@misc{oai:repo.qst.go.jp:00068544, author = {張, 明栄 and 土山, 明男 and 原田平, 輝志 and 古塚, 賢士 and 吉田, 勇一郎 and 木田, 多香依 and 野口, 順子 and 入江, 俊章 and 鈴木, 和年 and 張 明栄 and 原田平 輝志 and 古塚 賢士 and 吉田 勇一郎 and 入江 俊章 and 鈴木 和年}, month = {Nov}, note = {N-[18F]Fluoroethyl-4-piperidyl acetate ([18F]FEtP4A), an analog of acetyicholine, was designed as a PET tracer for mapping braine acetylcholinesterase (AchE) activity. Thistracer was prepared by reacting 4-piperidyl acetate (P4A) with [18F]Fluoroethyl bromide ([18F]FEtBr) at 130 degree-C for 30 min. [18F]FEtP4A showed an excellent BBB permeability into brain and its initial uptake in the brain was >8% injected dose /g tissue. The distribution pattern of radioactivity in brain was striatum>cerebral cortex>cerebellum within 10_120 min postinjection, which reflected the distribution rank pattern of AchE activity in the brain. Chemical analysis of in vivo or in vitro radioactive metabolites in mouse and rat brains indicated that. [18F]FEtP4A was specifically hydrolyzed to N-[18F]hluoroethyl-4-piperidinol([18F]FEtP4OH) by AchE. From these results, [18F]FEtP4A may become a promising PET tracer for mapping brain AchE., 第10回日本薬学会医薬化学部会年会}, title = {脳内アセチルコリンエステラーゼPETイメージング剤[18F]FEtP4Aの創製}, year = {2001} }