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N-[18F]Fluoroethylpiperidin-4ylmethyl Acetate, a Novel Lipophilic Acetylcholine Analogue for PET Measurement of Brain Acetylcholinesterase Activity
https://repo.qst.go.jp/records/44211
https://repo.qst.go.jp/records/44211f650ca73-f3b2-4de0-b498-a393f528827e
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2006-06-08 | |||||
| タイトル | ||||||
| タイトル | N-[18F]Fluoroethylpiperidin-4ylmethyl Acetate, a Novel Lipophilic Acetylcholine Analogue for PET Measurement of Brain Acetylcholinesterase Activity | |||||
| 言語 | ||||||
| 言語 | eng | |||||
| 資源タイプ | ||||||
| 資源タイプ識別子 | http://purl.org/coar/resource_type/c_6501 | |||||
| 資源タイプ | journal article | |||||
| アクセス権 | ||||||
| アクセス権 | metadata only access | |||||
| アクセス権URI | http://purl.org/coar/access_right/c_14cb | |||||
| 著者 |
Kikuchi, Tatsuya
× Kikuchi, Tatsuya× Zhang, Ming-Rong× Ikota, Nobuo× Fukushi, Kiyoshi× Okamura, Toshimitsu× Suzuki, Kazutoshi× Arano, Yasushi× Irie, Toshiaki× 菊池 達矢× 張 明栄× 伊古田 暢夫× 福士 清× 岡村 敏充× 鈴木 和年× 荒野 泰× 入江 俊章 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | 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. | |||||
| 書誌情報 |
Journal of Medicinal Chemistry 巻 48, 号 7, p. 2577-2583, 発行日 2005 |
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| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 0022-2623 | |||||
