Glossmann H, Ferry D R, Goll A, Striessnig J, Zernig G
Arzneimittelforschung. 1985;35(12A):1917-35.
The biochemical and biophysical features of the voltage-dependent calcium channels, as discovered in vitro by means of radiolabelled drugs, are presented. The concept of distinct but reciprocally allosterically coupled drug receptor domains linked to calcium binding sites is explained. The evidence for the existence of isochannels (and isoreceptors) is reviewed and the voltage-dependence of 1,4-dihydropyridine binding and action is discussed. The structure of the channel is investigated by radiation-inactivation and by photoaffinity labelling. Low affinity binding sites for calcium channel drugs are shown to reside on the nucleoside carrier.
本文介绍了通过放射性标记药物在体外发现的电压依赖性钙通道的生化和生物物理特性。解释了与钙结合位点相连的不同但相互变构偶联的药物受体结构域的概念。综述了同型通道（和同型受体）存在的证据，并讨论了1,4 -二氢吡啶结合和作用的电压依赖性。通过辐射灭活和光亲和标记研究了通道的结构。结果表明，钙通道药物的低亲和力结合位点位于核苷载体上。
