Differential effects of remacemide and desglycinyl-remacemide on epileptiform burst firing in the rat hippocampal slice.

Abstract:

:Remacemide is a potential anticonvulsant drug with an active metabolite, desglycinyl-remacemide (DGR). Both moieties have been reported to block neuronal Na(+) channels and the N-methyl-D-aspartate (NMDA) subtype of glutamate receptor. The effects of remacemide and DGR on zero Mg(2+)/4-aminopyridine-induced epileptiform discharges were investigated in the rat hippocampal slice preparation and compared with carbamazepine (CBZ), a prototypic Na(+) channel blocker, and AR-R15896AR, a putative NMDA channel blocker. Remacemide (0-100 microM) was without significant effect, while DGR, CBZ and AR-R15896AR all decreased burst frequency in a concentration (0-100 microM) dependent manner. These findings suggest that remacemide is not sufficiently potent at the Na(+) channel or NMDA receptor to attenuate epileptiform activity in this model and that the anticonvulsant effects of the drug may be mediated by DGR.

journal_name

Neurosci Lett

journal_title

Neuroscience letters

authors

Santangeli S,Sills GJ,Stone TW,Brodie MJ

doi

10.1016/s0304-3940(01)02511-3

keywords:

subject

Has Abstract

pub_date

2002-03-15 00:00:00

pages

33-6

issue

1-2

eissn

0304-3940

issn

1872-7972

pii

S0304394001025113

journal_volume

321

pub_type

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