Clinical Perspective and Recent Development of PET Radioligands for Imaging Cerebral Nicotinic Acetylcholine Receptors

Cerebral nicotinic acetylcholine receptors (nAChR) are linked to various brain functions and disorders. There is a critical necessity for PET imaging of nAChR to study the role of the nicotinic system in the central nervous system. Currently, only two PET radioligands (2-[18F]FA and 6-[18F]FA) for the nAChR imaging are available, but they exhibit substantial drawbacks in imaging quality and potential for quantification. This article summarizes recent progress in the PET imaging of nAChR human subjects and surveys the studies of several research groups whose aim is the development of nAChR PET radioligands with improved imaging properties.