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

Biochemical pharmacology  – May 01, 1987

Source: PubMed

Summary

5-methoxy-N,N-dimethyltryptamine and N,N-dimethyltryptamine rapidly enter and exit tissues after intraperitoneal administration. In studies involving 20 animals, significant metabolic pathways were identified, including oxidative deamination and N-demethylation, with N-oxides emerging as major metabolites. Notably, pretreating animals with iproniazid successfully redirected metabolism away from indole acids towards the original compounds and their unique metabolites. This highlights potential avenues for optimizing the therapeutic effects of these compounds through metabolic manipulation.

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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