Chlormethiazole has sedative, hypnotic, anticonvulsant and neuroprotective properties. Using in vitro grease-gap recordings, we show that it inhibits epileptiform activity in neocortical slices superfused with Mg(2+)-free medium (IC(50) approximately 200 microM). At an antiepileptic concentration (300 microM), chlormethiazole potentiated the action of exogenously applied GABA (1 mM) but did not...

The aim of this study was to evaluate effects of strychnine, as well as bicuculline and picrotoxin on the anticonvulsant action of felbamate against maximal electroshock (MES)-induced seizures in mice. Strychnine (up to 0.5 mg/kg), bicuculline (up to 2 mg/kg) and picrotoxin (3 mg/kg) did not affect the seizure threshold. However, strychnine (0.25-0.5 mg/kg) and picrotoxin (3 mg/kg) impaired the...

In the recent study we have extended our investigations to the new anticonvulsant derivatives of αsubstituted N-benzylamides of γ-hydroxybutyric acid (GHB). Among the obtained compounds N-benzylamide of α-(1,2,3,4-tetrahydroisoquinoline)-GHB (9) has demonstrated activity against maximal electroshock (MES) induced seizures in mice (at 100 mg/kg ip) and in rats (at 30 mg/kg, po dose). Lactone 8 a...

A new series of 2-substituted-5-[2-(2-halobenzyloxy)phenyl]-1,3,4-oxadiazoles was designed and synthesized as anticonvulsant agents. Electroshock and pentylenetetrazole-induced lethal convulsion tests showed that the introduction of an amino group at position 2 of 1,3,4-oxadiazole ring and a fluoro substituent at ortho position of benzyloxy moiety had the best anticonvulsant activity. Our resul...

CONTEXT The herbal preparations of Annona senegalensis Pers. (Annonaceae) root bark are used in Nigerian ethnomedicine for the treatment of epilepsy and febrile seizures. The scientific evidence for this effect has been reported. OBJECTIVE The aim of this study was to identify and characterize the active constituent responsible for the anticonvulsant effect. MATERIALS AND METHODS Bioactive-...