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Bioorg Med Chem. 2009 Jun 1;17(11):3770-4. doi: 10.1016/j.bmc.2009.04.057. Epub 2009 May 3.

A novel photoaffinity ligand for the dopamine transporter based on pyrovalerone.

Author information

1
Division of Pharmaceutical Sciences, Duquesne University Mylan School of Pharmacy, 600 Forbes Avenue, Pittsburgh, PA 15282, USA. lapinskyd@duq.edu

Abstract

Non-tropane-based photoaffinity ligands for the dopamine transporter (DAT) are relatively unexplored in contrast to tropane-based compounds such as cocaine. In order to fill this knowledge gap, a ligand was synthesized in which the aromatic ring of pyrovalerone was substituted with a photoreactive azido group. The analog 1-(4-azido-3-iodophenyl)-2-pyrrolidin-1-yl-pentan-1-one demonstrated appreciable binding affinity for the DAT (K(i)=78+/-18 nM), suggesting the potential utility of a radioiodinated version in structure-function studies of this protein.

PMID:
19442525
PMCID:
PMC2696686
DOI:
10.1016/j.bmc.2009.04.057
[Indexed for MEDLINE]
Free PMC Article

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