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Quantitative Molecular Imaging of Neuronal Nicotinic Acetylcholine Receptors in the Human Brain with A-85380 Radiotracers

[ Vol. 7 , Issue. 2 ]


Shahrdad Lotfipour, Mark Mandelkern and Arthur L. Brody   Pages 107 - 112 ( 6 )


Neuronal nicotinic acetylcholine receptors (nAChRs) have been implicated in a spectrum of cognitive functions as well as psychiatric and neurodegenerative disorders, including tobacco addiction and Alzheimer's Disease. The examination of neuronal nAChRs in living humans is a relatively new field. Researchers have developed brain-imaging radiotracers for nAChRs, with radiolabeled A-85380 compounds having the most widespread use. We provide a brief background on nAChRs, followed by a discussion of the development and application of A-85380 radiotracers in human imaging studies. We describe potential future studies using nicotinic receptor radioligands for the study of tobacco addiction, including the mechanism of action of the smoking-cessation therapy varenicline. Throughout this review, we focus on the significant potential that resides in the identification and quantification of nAChRs in the living human brain.


Nicotinic acetylcholine receptors, positron emission tomography, single-photon emission computed tomography, human brain imaging, tobacco dependence, varenicline, 2FA, 5IA, A-85380, endogenous, neurotransmitter, Toxicology


Semel Institute, Department of Psychiatry, David Geffen School of Medicine, University of California, Los Angeles, CA 90095, USA.

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