PT  - JOURNAL ARTICLE
AU  - C. D. MORGAN
AU  - F. CATTABENI
AU  - E. COSTA
TI  - METHAMPHETAMINE, FENFLURAMINE AND THEIR N-DEALKYLATED METABOLITES: EFFECT ON MONOAMINE CONCENTRATIONS IN RAT TISSUES
DP  - 1972 Jan 01
TA  - Journal of Pharmacology and Experimental Therapeutics
PG  - 127--135
VI  - 180
IP  - 1
4099  - http://jpet.aspetjournals.org/content/180/1/127.short
4100  - http://jpet.aspetjournals.org/content/180/1/127.full
SO  - J Pharmacol Exp Ther1972 Jan 01; 180
AB  - The sensitive technique of gas chromatography-mass spectrometry was used to detect and identify metabolites of methamphetamine and fenfluramine in rat tissue after i.p. administration of doses which cause tissue monoamine depletion. Methamphetamine (90µmol/kg) causes a long-lasting depletion of heart norepinephrine and a shorter-lasting depletion of brain norepinephrine and 5-hydroxytryptamine, whereas fenfluramine (90µmol/kg) produces a selective and long-lasting depletion of brain 5-hydroxytryptamine. After production of trimethylsilyl heptafluorobutyryl derivatives of these drugs and their metabolites, the technique of mass fragmentography facilitated the detection and identification of the N-dealkylated metabolites of methamphetamine, amphetamine and p-hydroxyamphetamine in tissues. The N-dealkylated metabolite of fenfiuramine, norfenfluramine, was similarly detected in tissue homogenates of rats killed up to 24 hours after injection. The N-dealkylation of both drugs involves a stereoisomeric dependence and gives rise to metabolites which persist in tissues and conceivably are involved in tissue monoamine depletion. © 1972, by The Williams & Wilkins Company