Felbamate inhibits cloned voltage-dependent Na+ channels from human and rat brain

Maurizio Taglialatela; Ennio Ongini; Arthur M. Brown; Gianfranco Di Renzo; Lucio Annunziato

doi:10.1016/S0014-2999(96)00802-3

Felbamate inhibits cloned voltage-dependent Na+ channels from human and rat brain

Maurizio Taglialatela, Ennio Ongini, Arthur M. Brown, Gianfranco Di Renzo, Lucio Annunziato

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Abstract

The novel antiepileptic and neuroprotective drug felbamate (1 mM) caused a marked inhibition of voltage-dependent Na⁺ currents expressed in Xenopus oocytes upon injection of the cRNA encoding α-subunits from rat and human brain. This inhibition was present only if felbamate was perfused on the intracellular side of the membrane. In addition, felbamate seems to preferentially bind to and stabilize the inactivated state of the channel, resembling the action of local anesthetics. This study provides an additional mechanism by which felbamate might exert its wide-spectrum anticonvulsant and neuroprotective action.

Original language	English
Pages (from-to)	373-377
Number of pages	5
Journal	European Journal of Pharmacology
Volume	316
Issue number	2-3
DOIs	https://doi.org/10.1016/S0014-2999(96)00802-3
Publication status	Published - Dec 5 1996

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Keywords

Anti-epileptic
Felbamate
Na channel
Voltage-dependent

ASJC Scopus subject areas

Cellular and Molecular Neuroscience
Pharmacology

Cite this

Taglialatela, M., Ongini, E., Brown, A. M., Di Renzo, G., & Annunziato, L. (1996). Felbamate inhibits cloned voltage-dependent Na+ channels from human and rat brain. European Journal of Pharmacology, 316(2-3), 373-377. https://doi.org/10.1016/S0014-2999(96)00802-3

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10.1016/S0014-2999(96)00802-3