New iodoreboxetine analogues for SPECT imaging of the noradrenaline transporter

A new route for the stereoselective synthesis of iodinated reboxetine analogues has been developed for the generation of SPECT imaging agents for the noradrenaline transporter (NAT). (2S,3S)- and (2R,3R)-iodoreboxetine were prepared and biological testing against various mono-amine transporters showed these compounds to be potent and selective for NAT.

(2S,3S)- and (2R,3R)-iodoreboxetine analogues have been prepared in a stereoselective manner and biological testing against various mono-amine transporters have shown these compounds to be potent and selective for the noradrenaline transporter.Figure optionsDownload as PowerPoint slide