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大鼠体内5-甲氧基-N,N-二甲基色胺和N,N-二甲基色胺的代谢

In vivo metabolism of 5-methoxy-N,N-dimethyltryptamine and N,N-dimethyltryptamine in the rat.

作者信息

Sitaram B R, Lockett L, Talomsin R, Blackman G L, McLeod W R

出版信息

Biochem Pharmacol. 1987 May 1;36(9):1509-12. doi: 10.1016/0006-2952(87)90118-3.

DOI:10.1016/0006-2952(87)90118-3
PMID:3472526
Abstract

Following intraperitoneal administration, 5-methoxy-N,N-dimethyltryptamine and N,N-dimethyltryptamine are subject to both a very rapid uptake into, and clearance from, all tissues examined. The current studies in vivo confirm previous in vitro observations that the routes involved in the metabolism of these compounds include oxidative deamination, N-demethylation, O-demethylation, and N-oxidation. The analysis of metabolic profiles in various tissues led to the identification of the N-oxides as major metabolites. The successful inhibition and redirection of metabolism away from the indole acids towards the parent compounds and their structurally unique metabolites were demonstrated in animals pretreated with iproniazid.

摘要

腹腔注射后,5-甲氧基-N,N-二甲基色胺和N,N-二甲基色胺会迅速被所有检测组织摄取并清除。目前的体内研究证实了先前的体外观察结果,即这些化合物代谢所涉及的途径包括氧化脱氨、N-去甲基化、O-去甲基化和N-氧化。对各种组织中代谢谱的分析导致鉴定出N-氧化物为主要代谢产物。在用异烟肼预处理的动物中,成功证明了代谢从吲哚酸转向母体化合物及其结构独特的代谢产物的抑制和重定向。

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