@article{oai:repo.qst.go.jp:00046088, author = {Yamasaki, Tomoteru and Fujinaga, Masayuki and Yoshida, Yuichiro and Kumata, Katsushi and Yui, Joji and Kawamura, Kazunori and Hatori, Akiko and Fukumura, Toshimitsu and Zhang, Ming-Rong and 山崎 友照 and 藤永 雅之 and 吉田 勇一郎 and 熊田 勝志 and 由井 譲二 and 河村 和紀 and 羽鳥 晶子 and 福村 利光 and 張 明栄}, issue = {10}, journal = {Bioorganic & Medicinal Chemistry Letters}, month = {May}, note = {The purpose of this study was to develop 4-[18F]fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide ([18F]FITM, [18F]4) as a new PET ligand for imaging metabotropic glutamate receptor subtype 1 (mGluR1). [18F]4 was synthesized by [18F]fluorination of a novel nitro precursor 3 with [18F]KF in the presence of Kryptofix 222. At the end of synthesis, 429-936 MBq (n = 8) of [18F]4 was obtained with >99% radiochemical purity and 204-559 GBq/mumol specific activity starting from 6.7 to 13.0 GBq of [18F]F;. The brain distribution of [18F]4 was determined by the in vitro and ex vivo autoradiography using rat brain sections. The in vitro and in vivo specific binding of [18F]4 to mGluR1 was detected in the cerebellum, thalamus, hippocampus, and striatum. These results suggest that [18F]4 is a promising PET ligand for the in vivo evaluation of mGluR1.}, pages = {2998--3001}, title = {Radiosynthesis and preliminary evaluation of 4-[18F]fluoro-N-[4-[6-(isopropylamino) pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide as a new positron emission tomography ligand for metabotropic glutamate receptor subtype 1}, volume = {21}, year = {2011} }