title: Cerebral and peripheral demethylation of psychotomimetics measured by expired 14CO2.
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.
authors.affiliation: Biomedical Division, Lawrence Berkeley Laboratory, University of California, Berkeley, CA 94720.
authors.forename: T
authors.initials: T
authors.lastname: Sargent
authors.forename: U
authors.initials: U
authors.lastname: Braun
authors.forename: G
authors.initials: G
authors.lastname: Braun
authors.forename: N
authors.initials: N
authors.lastname: Kusubov
authors.forename: K S
authors.initials: KS
authors.lastname: Bristol
mesh_terms: D000662:Amphetamines / Q000008:administration & dosage / Q000493:pharmacokinetics*; D000818:Animals; D001711:Biotransformation; D001921:Brain / Q000378:metabolism*; D002245:Carbon Dioxide / Q000032:analysis*; D002250:Carbon Radioisotopes / Q000032:analysis; D006213:Hallucinogens / Q000008:administration & dosage / Q000493:pharmacokinetics*; D006801:Humans; D007267:Injections; D007275:Injections, Intravenous; D008732:Methoxydimethyltryptamines / Q000493:pharmacokinetics*; D008745:Methylation; D015394:Molecular Structure; D010627:Phenethylamines / Q000008:administration & dosage / Q000493:pharmacokinetics*; D051381:Rats; D011919:Rats, Inbred Strains; D011985:Receptors, Serotonin / Q000378:metabolism; D012559:Schizophrenia / Q000378:metabolism; D013329:Structure-Activity Relationship; D014363:Tryptamines / Q000493:pharmacokinetics*
chemical_list: D000662:Amphetamines; D002250:Carbon Radioisotopes; D006213:Hallucinogens; D008732:Methoxydimethyltryptamines; D010627:Phenethylamines; D011985:Receptors, Serotonin; D014363:Tryptamines; C013344:2,4,5-trimethoxyphenylisopropylamine; D002245:Carbon Dioxide; C059578:2,4,5-trimethoxyphenethylamine