的自发去极化。得出的结论是,膜离子电流在糖苷正性肌力作用和许多毒性作用中可能仅起次要作用。