Pharmacological profile of the new anticonvulsant etazepine.

The pharmacological profile of the new anticonvulsant etazepine (5,6-dihydro-5-methyl-11H-11-ethoxy-dibenzo[b,e]azepin-6-one) was investigated. It protected mice and rats from a wide variety of convulsant agents (maximal electroshock, pentetrazol (metrazole), bicuculline, strychnine, 3-mercaptopropionic acid, nicotine, cefazoline and kainic acid) at doses about 16-45 times lower than those exerting neurotoxic effects (depending on the test used). The anticonvulsant effect of etazepine was long-acting (more than 24 h) and did not seem to develop tolerance. Moreover, etazepine did not prolong thiopental-induced sleeping time. Based on pharmacological studies etazepine seems to exert its anticonvulsant effects by activating the GABAergic system.