Abstract
We synthesized and evaluated 1-(4-fluorobenzyl)-4-[(5,6-dimethoxy-1-oxoindan-2-yl)methyl]piperidine (4-FDP), which is an analog of donepezil. The 4-[ 18F]FDP was prepared by reductive alkylation of debenzylated donepezil with 4-[ 18F]fluorobenzaldehyde in high radiochemical yield (decay-corrected, 40–52%) and with high effective specific activity (30–38 GBq/μmol). Tissue distribution studies in mice demonstrated nonspecific distribution of the 4-[ 18F]FDP in brain regions, suggesting that this radioligand may not be a suitable agent for in vivo studies of acetylcholinesterase (AChE), despite its potent in vitro biological activity.
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