Actions of amphetamine derivatives and cathinone at the noradrenaline transporter.
Linda Cleary, James R. Docherty
European Journal of Pharmacology August 22, 2003 DOI: 10.1016/s0014-2999(03)02173-3 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | In vitro pharmacological study Peer reviewed |
|---|---|
| Population | Rat left ventricular slices and rat cerebral cortex membranes |
| Interventions | MDMA MDA cathinone MDEA cocaine |
| Measures | [3H]noradrenaline uptake, [3H]nisoxetine binding |
| Key points | MDMA, MDA, cathinone, and MDEA all inhibited noradrenaline uptake in rat left ventricular slices, with cocaine, cathinone, and MDMA roughly equipotent and MDA and MDEA significantly less potent. In rat cerebral cortex membranes, MDMA was least potent at displacing [3H]nisoxetine binding. The authors report that the nisoxetine displacement results did not match the functional potency observed in paced rat right ventricle. |
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.
Citations in the library
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- Effects of MDMA, MDA and MDEA on blood pressure, heart rate, locomotor activity and body temperature in the rat involveα‐adrenoceptors British Journal of Pharmacology February 20, 2006
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