Design and synthesis of (2R,3S)-iodoreboxetine analogues for SPECT imaging of the noradrenaline transporter |
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| Authors: | Nicola K. Jobson Andrew R. Crawford Deborah Dewar Sally L. Pimlott Andrew Sutherland |
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| Affiliation: | 1. WestCHEM, Department of Chemistry, The Joseph Black Building, University of Glasgow, Glasgow G12 8QQ, UK;2. Division of Clinical Neuroscience, Faculty of Medicine, University of Glasgow, Glasgow G12 8QQ, UK;3. West of Scotland Radionuclide Dispensary, University of Glasgow and North Glasgow University Hospital NHS Trust, Glasgow G11 6NT, UK |
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| 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 (Ki 8.4 nM) and good selectivity for NAT. |
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