Cerebral and peripheral demethylation of psychotomimetics measured by expired 14CO2.

International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology  – January 01, 1989

Source: PubMed

Summary

Demethylation of psychotomimetic compounds reveals intriguing metabolic pathways. In a study involving rats, 5-Methoxy-N,N-dimethyltryptamine showed no demethylation, challenging existing theories. Conversely, 2,4,5-Trimethoxyphenalkylamines were demethylated significantly less in the brain compared to peripheral sites, especially at the p-methoxy position. This suggests a potential biochemical mechanism that could trigger psychosis from within the body. The findings indicate that the brain may metabolize these compounds differently than other tissues, with implications for understanding psychotic disorders.

Abstract

Demethylation of psychotomimetic compounds was measured by labeling each methyl and methoxy substitutent separately with 14C and injecting it into rats, intravenously and intracerebrally. Expired [14C]CO2 was measured continuously and the resultant multi-exponential curves yielded rates and integral demethylation. 5-Methoxy-N,N-dimethyltryptamine was not demethylated, eliminating one proposed metabolic pathway. 2,4,5-Trimethoxyphenalkylamines were demethylated less in the brain than peripherally, markedly so at the p-methoxy position, suggesting a possible biochemical site for endogenous induction of psychosis.

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