Felbamate, a novel antiepileptic drug, reverses increases in intracellular Ca2+ concentration

Electrophysiological actions of felbamate on rat striatal neurones

“…Calibrations (McCabe et al, 1993;Rho et al, 1994;Domenici et al, 1994), to our knowledge this study represents the first investigation of the electrophysiological actions of FBM on an identified glutamatergic pathway in the mammalian brain. It is worth noting that both limitation of firing activity of striatal neurones and modulation of corticostriatal synaptic potentials occurred at concentrations very similar to those achieved either in the brain and plasma of FBM-treated animals and in plasma of human subjects during clinical trials (McCabe et al, 1993;Wagner et al, 1990), or in surgical samples from patients receiving therapeutic dosages of this drug (Adusumalli et al, 1994;Taylor et al, 1995).…”

NMDA Receptor Antagonist Felbamate Reduces Behavioral Deficits and Blood–Brain Barrier Permeability Changes after Experimental Subarachnoid Hemorrhage in the Rat

“…FBM is a novel anti-epileptic drug with a broad anticonvulsivant profile (Arcadi et al, 1997;McCabe et al, 1993;Reckilin et al, 2003;Sbuaib et al, 1996;Soderpalm et al, 2002;Swiader et al, 2003;Wallis et al, 1992;Wasterlain et al, 1992;Taylor et al, 1995). The dosage of FBM as an anticonvulsant is 1200 mg/day for adults and 15 mg/kg/day for pediatric patients.…”

“…FBM administration reduced delayed hippocampal neuronal death induced by transient cerebral ischemia in the Mongolian gerbil (Wasterlain et al, 1992). Several mechanisms of action for FBM have been identified, including inhibition of voltage-sensitive sodium and calcium channels, potentiation of ␥-amino-butyric acid (GABA)-mediated chloride currents, and interaction with the NMDA receptor complex through inhibition of the strychnine-insensitive glycine binding site (McCabe et al, 1993;Świader et al, 2003;Taylor et al, 1995). Specifically, FBM reduces excitatory glutamatergic neurotransmission and intracellular calcium concentrations (Soderpalm, 2002).…”

Anticonvulsant effect of felbamate in the pentylenetetrazole kindling model of epilepsy in the rat

“…The interaction of felbamate with this site may mediate its inhibitory effect on NMDA receptor channel openings. In keeping with these findings, it has been reported that felbamate antagonizes the stimulatory effect of glyeine on NMDA-induced Ca 2 + transients in cerebellar granule cells (Taylor et al 1995). Further, this effect can be detected at concentrations (300 gM) that are in the range of those achieved in the rat brain following the administration of anticonvulsant doses of felbamate (Adusumalli et al 1993).…”

“…Thus, there is growing evidence that felbamate may have an inhibitory effect on NMDA receptor-mediated neurotransmission, although the molecular mechanisms involved have not yet been clearly defined (Coffin et al 1994;De Sarro et al 1994;Rho et al 1994;Subramaniam et al 1995;Taylor et al 1995). In addition, felbamate appears to have blocking effects on voltage-gated Na + channels and Ca 2+ conductances in the mammalian brain (White et al 1992;Libri and Constanti 1994).…”