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Uptake and Release Effects of Diethylpropion and its Metabolites with Biogenic Amine Transporters (HanYu et al 2000)

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Uptake and Release Effects of Diethylpropion and its Metabolites with Biogenic Amine Transporters (HanYu et al 2000)

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Bioorganic & Medicinal Chemistry 8 (2000) 2689±2692

HanYu, Richard B.Rothman, Christina M.Dersch, John S.Partilla
and Kenner C.Rice

Abstract
Three metabolites of diethylpropion (1), ()2-ethylamino-1-phenyl-propan-1-one (2), (1R,2S)-(-)-N,N-diethylnorephe-
drine (3a) and (1S,2R)-(ÿ)-N,N-diethylnorephedrine (3b) were synthesized. Their uptake and release effects with biogenic amine
transporters were evaluated. A major finding of this study is that the in vivo activity of diethylpropion on biogenic amine transporters is most likely due to metabolite 2 as diethylpropion (1) and the metabolites 3a and 3b showed little or no e€ect in the assays studied. These studies also revealed that 2 acted as a substrate at the norepinephrine (IC50=99 nM) and serotonin transporters (IC50=2118 nM) and an uptake inhibitor at the dopamine transporter (IC50=1014 nM). The potent action of 2 at the NE transporter supports the hypothesis that amphetamine-type subjective effects may be mediated in part by brain norepinephrine.

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