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    Eur J Pharmacol. 2003 Aug 22;476(1-2):31-4.

    Actions of amphetamine derivatives and cathinone at the noradrenaline transporter.

    Cleary L, Docherty JR.

    Source

    Department of Physiology, Royal College of Surgeons in Ireland, 123 St. Stephen's Green, Dublin 2, Ireland.

    Abstract

    We have recently shown that methylenedioxymethamphetamine (MDMA), methylenedioxyamphetamine (MDA), cathinone and methylenedioxyethylamphetamine (MDEA) have a cocaine-like action to potentiate the contractile actions of noradrenaline but not isoprenaline in the 1-Hz paced rat right ventricle. The purpose of this study was to directly test the actions of these compounds at the noradrenaline transporter. In rat left ventricular slices, potency (-log IC50) values at inhibiting uptake of [3H]noradrenaline were: cocaine 6.16+/-0.15, cathinone 6.03+/-0.16, MDMA 6.05+/-0.07, MDA 5.68+/-0.06 and MDEA 5.56+/-0.08. MDEA and MDA were significantly less potent. In rat cerebral cortex membranes, MDMA was significantly less potent at displacing [3H]nisoxetine binding; -log EC50 values: cocaine 5.04+/-0.08, cathinone 5.40+/-0.14, MDA 4.66+/-0.11, MDEA 4.99+/-0.15, MDMA 4.22+/-0.07. The noradrenaline uptake studies showed that MDEA was least potent: MDEA was also least potent functionally in the paced rat right ventricle. The [3H]nisoxetine displacement studies did not compare with the functional studies.

    PMID:
    12969746
    [PubMed - indexed for MEDLINE]

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