The Effect of Lamotrigine on Nav1.4 Voltage-Gated Sodium Channels

Journal of Pharmacological Sciences

Taku Amano¹  Yoshihiko Nakatani¹  Haruka Masuko¹ 

[1] Department of Pharmacotherapeutics, School of Pharmacy, International University of Health and Welfare, Japan

关键词: lamotrigine;    Nav1.4;    voltage-clamp;   

DOI  :  10.1254/jphs.13116SC

学科分类：药学

来源: Nihon Yakuri Gakkai Henshuubu / Japanese Pharmacological Society

【 摘 要 】

References(14)Cited-By(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.

【 授权许可】

Unknown