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Synthesis and biological evaluation of 1-(4-[18F]fluorobenzyl)-4-[(5,6-dimethoxy-1-oxoindan-2-yl)methyl]piperidine for in vivo studies of acetylcholinesterase |
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| Authors: | Lee S Y Choe Y S Sugimoto H Kim S E Hwang S H Lee K Choi Y Lee J Kim B |
| Affiliation: | 1 Department of Nuclear Medicine, Samsung Medical Center, Sungkyunkwan University School of Medicine, Center for Clinical Research, Samsung Biomedical Research Institute, Seoul, South Korea 2 School of Pharmacy, Seoul National University, Seoul, South Korea 3 Tsukuba Research Laboratories, Eisai Co., Ltd., Tsukuba-shi, Ibaraki, Japan |
| 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. |
| Keywords: | Alzheimer’s disease 4-fluorodonepezil 18F Acetylcholinesterase |
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