Romey G, Garcia L, Rieger F, Lazdunski M
Centre de Biochimie du Centre National de la Recherche Scientifique, Nice, France.
Biochem Biophys Res Commun. 1988 Nov 15;156(3):1324-32. doi: 10.1016/s0006-291x(88)80777-0.
The L-type Ca2+ channel is blocked by 1,4-dihydropyridines (DHP), by phenylalkylamines, by diphenylbutylpiperidines or by benzolactams. We first show with mouse muscle cells in culture that all these L-type Ca2+ channel blockers block contraction. However, voltage-clamp analysis associated to contraction measurements also clearly show that Ca2+ influx through L-type Ca2+ channels is not required for contraction. Therefore, there is a need for a voltage-sensor which would be responsible for the excitation-contraction (E-C) coupling. We are showing here that the voltage-sensor involved in E-C coupling and the L-type Ca2+ channel have a similar pharmacology. Some of the blockers used are more active on the voltage sensor, others on the L-type Ca2+ channel.
L型钙通道可被1,4-二氢吡啶（DHP）、苯烷基胺、二苯基丁基哌啶或苯并内酰胺阻断。我们首先在培养的小鼠肌肉细胞中证明，所有这些L型钙通道阻滞剂均可阻断收缩。然而，与收缩测量相关的电压钳分析也清楚地表明，通过L型钙通道的钙内流并非收缩所必需。因此，需要一种负责兴奋-收缩（E-C）偶联的电压传感器。我们在此表明，参与E-C偶联的电压传感器与L型钙通道具有相似的药理学特性。所使用的一些阻滞剂对电压传感器的活性更高，另一些则对L型钙通道的活性更高。
