Inhibition of the rat brain sodium channel Nav1.2 after prolonged exposure to gabapentin

Epilepsy Research
Yi LiuChristopher M Flores

Abstract

Prolonged exposure of neurons to gabapentin inhibits repetitive firing of Na(+)-dependent action potentials. Here, we studied the effect of such prolonged exposure to gabapentin on a rat sodium channel, Nav1.2. After 3 days of continuous incubation with gabapentin (10-1000 microM), Nav1.2 current density was decreased dose-dependently relative to untreated cells. The reduction was 57% at 30 microM gabapentin, while higher concentrations (100-1000 microM) did not result in greater effects. Prolonged treatment with gabapentin also caused the channel to inactivate at more hyperpolarized potentials. These effects provide a mechanistic basis for the inhibition of Na(+)-dependent repetitive firing upon prolonged exposure to gabapentin and may contribute to its anticonvulsant activity.

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Citations

Feb 26, 2013·Archives of Pharmacal Research·Ankesh KukkarAmteshwar Singh Jaggi
Apr 9, 2008·Pediatric Research·Beatrix S TraaAnne M Comi
Sep 15, 2010·Nihon yakurigaku zasshi. Folia pharmacologica Japonica·Yasuo OchiAkio Arakawa
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