Evaluation of (-)-[18 F]Flubatine-specific binding: Implications for reference region approaches.
Synapse
; 72(3)2018 03.
Article
en En
| MEDLINE
| ID: mdl-29105121
ABSTRACT
We aimed to characterize changes in binding of (-)-[18 F]Flubatine to α4 ß2 *-nicotinic acetylcholine receptors (α4 ß2 *-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 â¼125 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 ß2 *-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.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Banco de datos:
MEDLINE
Asunto principal:
Benzamidas
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Encéfalo
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Receptores Nicotínicos
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Compuestos Bicíclicos Heterocíclicos con Puentes
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Radiofármacos
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Tomografía de Emisión de Positrones
Tipo de estudio:
Evaluation_studies
Límite:
Adult
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Female
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Humans
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Male
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Middle aged
Idioma:
En
Revista:
Synapse
Asunto de la revista:
NEUROLOGIA
Año:
2018
Tipo del documento:
Article