Felbamate inhibits cloned voltage-dependent Na+ channels from human and rat brain.
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.
Taglialatela
M
M
Department of Neuroscience, School of Medicine, University of Naples Federico II, Italy. mtaglial@unina.it
Ongini
E
E
Brown
A M
AM
Di Renzo
G
G
Annunziato
L
L
D000818:Animals; D001921:Brain / Q000187:drug effects*; D000078328:Felbamate; D006801:Humans; D018696:Neuroprotective Agents / Q000494:pharmacology*; D009865:Oocytes / Q000187:drug effects; D048448:Phenylcarbamates; D011409:Propylene Glycols / Q000494:pharmacology*; D051381:Rats; D015222:Sodium Channels / Q000187:drug effects*
D018696:Neuroprotective Agents; D048448:Phenylcarbamates; D011409:Propylene Glycols; D015222:Sodium Channels; D000078328:Felbamate