Atypical dopamine efflux caused by 3,4-methylenedioxypyrovalerone (MDPV) via the human dopamine transporter

作者：Shekar Aparna; Aguilar Jenny I; Galli Greta; Cozzi Nicholas V; Brandt Simon D; Ruoho Arnold E; Baumann Michael H; Matthies Heinrich J G; Galli Aurelio^*

来源：Journal of Chemical Neuroanatomy, 2017, 83: 69-74.

DOI：10.1016/j.jchemneu.2017.01.004

• 3,4-methylenedioxypyrovalerone
• Dopamine transporter
• Amphetamine
• Drosophila

Synthetic cathinones are similar in chemical structure to amphetamines, and their behavioral effects are associated with enhanced dopaminergic signaling. The past ten years of research on the common constituent of bath salts, MDPV (the synthetic cathinone 3,4-methylenedioxypyrovalerone), has aided the understanding of how synthetic cathinones act at the dopamine (DA) transporter (DAT). Several groups have described the ability of MDPV to block the DAT with high-affinity. In this study, we demonstrate for the first time a new mode of action of MDPV, namely its ability to promote DATmediated DA efflux. Using single cell amperometric assays, we determined that low concentrations of MDPV (1 nM) can cause reverse transport of DA via DAT. Notably, administration of MDPV leads to hyperlocomotion in Drosophila melanogaster. These data describe further how MDPV acts at the DAT, possibly paving the way for novel treatment strategies for individuals who abuse bath salts.

• 出版日期2017-10
• 单位NIH