Title: 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 Lee SY, Choe YS, Sugimoto H, Kim SE, Hwang SH, Lee K, Choi Y, Lee J, Kim B Ref: Nucl Med Biol, 27:741, 2000 : PubMed
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-[(18)F]FDP was prepared by reductive alkylation of debenzylated donepezil with 4-[(18)F]fluorobenzaldehyde in high radiochemical yield (decay-corrected, 40-52%) and with high effective specific activity (30-38 GBq/micromol). Tissue distribution studies in mice demonstrated nonspecific distribution of the 4-[(18)F]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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Lee SY, Choe YS, Sugimoto H, Kim SE, Hwang SH, Lee K, Choi Y, Lee J, Kim B (2000) 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 Nucl Med Biol27: 741-4
Lee SY, Choe YS, Sugimoto H, Kim SE, Hwang SH, Lee K, Choi Y, Lee J, Kim B (2000) Nucl Med Biol27: 741-4