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.
Publication types
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Comparative Study
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Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
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Amphetamines / administration & dosage
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Amphetamines / pharmacokinetics*
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Animals
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Biotransformation
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Brain / metabolism*
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Carbon Dioxide / analysis*
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Carbon Radioisotopes / analysis
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Hallucinogens / administration & dosage
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Hallucinogens / pharmacokinetics*
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Humans
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Injections
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Injections, Intravenous
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Methoxydimethyltryptamines / pharmacokinetics*
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Methylation
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Molecular Structure
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Phenethylamines / administration & dosage
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Phenethylamines / pharmacokinetics*
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Rats
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Rats, Inbred Strains
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Receptors, Serotonin / metabolism
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Schizophrenia / metabolism
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Structure-Activity Relationship
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Tryptamines / pharmacokinetics*
Substances
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Amphetamines
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Carbon Radioisotopes
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Hallucinogens
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Methoxydimethyltryptamines
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Phenethylamines
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Receptors, Serotonin
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Tryptamines
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2,4,5-trimethoxyphenylisopropylamine
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Carbon Dioxide
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2,4,5-trimethoxyphenethylamine