Kass R S
Department of Physiology, University of Rochester, NY 14642.
Circ Res. 1987 Oct;61(4 Pt 2):I1-5.
This study investigated the voltage-dependent actions of the stereoisomers of the 1,4-dihydropyridine Bay K 8644 on calcium channel currents in heart cells. Whole-cell currents were recorded from enzymatically dispersed ventricular myocytes using the patch-clamp technique. Both enantiomers of this compound modulate calcium channel current in a voltage-dependent manner. The most prominent effect of (+)-Bay K 8644 is an inhibition of calcium channel current, which is more pronounced when currents are measured from depolarized holding potentials. (-)-Bay K 8644 resembles the racemic compound; it enhances or inhibits currents depending on holding potential. The results of this study suggest that the dual activity of the racemic compound is not because of opposing actions of its component enantiomers.
本研究调查了1,4 - 二氢吡啶类化合物Bay K 8644的立体异构体对心脏细胞钙通道电流的电压依赖性作用。采用膜片钳技术记录酶解分散的心室肌细胞的全细胞电流。该化合物的两种对映体均以电压依赖性方式调节钙通道电流。(+)-Bay K 8644最显著的作用是抑制钙通道电流,当从去极化的钳制电位测量电流时,这种抑制作用更为明显。(-)-Bay K 8644与外消旋化合物相似;它根据钳制电位增强或抑制电流。本研究结果表明,外消旋化合物的双重活性并非因其组成对映体的相反作用所致。