Jobson, N., Crawford, A., Dewar, D., Pimlott, S. and Sutherland, A. (2009) Design and synthesis of (2R,3S)-iodoreboxetine analogues for SPECT imaging of the noradrenaline transporter. Bioorganic and Medicinal Chemistry Letters, 19(17), pp. 4996-4998. (doi: 10.1016/j.bmcl.2009.07.064)
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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.
Item Type: | Articles |
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Status: | Published |
Refereed: | Yes |
Glasgow Author(s) Enlighten ID: | Dewar, Dr Deborah and Pimlott, Dr Sally and Sutherland, Professor Andrew |
Authors: | Jobson, N., Crawford, A., Dewar, D., Pimlott, S., and Sutherland, A. |
College/School: | College of Medical Veterinary and Life Sciences > School of Psychology & Neuroscience College of Science and Engineering > School of Chemistry |
Journal Name: | Bioorganic and Medicinal Chemistry Letters |
ISSN: | 0960-894X |
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