Oyama Y, Sadoshima J, Tokutomi N, Akaike N
Department of Physiology, Faculty of Medicine, Kyushu University, Fukuoka, Japan.
Brain Res. 1988 Mar 1;442(2):223-8. doi: 10.1016/0006-8993(88)91507-7.
The action of lidocaine on the Ca2+ current (ICa) was studied on single isolated neurons of frog dorsal root ganglia using a 'concentration-clamp' technique which combines intracellular perfusion with a rapid external solution change. Lidocaine decreased the peak amplitude of ICa at a threshold concentration of 10 microM. Higher concentrations gave a dose-dependent increase in inhibition of ICa. Lidocaine also depressed the Na+ current (INa) at a threshold concentration 10 times lower than that for decreasing the amplitude of ICa of neurons isolated from same ganglia. The rate of inhibitory action on ICa was slowed at more negative holding potentials (VH). Lidocaine appears to block both closed and open Ca2+ channels, but acts more profoundly on open channels.
利用一种“浓度钳”技术,将细胞内灌注与细胞外溶液快速更换相结合,在青蛙背根神经节的单个分离神经元上研究了利多卡因对钙离子电流(ICa)的作用。利多卡因在阈值浓度为10微摩尔时降低了ICa的峰值幅度。更高的浓度使对ICa的抑制呈剂量依赖性增加。利多卡因还在比降低同一神经节分离出的神经元ICa幅度的阈值浓度低10倍的浓度下抑制钠离子电流(INa)。在更负的钳制电位(VH)下,对ICa的抑制作用速率减慢。利多卡因似乎能阻断关闭和开放的钙离子通道,但对开放通道的作用更显著。