Antileptazol activity and kinetics of clobazam and N-desmethyl-clobazam in the guinea-pig.
The kinetic profiles and antileptazol activity of clobazam and its main metabolite were compared to assess the metabolite's contribution to the anticonvulsant activity of clobazam in the guinea-pig. The metabolite was less effective than the parent compound in terms of doses and active brain levels. However, the metabolite formed after clobazam administration accounted for the persistence of antileptazol activity in this animal species.
D000818:Animals; D014151:Anti-Anxiety Agents; D000927:Anticonvulsants; D001569:Benzodiazepines; D001570:Benzodiazepinones / Q000378:metabolism / Q000494:pharmacology*; D001921:Brain / Q000378:metabolism; D000078306:Clobazam; D006168:Guinea Pigs; D006207:Half-Life; D007700:Kinetics; D008297:Male; D010433:Pentylenetetrazole / Q000037:antagonists & inhibitors*; D013045:Species Specificity; D013997:Time Factors
D014151:Anti-Anxiety Agents; D000927:Anticonvulsants; D001570:Benzodiazepinones; D001569:Benzodiazepines; D000078306:Clobazam; C024581:N-desmethylclobazam; D010433:Pentylenetetrazole