Department of Pharmacotherapeutics, School of Pharmacy, International University of Health and Welfare, Japan.
J Pharmacol Sci. 2013;123(2):203-6. doi: 10.1254/jphs.13116sc. Epub 2013 Oct 4.
Lamotrigine (LTG) is an anticonvulsant drug used in the treatment of epilepsy and bipolar disorder and it has been known that LTG targets voltage-dependent sodium channels (VGSCs). In this study, we investigated the effect of LTG on the Nav1.4 Na(+) current using HEK293 cells expressing mouse Nav1.4 VGSCs. By the treatment of LTG, Nav1.4 Na(+) current was inhibited in a dose-dependent manner. Moreover, 100 μM LTG decreased Nav1.4 Na(+) current around 40% and shifted the V1/2 of the inactivation curve to the hyperpolarization side by 20.96 mV. These findings suggest that LTG inhibits Nav1.4 Na(+) current and modifies the kinetics of the inactivated state.
拉莫三嗪（LTG）是一种抗惊厥药物，用于治疗癫痫和双相情感障碍，已知 LTG 靶向电压门控钠离子通道（VGSCs）。在这项研究中，我们使用表达小鼠 Nav1.4 VGSCs 的 HEK293 细胞研究了 LTG 对 Nav1.4 Na+电流的影响。通过 LTG 处理，Nav1.4 Na+电流呈剂量依赖性抑制。此外，100μM LTG 使 Nav1.4 Na+电流减少约 40%，并将失活曲线的 V1/2 向超极化方向移动 20.96 mV。这些发现表明 LTG 抑制 Nav1.4 Na+电流并改变失活状态的动力学。
