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

Yoshihiko Nakatani; Haruka Masuko; Taku Amano

Journal of Pharmacological Sciences (Jan 2013)

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

Yoshihiko Nakatani,
Haruka Masuko,
Taku Amano

Affiliations

Yoshihiko Nakatani: Department of Pharmacotherapeutics, School of Pharmacy, International University of Health and Welfare, 2600-1 Kitakanemaru, Ohtawara, Tochigi 324-8501, Japan
Haruka Masuko: Department of Pharmacotherapeutics, School of Pharmacy, International University of Health and Welfare, 2600-1 Kitakanemaru, Ohtawara, Tochigi 324-8501, Japan
Taku Amano: Department of Pharmacotherapeutics, School of Pharmacy, International University of Health and Welfare, 2600-1 Kitakanemaru, Ohtawara, Tochigi 324-8501, Japan; Corresponding author. [email protected]

Journal volume & issue: Vol. 123, no. 2
pp. 203 – 206

Abstract

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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

Published in Journal of Pharmacological Sciences

ISSN: 1347-8613 (Print)
Publisher: Elsevier
Country of publisher: Japan
LCC subjects: Medicine: Therapeutics. Pharmacology
Website: http://www.journals.elsevier.com/journal-of-pharmacological-sciences

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