Evaluation of [18F]-(-)-norchlorofluorohomoepibatidine ([18F]-(-)-NCFHEB) as a PET radioligand to image the nicotinic acetylcholine receptors in non-human primates

An efficient microfluidic synthetic method was developed for preparation of [18F]-(-)-NCFHEB. PET examination in rhesus monkeys showed that [18F]-(-)-NCFHEB entered the brain readily and its regional radioactivity uptake pattern was in accordance with the known distribution of α4β2 receptors. Estimated non-displaceable binding potential (BPND) values in brain regions were better than those of [18F]2-FA and comparable to [18F]AZAN. These results confirm previous findings and support further examination of [18F]-(-)-NCFHEB in humans.