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

Andrew G. Horti, Hiroto Kuwabara, Daniel P. Holt, Robert F. Dannals, Dean F. Wong

Research output: Contribution to journalReview articlepeer-review

21 Scopus citations


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-[18F]FA, but slow brain kinetics is the substantial drawback of 2-[18F]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 ([18F]AZAN).

Original languageEnglish
Pages (from-to)159-166
Number of pages8
JournalJournal of Labelled Compounds and Radiopharmaceuticals
Issue number3-4
StatePublished - 2013


  • PET
  • nAChR
  • nicotine
  • radioligand


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