Syntheses and biological evaluation of 18F-labeled 3-(1-benzyl-piperidin-4-yl)-1-(1-methyl-1H-indol-3-yl)propan-1-ones for in vivo mapping of acetylcholinesterase

Add time:07/30/2019    Source:sciencedirect.com

We synthesized novel 18F-labeled acetylcholinesterase (AChE) inhibitors, 3-[1-(3- and 4-[18F]fluoromethylbenzyl)piperidin-4-yl]-1-(1-methyl-1H-indol-3-yl)propan-1-ones ([18F]1 and [18F]2) and 3-[1-(4-[18F]fluorobenzyl)piperidin-4-yl]-1-(1-methyl-1H-indol-3-yl)propan-1-one ([18F]3) in high yields (decay-corrected, 25%–40%) and with high effective specific activities (>37 GBq/μmol). Tissue distribution studies of the [18F]1 and the [18F]3 in mice showed the nonspecific bindings in brain regions, with metabolic defluorination of the [18F]1. The result suggests that these radioligands may not be suitable agents for in vivo mapping of AChE, despite their potent in vitro anti-AChE activities.

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