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Evaluation of (-)-[18 F]Flubatine-specific binding: Implications for reference region approaches
- Source :
- Synapse. 72:e22016
- Publication Year :
- 2017
- Publisher :
- Wiley, 2017.
-
Abstract
- We aimed to characterize changes in binding of (-)-[18 F]Flubatine to α4 β2 *-nicotinic acetylcholine receptors (α4 β2 *-nAChRs) during a tobacco cigarette smoking challenge. Displacement of (-)-[18 F]Flubatine throughout the brain was quantified as change in (-)-[18 F]Flubatine distribution volume (VT ), with particular emphasis on regions with low VT . Three tobacco smokers were imaged with positron emission tomography (PET) during a 210 min bolus-plus-constant infusion of (-)-[18 F]Flubatine. A tobacco cigarette was smoked in the PET scanner ∼125 min after the start of (-)-[18 F]Flubatine injection. Equilibrium analysis was used to estimate VT at baseline (90-120 min) and after cigarette challenge (180-210 min), at the time of greatest receptor occupancy by nicotine. Smoking reduced VT by 21 ± 9% (average ±SD) in corpus callosum, 17 ± 9% in frontal cortex, 36 ± 11% in cerebellum, and 22 ± 10% in putamen. The finding of displaceable (-)-[18 F]Flubatine binding throughout the brain is an important consideration for reference region-based quantification approaches with this tracer. We observed displacement of (-)-[18 F]Flubatine binding to α4 β2 *-nicotinic acetylcholine receptors in corpus callosum by a tobacco cigarette challenge. We conclude that reference region approaches utilizing corpus callosum should first perform careful characterization of displaceable (-)-[18 F]Flubatine binding and nondisplaceable kinetics in this putative reference region.
- Subjects :
- medicine.medical_specialty
Cerebellum
Chemistry
Putamen
Corpus callosum
030227 psychiatry
White matter
Nicotine
03 medical and health sciences
Cellular and Molecular Neuroscience
0302 clinical medicine
Nicotinic agonist
Endocrinology
medicine.anatomical_structure
Internal medicine
medicine
Receptor
030217 neurology & neurosurgery
Acetylcholine receptor
medicine.drug
Subjects
Details
- ISSN :
- 08874476
- Volume :
- 72
- Database :
- OpenAIRE
- Journal :
- Synapse
- Accession number :
- edsair.doi...........004ab6ae3e002065bcf934e54c7ac65b