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丙硫氧嘧啶对细胞色素b5和NADH细胞色素b5还原酶的选择性诱导作用。

Selective induction of cytochrome b5 and NADH cytochrome b5 reductase by propylthiouracil.

作者信息

Kariya K, Lee E, Yamaoka M, Ishikawa H

出版信息

Life Sci. 1984 Dec 3;35(23):2327-34. doi: 10.1016/0024-3205(84)90524-1.

Abstract

Both the cytochrome b5 level and NADH cytochrome b5 reductase activity in rat liver microsomes were increased 2-fold by repeated i.p. administration of 1.5 mmol/kg propylthiouracil (PTU) for 2 weeks, but neither the cytochrome P-450 level nor NADPH cytochrome P-450 reductase activity were affected by the treatment. Liver microsomes from PTU-treated rats showed a significant decrease in aminopyrine N-demethylation, but not in benzphetamine N-demethylation, aniline hydroxylation or 7-ethoxycoumarin O-deethylation. A single administration of the compound had no effect on any components of the system. In vitro, drug hydroxylation activities were not affected by PTU up to 1.0 mM. From the above evidence, repeated administration of PTU selectively induced cytochrome b5 and NADH cytochrome b5 reductase in rat liver microsomes.

摘要

通过腹腔注射1.5 mmol/kg丙硫氧嘧啶(PTU),连续2周,大鼠肝微粒体中的细胞色素b5水平和NADH细胞色素b5还原酶活性均增加了2倍,但细胞色素P-450水平和NADPH细胞色素P-450还原酶活性均未受该处理的影响。PTU处理大鼠的肝微粒体中氨基比林N-脱甲基作用显著降低,但苄非他明N-脱甲基作用、苯胺羟化作用或7-乙氧基香豆素O-脱乙基作用未受影响。单次给药该化合物对该系统的任何组分均无影响。在体外,高达1.0 mM的PTU对药物羟化活性无影响。根据上述证据,重复给药PTU可选择性诱导大鼠肝微粒体中的细胞色素b5和NADH细胞色素b5还原酶。

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