TY - JOUR
T1 - Felbamate inhibits cloned voltage-dependent Na+ channels from human and rat brain
AU - Taglialatela, Maurizio
AU - Ongini, Ennio
AU - Brown, Arthur M.
AU - Di Renzo, Gianfranco
AU - Annunziato, Lucio
PY - 1996/12/5
Y1 - 1996/12/5
N2 - 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.
AB - 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.
KW - Anti-epileptic
KW - Felbamate
KW - Na channel
KW - Voltage-dependent
UR - http://www.scopus.com/inward/record.url?scp=0030571493&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0030571493&partnerID=8YFLogxK
U2 - 10.1016/S0014-2999(96)00802-3
DO - 10.1016/S0014-2999(96)00802-3
M3 - Article
C2 - 8982710
AN - SCOPUS:0030571493
VL - 316
SP - 373
EP - 377
JO - European Journal of Pharmacology
JF - European Journal of Pharmacology
SN - 0014-2999
IS - 2-3
ER -