Journal of Pharmacological Sciences
Online ISSN : 1347-8648
Print ISSN : 1347-8613
ISSN-L : 1347-8613
The Effect of Lamotrigine on Nav1.4 Voltage-Gated Sodium Channels
Yoshihiko NakataniHaruka MasukoTaku Amano
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JOURNALS FREE ACCESS Advance online publication

Article ID: 13116SC

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Abstract

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.

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© 2013 The Japanese Pharmacological Society
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