Saxena N, Pandey V C, Puri S K, Dutta G P
Indian J Med Res. 1989 Sep;89:330-3.
A new 8-aminoquinoline derivative (compound 80/53) synthesized at the Central Drug Research Institute, Lucknow (India), has been found to be an active anti-relapse (tissue schizontocidal) compound. Compound 80/53 at 8.75 mg/kg x 4 days and primaquine at 7.00 mg/kg (base) x 4 days given orally to Swiss mice led to inhibition of the different components of the hepatic microsomal mixed function oxidase system to varying degrees. Compound 80/53 inhibited cytochrome P-450, aminopyrine-N-demethylase, aniline and benzo (a) pyrene hydroxylase, cytochrome b5 and heme content of the normal mice by 12, 14, 0, 57, 20 and 6 per cent respectively, whereas the inhibition caused by primaquine in these components was 25, 21, 17, 48, 26 and 6 per cent respectively. Thus, there was less inhibition of hepatic microsomal MFO system of mice by compound 80/53 as compared to that by primaquine.
印度勒克瑙中央药物研究所合成的一种新型8-氨基喹啉衍生物（化合物80/53），已被发现是一种有效的抗复发（组织裂殖体杀灭）化合物。给瑞士小鼠口服8.75毫克/千克×4天的化合物80/53和7.00毫克/千克（碱）×4天的伯氨喹，会在不同程度上抑制肝微粒体混合功能氧化酶系统的不同组分。化合物80/53分别使正常小鼠的细胞色素P-450、氨基比林-N-脱甲基酶、苯胺和苯并（a）芘羟化酶、细胞色素b5和血红素含量抑制12%、14%、0%、57%、20%和6%，而伯氨喹对这些组分的抑制分别为25%、21%、17%、48%、26%和6%。因此，与伯氨喹相比，化合物80/53对小鼠肝微粒体MFO系统的抑制作用较小。
