Pacifici G M, Cuoci L, Placidi G F
Gen Pharmacol. 1984;15(4):353-5. doi: 10.1016/0306-3623(84)90014-4.
The distribution in subcellular fractions of pinazepam (Pz) and its metabolite N-desmethyldiazepam (N-Dz) was studied after a single oral administration of Pz (20 mg/kg body wt) to rats. Animals were killed 2 min and 6 hr after dosing. The amounts of the parent drug and its metabolite retrieved in the microsomal fraction were small, but significantly higher than those in the nuclear, mitochondrial and soluble fractions. The cytosol contained the lowest percentages of both drugs. No substantial difference was found in the subcellular distribution pattern of both Pz and N-Dz 2 min and 6 hr after administration.
给大鼠单次口服匹那西泮(Pz,20毫克/千克体重)后,研究了匹那西泮及其代谢产物N-去甲基地西泮(N-Dz)在亚细胞组分中的分布情况。给药后2分钟和6小时处死动物。微粒体组分中回收的母体药物及其代谢产物的量很少,但显著高于细胞核、线粒体和可溶性组分中的量。胞质溶胶中两种药物的含量百分比最低。给药后2分钟和6小时,Pz和N-Dz的亚细胞分布模式没有发现实质性差异。