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The Designer Methcathinone Analogs, Mephedrone and Methylone, are Substrates for Monoamine Transport

The Designer Methcathinone Analogs, Mephedrone and Methylone, are Substrates for Monoamine Transport

  1. Shampoo
    The nonmedical use of ‘designer’ cathinone analogs, such as 4-methylmethcathinone (mephedrone) and 3,4-methylenedioxymethcathinone (methylone), is increasing worldwide, yet little information is available regarding the mechanism of action for these drugs. Here, we
    employed in vitro and in vivo methods to compare neurobiological effects of mephedrone and methylone with those produced by the
    structurally related compounds, 3,4-methylenedioxymethamphetamine (MDMA) and methamphetamine. In vitro release assays using rat
    brain synaptosomes revealed that mephedrone and methylone are nonselective substrates for plasma membrane monoamine
    transporters, similar to MDMA in potency and selectivity. In vivo microdialysis in rat nucleus accumbens showed that i.v. administration of
    0.3 and 1.0 mg/kg of mephedrone or methylone produces dose-related increases in extracellular dopamine and serotonin (5-HT), with
    the magnitude of effect on 5-HT being greater. Both methcathinone analogs were weak motor stimulants when compared with
    methamphetamine. Repeated administrations of mephedrone or methylone (3.0 and 10.0 mg/kg, s.c., 3 doses) caused hyperthermia but
    no long-term change in cortical or striatal amines, whereas similar treatment with MDMA (2.5 and 7.5 mg/kg, s.c., 3 doses) evoked robust
    hyperthermia and persistent depletion of cortical and striatal 5-HT. Our data demonstrate that designer methcathinone analogs are
    substrates for monoamine transporters, with a profile of transmitter-releasing activity comparable to MDMA. Dopaminergic effects of
    mephedrone and methylone may contribute to their addictive potential, but this hypothesis awaits confirmation. Given the widespread
    use of mephedrone and methylone, determining the consequences of repeated drug exposure warrants further study