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

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

Research output: Contribution to journalArticlepeer-review

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 languageEnglish
Pages (from-to)373-377
Number of pages5
JournalEuropean Journal of Pharmacology
Volume316
Issue number2-3
DOIs
Publication statusPublished - Dec 5 1996

Keywords

  • Anti-epileptic
  • Felbamate
  • Na channel
  • Voltage-dependent

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience
  • Pharmacology

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