Inhibition of plasma membrane monoamine
transporters by beta-ketoamphetamines

by
Cozzi NV, Sievert MK, Shulgin AT, Jacob P 3rd, Ruoho AE.
Department of Pharmacology,
East Carolina University School of Medicine,
Greenville, NC 27858, USA.
ncozzi@brody.med.ecu.edu
Eur J Pharmacol. 1999 Sep 17;381(1):63-9.


ABSTRACT

Methcathinone and methylone, the beta-ketone analogues of methamphetamine and 3,4-methylenedioxymethamphetamine (MDMA), respectively, were tested for neurotransmitter uptake inhibition in vitro. The beta-ketones were threefold less potent than the nonketo drugs at inhibiting platelet serotonin accumulation, with IC(50)'s of 34.6+/-4.8 microM and 5.8+/-0.7 microM, respectively. Methcathinone and methylone were similar in potency to methamphetamine and MDMA at catecholamine transporters individually expressed in transfected glial cells. For dopamine uptake, IC(50)'s were 0.36+/-0.06 microM and 0.82+/-0.17 microM, respectively; for noradrenaline uptake, IC(50) values were 0.51+/-0.10 microM and 1. 2+/-0.1 microM, respectively. In chromaffin granules, IC(50)'s for serotonin accumulation were 112+/-8.0 microM for methcathinone and 166+/-12 microM for methylone, 10-fold higher than the respective values for methamphetamine and MDMA. Our results indicate that methcathinone and methylone potently inhibit plasma membrane catecholamine transporters but only weakly inhibit the vesicle transporter.

Methylone
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Methylone and the catecholamines
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Methylone and monoamine neurotransmission


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