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Nichols; MDA, MDMA and PMA in Serotonin Release

Nichols; MDA, MDMA and PMA in Serotonin Release

  1. Alfa
    Effects of Certain Hallucinogenic Amphetamine Analogues on the Release of
    [3H]Serotonin from Rat Brain Synaptosomes

    Journal of Medicinal Chemistry 1982 May;25(5):530-5

    The enantiomers of 3,4-(methylenedioxy)amphetamine (MDA), p-methoxyamphetamine (PMA), and N-Me-MDA (MDMA), along with their alpha, alpha-dimethylated derivatives, were evaluated for an effect on the release of [3H]serotonin from rat whole brain synaptosomes. The amphetamine isomers were all potent in inducing the release of [3H]serotonin at bath concentrations of 1 and 10 micrometers but were inactive at 0.1 micrometers. No significant difference in isomer potency was observed at the 10 micrometers concentration. However, at 1 micrometer the (+) isomer of MDMA was more effective in inducing release than was the (-) isomer. Since it is the (+) isomer which is clinically active, this result suggests that transmitter release may play a role in the biological activity of MDMA. By contrast, the alpha, alpha-dimethyl compounds were not effective in releasing serotonin, even at the highest bath concentration