Design and evaluation of radioactive acetylcholine analogs for mapping brain acetylcholinesterase (AchE) in vivo.

Abstract

For mapping brain acetylcholinesterase (AchE) in vivo, seven radioactive acetylcholine analogs, N-[14C]methylpiperidyl-3- and 4-acetates, propionates, isobutyrates, and 3-butyrate were newly synthesized and evaluated in mice. The esters readily entered the brain and were hydrolyzed into the hydrophilic metabolite, which was trapped. In brain homogenates, the esters showed a wide range of enzymatic reactivity (about 40-fold), and high specificity for AchE (more than 82%) except the butyrate. Intra-brain distribution of the esters reflected a pattern of AchE activity.

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@article{Irie1994DesignAE, title={Design and evaluation of radioactive acetylcholine analogs for mapping brain acetylcholinesterase (AchE) in vivo.}, author={Toshiaki Irie and Kiyoshi Fukushi and Yukari Akimoto and Hiroshi Tamagami and Takenori Nozaki}, journal={Nuclear medicine and biology}, year={1994}, volume={21 6}, pages={801-8} }