Effect of lamotrigine on Na(v)1.4 voltage-gated sodium channels.

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.

journal_name

J Pharmacol Sci

authors

Nakatani Y,Masuko H,Amano T

doi

10.1254/jphs.13116sc

subject

Has Abstract

pub_date

2013-01-01 00:00:00

pages

203-6

issue

2

eissn

1347-8613

issn

1347-8648

pii

DN/JST.JSTAGE/jphs/13116SC

journal_volume

123

pub_type

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