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Methylene‐dioxy‐pyrovalerone (MDPV) is a potent inhibitor of hDAT and hNET
Author(s) -
Solis Ernesto,
Cameron Krasnodara N,
Kolanos Renata,
Glen Richard A,
De Felice Louis J
Publication year - 2013
Publication title -
the faseb journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.709
H-Index - 277
eISSN - 1530-6860
pISSN - 0892-6638
DOI - 10.1096/fasebj.27.1_supplement.885.2
Subject(s) - norepinephrine transporter , dopamine transporter , chemistry , transporter , dopamine , pharmacology , xenopus , hek 293 cells , catecholamine , biochemistry , biology , neuroscience , gene
Bath salts is a relatively new abused drug with varying composition of either a single or a combination of β‐ketophenylethylamines. A common ingredient of bath salts is methylenedioxypyrovalerone (MDPV). Recent studies have shown MDPV is a potent uptake inhibitor for the human dopamine transporter (hDAT) and the human norepinephrine transporter (hNET). Here we explore the effect of MDPV on the electrical currents mediated by hDAT expressed in Xenopus laevis oocytes, as well as its effect on the uptake of fluorescent substrates mediated by hDAT or hNET expressed in HEK‐293 cells. These data will characterize MDPV action on catecholamine transporters and further our understanding of this abused drug. Our data shows MDPV is 30 fold more potent than cocaine (COC) in inhibiting dopamine (DA) uptake and its inhibition is longer lasting in both expression systems. We will further investigate the structural determinants responsible for the unique properties of MDPV.