@article{oai:repo.qst.go.jp:00044211,
 author = {Kikuchi, Tatsuya and Zhang, Ming-Rong and Ikota, Nobuo and Fukushi, Kiyoshi and Okamura, Toshimitsu and Suzuki, Kazutoshi and Arano, Yasushi and Irie, Toshiaki and 菊池 達矢 and 張 明栄 and 伊古田 暢夫 and 福士 清 and 岡村 敏充 and 鈴木 和年 and 荒野 泰 and 入江 俊章},
 issue = {7},
 journal = {Journal of Medicinal Chemistry},
 month = {},
 note = {The reduction of acetylcholinesterase (AchE) actvity in the brain has been measured in dementia disorders such as Alzheimer's disease and dementia with Lewy bodies 11C-lebeled acetylcholine analogues, N-[11C]methylpiperidein-4-yl acetate and propionate, and positron emission tomography (PET). Our aim was to develop an 18F-labeled acetylcholine analogue useful for brain AchE mapping with PET, since 18F, with a longer half-life, has advantages over 11C. In a preliminary study, a series of N-[11C]ethylpiperidin-3-yl or -4-ylmethanol esters (acetyl and propionyl esters) were newly designed and evaluated in vitro regarding the reactivity with and specificity to AchE using purified human enzymes, leading to a novel 18F-labeled acetylcholine analogue, N-[18F]fluoroethylpiperidin-4-ylmethyl acetate. In ret experiments, the 18F-labeled candidate showed desirable properties for PET AchE measurement: high brain uptake of the authentic eater, high AchE specificity, a moderate hydrolysis rate, and low membrane permeability (metabolic trapping) of the metabolite.},
 pages = {2577--2583},
 title = {N-[18F]Fluoroethylpiperidin-4ylmethyl Acetate, a Novel Lipophilic Acetylcholine Analogue for PET Measurement of Brain Acetylcholinesterase Activity},
 volume = {48},
 year = {2005}
}