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

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

Biochemical pharmacology May 1, 1987 DOI: 10.1016/0006-2952(87)90118-3 via PubMed

Summary

AI-generated from the abstract

After injection into the abdominal cavity, 5-methoxy-N,N-dimethyltryptamine and N,N-dimethyltryptamine are rapidly taken up by and cleared from all tissues examined. Live-animal experiments confirm earlier lab findings that these compounds are metabolized through oxidative deamination, N-demethylation, O-demethylation, and N-oxidation. Analysis of metabolic profiles across tissues identified N-oxides as major metabolites. Pretreating animals with iproniazid successfully inhibited and redirected metabolism away from indole acids toward the parent compounds and their structurally unique metabolites.

Study at a glance

Characteristics In vivo study Peer reviewed
Population Animals
Intervention iproniazid
Citations 75
Key finding N-oxides are major metabolites of 5-methoxy-N,N-dimethyltryptamine and N,N-dimethyltryptamine, and iproniazid pretreatment redirects metabolism away from indole acids toward parent compounds and unique metabolites.

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.

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