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腹腔注射后N,N-二甲基色胺和α,α,β,β-四氘代-N,N-二甲基色胺的脑内水平比较。体内动力学同位素效应。

Comparison of the brain levels of N,N-dimethyltryptamine and alpha, alpha, beta, beta-tetradeutero-N-N-dimethyltryptamine following intraperitoneal injection. The in vivo kinetic isotope effect.

作者信息

Barker S A, Beaton J M, Christian S T, Monti J A, Morris P E

出版信息

Biochem Pharmacol. 1982 Aug 1;31(15):2513-6. doi: 10.1016/0006-2952(82)90062-4.

DOI:10.1016/0006-2952(82)90062-4
PMID:6812592
Abstract

A comparison of the brain levels (microgram/g wet weight of tissue) of the hallucinogen N,N-dimethyltryptamine (DMT) and its deuterated analog alpha, alpha, beta, beta-tetradeutero-DMT (D4DMT) as a function of time and dose is reported. It was observed that the presence of deuterium in the alpha- and beta-positions of the ethylamine side-chain led to a potentiation of the level of DMT in brain. Strikingly different dynamics of uptake and clearance were also noted. We propose that these results are due to primary kinetic isotope effect, illustrating the importance of the alpha-position in the metabolism of DMT.

摘要

本文报告了致幻剂N,N-二甲基色胺(DMT)及其氘代类似物α,α,β,β-四氘代-DMT(D4DMT)的脑内水平(微克/克组织湿重)随时间和剂量变化的比较。研究发现,乙胺侧链α位和β位存在氘会使脑内DMT水平增强。同时还注意到摄取和清除的动力学存在显著差异。我们认为这些结果是由于初级动力学同位素效应,这说明了α位在DMT代谢中的重要性。

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