Plasma concentrations of clobazam and its N-desmethyl metabolite; protection against pentetrazol-induced convulsions in mice.
The anticonvulsant effects of acute administration of clobazam and its principal metabolite N-desmethylclobazam were studied in mice. Pentetrazol, given by slow intravenous infusion 1 or 2 h after the anticonvulsant dose, was used as the convulsant stimulus. Log dose response relationships for both clobazam and N-desmethylclobazam appeared linear, but there was no correlation between plasma concentrations of clobazam and protection. However, correlation between plasma concentrations of N-desmethylclobazam and protection was significant in both cases.
D000818:Animals; D014151:Anti-Anxiety Agents; D000927:Anticonvulsants; D001569:Benzodiazepines; D001570:Benzodiazepinones / Q000097:blood / Q000494:pharmacology*; D000078306:Clobazam; D007279:Injections, Subcutaneous; D008297:Male; D051379:Mice; D010433:Pentylenetetrazole / Q000037:antagonists & inhibitors / Q000633:toxicity; D012640:Seizures / Q000139:chemically induced
D014151:Anti-Anxiety Agents; D000927:Anticonvulsants; D001570:Benzodiazepinones; D001569:Benzodiazepines; D000078306:Clobazam; C024581:N-desmethylclobazam; D010433:Pentylenetetrazole