氯巴占和N-去甲基氯巴占在豚鼠体内的抗惊厥活性及动力学

Antileptazol activity and kinetics of clobazam and N-desmethyl-clobazam in the guinea-pig.

作者信息

Ballabio M, Caccia S, Garattini S, Guiso G, Zanini M G

出版信息

Arch Int Pharmacodyn Ther. 1981 Oct;253(2):192-9.

Abstract

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.

摘要

比较了氯巴占及其主要代谢物的动力学特征和抗惊厥活性，以评估该代谢物对氯巴占在豚鼠体内抗惊厥活性的贡献。就剂量和脑内活性水平而言，该代谢物的效果不如母体化合物。然而，氯巴占给药后形成的代谢物导致了该动物物种中抗惊厥活性的持续存在。