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

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

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 V...

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Bibliographic Details
Main Authors: Yoshihiko Nakatani, Haruka Masuko, Taku Amano
Format: Article
Language:English
Published: Elsevier 2013-01-01
Series:Journal of Pharmacological Sciences
Online Access:http://www.sciencedirect.com/science/article/pii/S1347861319302725
Description
Summary: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. Keywords:: lamotrigine, Nav1.4, voltage-clamp
ISSN:1347-8613

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