title: Recent PET radioligands with optimal brain kinetics for imaging nicotinic acetylcholine receptors.
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).
authors.affiliation: Division of Nuclear Medicine, Department of Radiology, Johns Hopkins University, Baltimore, MD, USA.
authors.forename: Andrew G
authors.initials: AG
authors.lastname: Horti
authors.forename: Hiroto
authors.initials: H
authors.lastname: Kuwabara
authors.forename: Daniel P
authors.initials: DP
authors.lastname: Holt
authors.forename: Robert F
authors.initials: RF
authors.lastname: Dannals
authors.forename: Dean F
authors.initials: DF
authors.lastname: Wong
mesh_terms: D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging*; D005462:Fluorine Radioisotopes / Q000737:chemistry / Q000493:pharmacokinetics; D006801:Humans; D008024:Ligands; D018722:Nicotinic Agonists / Q000138:chemical synthesis / Q000493:pharmacokinetics* / Q000494:pharmacology; D049268:Positron-Emission Tomography; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000493:pharmacokinetics* / Q000494:pharmacology; D011978:Receptors, Nicotinic / Q000378:metabolism*
chemical_list: D005462:Fluorine Radioisotopes; D008024:Ligands; D018722:Nicotinic Agonists; D019275:Radiopharmaceuticals; D011978:Receptors, Nicotinic; C403531:nicotinic receptor alpha4beta2
keywords: PET; nAChR; nicotine; radioligand