Jobson Nicola K, Crawford Andrew R, Dewar Deborah, Pimlott Sally L, Sutherland Andrew
WestCHEM, Department of Chemistry, University of Glasgow, Glasgow, UK.
Bioorg Med Chem Lett. 2009 Sep 1;19(17):4996-8. doi: 10.1016/j.bmcl.2009.07.064. Epub 2009 Jul 16.
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.
为了开发一种用于去甲肾上腺素转运体（NAT）的新型单光子发射计算机断层扫描（SPECT）成像剂，已开发出一种立体选择性的10步合成(2R,3S)-瑞波西汀碘苯氧基类似物的方法。对这些化合物针对各种单胺转运体的体外测试表明，一种邻碘苯氧基类似物对NAT具有优异的亲和力（K(i) 8.4 nM）和良好的选择性。
