Investigation of the binding kinetics of nicotinic acetylcholine receptors by PET/CT using fluorine-18 labeled Nifene and 2-Fluoro-3-(2(S)-azetidinylmethoxy)pyridine

Conclusions: Both 2-[18F]A85380 and [18F]Nifene were successfully employed in PET/CT mouse brain imaging for the kinetic study of α4β2Rs nicotine receptor, making this study the first to use 2-[18F]A85380 in mouse models. The selectivity of the synthesized probes is consistent with other publications showing the distribution of the α4β2 nicotine receptor in the brain of human and mice. With an understanding of the differences in probe kinetics, we will be able to better study the precise mechanism of nicotine receptor upregulation and the displaceable binding of nicotine and varenicline, which has implications for not only smoking cessation but other neurological conditions such as dementia, anxiety, and attention deficits.

Source: Journal of Nuclear Medicine - May 20, 2019 Category: Nuclear Medicine Authors: Zhang, H., Mitchell, S., Tsai, H.-M., Bhuiyan, M., Leoni, L., Freifelder, R., Kao, C.-M., Zhuang, X., Green, W., Mukherjee, J., Chen, C.-T. Tags: Basic Science (Neurosciences) Posters Source Type: research