Literature DB >> 24096830

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

Yoshihiko Nakatani1, Haruka Masuko, Taku Amano.   

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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Year:  2013        PMID： 24096830     DOI： 10.1254/jphs.13116sc

Source DB:  PubMed          Journal:  J Pharmacol Sci        ISSN： 1347-8613            Impact factor:   3.337


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