The substituted amphetamines 3,4-methylenedioxymethamphetamine, methamphetamine, p-chloroamphetamine and fenfluramine induce 5-hydroxytryptamine release via a common mechanism blocked by fluoxetine and cocaine

Urs V. Berger, Xi F. Gu, Efrain C. Azmitia

Research output: Contribution to journalArticle

Abstract

The abilities of the substituted amphetamines 3,4-methylenedioxymethamphetamine (MDMA), methamphetamine, p-chloroamphetamine (PCA) and fenfluramine to induce synaptosomal [3H]serotonin (5-HT) release were compared using a novel microassay system. The rank order of release potencies was found to be (±)PCA {reversed tilde equals} (+)-fenfluramine > (+)-MDMA ≫ (+)-methamphetamine. Combination of two drugs at their EC50 did not cause more release than either drug alone at an equivalent concentration. In addition, the 5-HT uptake blockers fluoxetine and cocaine inhibited the release induced by MDMA, methamphetamine, PCA and fenfluramine to the same percentage. However, threshold concentrations of the substituted amphetamines known to inhibit uptake did not attenuate the release caused by higher concentrations of these compounds. These results suggests that MDMA, methamphetamine, PCA and fenfluramine cause 5-HT release via a common mechanism. Furthermore, these results indicate that the 5-HT uptake blockade induced by these substituted amphetamines in vitro is different from that induced by either fluoxetine or cocaine.

Original languageEnglish (US)
Pages (from-to)153-160
Number of pages8
JournalEuropean Journal of Pharmacology
Volume215
Issue number2-3
DOIs
StatePublished - May 14 1992

Keywords

  • 5-HT (5-hydroxytryptamine
  • Amphetamine analogues
  • Monoamine release
  • Synaptosomes
  • serotonin)

ASJC Scopus subject areas

  • Pharmacology

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