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Bioorg Med Chem Lett. 2009 Sep 1;19(17):4996-8. doi: 10.1016/j.bmcl.2009.07.064. Epub 2009 Jul 16.

Design and synthesis of (2R,3S)-iodoreboxetine analogues for SPECT imaging of the noradrenaline transporter.

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1
WestCHEM, Department of Chemistry, University of Glasgow, Glasgow, UK.

Abstract

A stereoselective 10-step synthesis of iodophenoxy analogues of (2R,3S)-reboxetine has been developed with the aim of generating a new SPECT imaging agent for the noradrenaline transporter (NAT). In vitro testing of these compounds against various mono-amine transporters showed an ortho-iodophenoxy analogue to have excellent affinity (K(i) 8.4 nM) and good selectivity for NAT.

PMID:
19640707
DOI:
10.1016/j.bmcl.2009.07.064
[Indexed for MEDLINE]
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