Evaluation of anticonvulsant activity of novel pyrrolidin-2-one derivatives.

Abstract

BACKGROUND: The aim of this study was to examine the anticonvulsant activity of some novel pyrrolidin-2-one derivatives with considerable affinity to serotonin 5-HT1A and α1-adrenergic receptors. METHODS: The maximal electroshock-induced seizure (MES) and pentetrazole (PTZ)-induced seizure models in mice were performed. RESULTS: As a results of the conducted studies, three compounds showing anticonvulsant activity were selected. The EP-40 molecule significantly reduced incidence of seizures in the maximal electroshock test. The EP-42 and EP-46 compounds demonstrated activity in the pentetrazole-induced seizures. CONCLUSION: The results may indicate that the decrease in the susceptibility to seizures induced by the new pyrrolidin-2-one derivatives is related to the significant affinity to serotonergic or α1-adrenergic receptors. Also putative mechanism of action of the test compounds can be linked with their GABA-ergic activity, because these novel derivatives are GABA analogs.