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J Labelled Comp Radiopharm. 2013 Mar-Apr;56(3-4):159-66. doi: 10.1002/jlcr.3020.

Recent PET radioligands with optimal brain kinetics for imaging nicotinic acetylcholine receptors.

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  • 1Division of Nuclear Medicine, Department of Radiology, Johns Hopkins University, Baltimore, MD, USA.


Cerebral neuronal nicotinic acetylcholine receptors (nAChRs) are implicated in various neurophysiological processes and in the pathophysiology and/or treatment strategies of various disorders. Positron emission tomography (PET) imaging of nAChR and, especially, the most prominent cerebral subtype α4β2-nAChR is important in smoking, epilepsy, attention deficit hyperactivity disorder, depression, schizophrenia, cognition, behavior, memory, and in research involving aging, cognitive impairments, and dementia. Most human α4β2-nAChR PET imaging has been performed with 2-[(18) F]FA, but slow brain kinetics is the substantial drawback of 2-[(18) F]FA that precludes widespread PET imaging research of nAChR in humans. Development of a better PET radioligand for α4β2-nAChR was a focus of substantial investigation that has been thoroughly reviewed (up to 2009) previously. This article attempts to summarize the peer-reviewed publications of the most recent development and preclinical studies of novel α4β2-nAChR PET radioligands with improved brain kinetics and first human studies with one of these radioligands ([(18) F]AZAN).


PET; nAChR; nicotine; radioligand

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