兔肝微粒体体外对N,N-二烷基苯胺的N-氧化和α-C-氧化作用
The N- and alpha- C-oxidation of N,N-dialkylanilines by rabbit liver microsomes in vitro.
作者信息
Gorrod J W, Temple D J, Beckett A H
出版信息
Xenobiotica. 1979 Jan;9(1):17-25. doi: 10.3109/00498257909034700.
PMID:760319
Abstract
- A method for the determination of N,N-dialkylanilines and their metabolites by g.l.c. is described. 2. N-Demethylation and N-oxidation are important routes of metabolism of N-alkyl-N-methylanilines. 3. N-dealkylation, except the removal of a N-t-butyl group, occurs during the metabolism of N,N-dialkylanilines. 4. N-oxidation was found with N,N-dimethyl and N,N-diethylaniline and all N-methyl-N-alkylanilines examined except N-methyl-N-t-butylaniline. 5. A good correlation was found between the hydrophobic bonding constant (pi) and the extent of demethylation of a series of N-alkyl-N-methylanilines.
摘要
- 描述了一种用气相色谱法测定N，N-二烷基苯胺及其代谢物的方法。2. N-去甲基化和N-氧化是N-烷基-N-甲基苯胺代谢的重要途径。3. N，N-二烷基苯胺代谢过程中会发生N-脱烷基化，但去除N-叔丁基的情况除外。4. 在N，N-二甲基苯胺和N，N-二乙苯胺以及除N-甲基-N-叔丁基苯胺外所检测的所有N-甲基-N-烷基苯胺中均发现了N-氧化现象。5. 发现一系列N-烷基-N-甲基苯胺的疏水键常数（π）与去甲基化程度之间存在良好的相关性。
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