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

      , , , ,

      European Journal of Pharmacology

      Elsevier BV

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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 alpha-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.

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          Author and article information

          Journal
          European Journal of Pharmacology
          European Journal of Pharmacology
          Elsevier BV
          00142999
          December 1996
          December 1996
          : 316
          : 2-3
          : 373-377
          Article
          10.1016/S0014-2999(96)00802-3
          8982710
          © 1996

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