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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.

Author information

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

Abstract

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).

KEYWORDS:

PET; nAChR; nicotine; radioligand

PMID:
24285321
DOI:
10.1002/jlcr.3020
[PubMed - indexed for MEDLINE]
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