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氰化物对大鼠肝脏微粒体中药物氧化作用的抑制

Inhibition by cyanide of drug oxidations in rat liver microsomes.

作者信息

Kitada M, Chiba K, Kamataki T, Kitagawa H

出版信息

Jpn J Pharmacol. 1977 Oct;27(5):601-8. doi: 10.1254/jjp.27.601.

Abstract

Cyanide inhibited microsomal activities of aniline hydroxylation and aminopyrine, ethylmorphine and codeine demethylations and produced a modified type II difference spectrum of cytochrome P-450 to give two spectral dissociation constants, 0.21mM and 1.05 mM. The binding of cyanide to cytochrome P-450 resulted in innhibition of NADPH-cytochrome P-450 reductase activity. The cyanide inhibition of drug oxidations was partially avoided by increasing oxygen tension. A possible mechanism for the inhibition of drug oxidations by cyanide is discussed.

摘要

氰化物抑制苯胺羟化以及氨基比林、乙基吗啡和可待因去甲基化的微粒体活性,并产生细胞色素P-450的一种修饰的II型差示光谱,得出两个光谱解离常数,分别为0.21mM和1.05mM。氰化物与细胞色素P-450的结合导致NADPH-细胞色素P-450还原酶活性受到抑制。通过提高氧张力可部分避免氰化物对药物氧化的抑制作用。文中讨论了氰化物抑制药物氧化的一种可能机制。

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