@article{oai:repo.qst.go.jp:00047347, author = {Kumata, Katsushi and Yui, Joji and Xie, Lin and Zhang, Yiding and Nengaki, Nobuki and Fujinaga, Masayuki and Yamasaki, Tomoteru and Shimoda, Yoko and Zhang, Ming-Rong and 熊田 勝志 and 由井 譲二 and 謝 琳 and 張 一鼎 and 念垣 信樹 and 藤永 雅之 and 山崎 友照 and 下田 陽子 and 張 明栄}, issue = {16}, journal = {Bioorganic & medicinal chemistry letters}, month = {Aug}, note = {Three compounds 1-3 containing methyl-sufanyl, sufinyl, or sulfonyl groups are strong inhibitors of glycogen synthase kinase 3β (GSK-3β), an enzyme associated with Alzheimer's disease. We labeled 1-3 with (11)C for a positron emission tomography (PET) brain imaging study. A novel thiophenol precursor 4 for radiosynthesis was prepared by reacting sulfoxide 2 with trifluoroacetic anhydride. [(11)C]1 was synthesized by reacting 4 with [(11)C]methyl iodide in 52±5% radiochemical yield (n=5, based on [(11)C]CO2, corrected for decay). Oxidation of [(11)C]1 with Oxone® produced [(11)C]2 and [(11)C]3, respectively. PET with [(11)C]1 and [(11)C]3 showed 2 fold higher brain uptake of radioactivity in a mouse model of cold water stress in which GSK-3β expression was increased, than in the controls.}, pages = {3230--3233}, title = {Radiosynthesis and preliminary PET evaluation of glycogen synthase kinase 3β (GSK-3β) inhibitors containing [(11)C]methylsulfanyl, [(11)C]methylsulfinyl or [(11)C]methylsulfonyl groups.}, volume = {25}, year = {2015} }