@article{oai:repo.qst.go.jp:00045985,
 author = {Fujinaga, Masayuki and Yamasaki, Tomoteru and Kawamura, Kazunori and Kumata, Katsushi and Hatori, Akiko and Yui, Joji and Yanamoto, Kazuhiko and Yoshida, Yuichiro and Ogawa, Masanao and Nengaki, Nobuki and Maeda, Jun and Fukumura, Toshimitsu and Zhang, Ming-Rong and 藤永 雅之 and 山崎 友照 and 河村 和紀 and 熊田 勝志 and 羽鳥 晶子 and 由井 譲二 and 柳本 和彦 and 吉田 勇一郎 and 小川 政直 and 念垣 信樹 and 前田 純 and 福村 利光 and 張 明栄},
 issue = {1},
 journal = {Bioorganic & Medicinal Chemistry},
 month = {Nov},
 note = {The purpose of this study was to synthesize 6-[1-(2-[18F]fluoro-3-pyridyl)-5-methyl-1H-1,2,3-triazol-4-yl]quinoline ([18F]FPTQ, [18F]7a) and to evaluate its potential as a positron emission tomography ligand for imaging metabotropic glutamate receptor type 1 (mGluR1) in the rat brain. Compound [18F]7a was synthesized by [18F]fluorination of 6-[1-(2-bromo-3-pyridyl)-5-methyl-1H-1,2,3-triazol-4-yl]quinoline
(7b) with potassium [18F]fluoride. At the end of synthesis, 1280–1830 MBq (n = 8) of [18F]7a was obtained with >98% radiochemical purity and 118–237 GBq/lmol specific activity using 3300–4000 MBq of [18F]F-. In vitro autoradiography showed that [18F]7a had high specific binding with mGluR1 in the rat brain. Biodistribution study using a dissection method and small-animal PET showed that [18F]7a had high uptake in the rat brain. The uptake of radioactivity in the cerebellum was reduced by unlabeled 7a and mGluR1-selective ligand JNJ-16259685 (2), indicating that [18F]7a had in vivo specific binding with mGluR1. Because of a low amount of radiolabeled metabolite present in the brain, [18F]7a may have a limiting potential for the in vivo imaging of mGluR1 by PET.},
 pages = {102--110},
 title = {Synthesis and evaluation of 6-[1-(2-[18F]fluoro-3-pyridyl)-5-methyl-1H-1,2,3-triazol-4-yl]quinoline for positron emission tomography imaging of the metabotropic glutamate receptor type 1 in brain},
 volume = {19},
 year = {2010}
}