Caccia S, Ballabio M, Zanini M G, Garattini S, Samanin R
Eur J Drug Metab Pharmacokinet. 1982;7(2):93-7. doi: 10.1007/BF03188724.
The antileptazol effect of CP 1414 S (7-nitro-2-amino-3-phenyl-3H-1,5-benzodiazepine-4-one) a newly developed 1,5 benzodiazepine, lasts longer in mice than in rats. After intraperitoneal injection (10 mg/kg) brain levels of the drug were higher and persisted for longer in the mouse than in the rat. Although it cannot be excluded tht possible metabolites of CP 1414 S may contribute to the anticonvulsant effect of CP 1414 S, in both species the protective effect correlates well with the brain concentrations of the drug.
新开发的1,5 - 苯二氮䓬类药物CP 1414 S(7 - 硝基 - 2 - 氨基 - 3 - 苯基 - 3H - 1,5 - 苯二氮䓬 - 4 - 酮)的抗印防己毒素作用在小鼠体内持续的时间比在大鼠体内长。腹腔注射(10毫克/千克)后,该药物在小鼠脑内的水平高于大鼠,且持续时间更长。虽然不能排除CP 1414 S的可能代谢产物可能对其抗惊厥作用有贡献,但在这两个物种中,保护作用都与药物在脑内的浓度密切相关。