Effect of lamotrigine on Na(v)1.4 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...

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Bibliographic Details
Published in:Journal of pharmacological sciences 2013-10, Vol.123 (2), p.203
Main Authors: Nakatani, Yoshihiko, Masuko, Haruka, Amano, Taku
Format: Article
Language:English
Subjects:
Animals
Anticonvulsants - pharmacology
Dose-Response Relationship, Drug
HEK293 Cells
Humans
Lamotrigine
Membrane Potentials - drug effects
Mice
Patch-Clamp Techniques
Triazines - pharmacology
Voltage-Gated Sodium Channel Blockers - pharmacology
Voltage-Gated Sodium Channels - drug effects
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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.
ISSN:1347-8648
DOI:10.1254/jphs.13116sc