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.
Borsini
F
F
A. Menarini Pharmaceuticals Research Division, Firenze, Italy.
Volterra
G
G
Cutrufo
C
C
Furio
M
M
Meli
A
A
D006916:5-Hydroxytryptophan / Q000494:pharmacology; D000374:Aggression / Q000187:drug effects; D000700:Analgesics; D000818:Animals; D000927:Anticonvulsants / Q000494:pharmacology*; D003984:Dibenzazepines / Q000494:pharmacology* / Q000633:toxicity; D004435:Eating / Q000187:drug effects; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D009422:Nervous System Diseases / Q000139:chemically induced; D051381:Rats; D012890:Sleep / Q000187:drug effects; D013239:Stereotyped Behavior / Q000187:drug effects; D015016:Yohimbine / Q000633:toxicity
D000700:Analgesics; D000927:Anticonvulsants; D003984:Dibenzazepines; D015016:Yohimbine; D006916:5-Hydroxytryptophan; C060314:etazepine