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The role of metabolism in 3,4-(+/-)-methylenedioxyamphetamine and 3.4-(+/-)-methylenedioxymethamphet

The role of metabolism in 3,4-(+/-)-methylenedioxyamphetamine and 3.4-(+/-)-methylenedioxymethamphet

  1. testodan
    3,4-Methylenedioxyamphetamine (MDA) and 3,4-
    methylenedioxymethamphetamine (MDMA, ecstasy) are ringsubstituted amphetamine derivatives with stimulant and hallucinogenic properties. The recreational use of these amphetamines, especiallyMDMA, is prevalent despite warnings of irreversible damage to the central nervous system. MDA and MDMA are primarily serotonergic
    neurotoxicants. Because (1) neither MDA nor MDMA produces neurotoxicity when injected directly into brain, (2) intracerebroventricular
    (ICV) administration of some major metabolites of
    MDA and MDMA fails to reproduce their neurotoxicity, (3) -methyldopamine (-MeDA) and N-methyl--MeDA are metabolites of
    both MDA and MDMA, (4) -MeDA and N-methyl--MeDA are readily oxidized to the corresponding ortho-quinones, which can undergo
    conjugation with glutathione (GSH), and (5) quinone thioethers exhibit a variety of toxicologic activities, we initiated studies on the potential role of thioether metabolites of -MeDA and N-methyl--
    MeDA in the neurotoxicity of MDA and MDMA..