SPECT imaging of the alpha 4 beta 2 nicotinic receptor using (5-I-123)A85380

In order to image nAChR density in vivo in humans, [5- I-123] -iodo-3-[2(S)-2-azetidinylmethoxylpyridine ([5- I-123]A85380) has been developed as a SPECT imaging tracer. This article outlines the radiochemical synthesis, in vitro validation in human post-mortem tissue and some initial in vivo clinical studies using the ligand [5-I-123/125]A85380. Limitations of the usefulness of the tracer for routine clinical use are also discussed. Copyright (c) 2007 John Wiley & Sons, Ltd.