@article{oai:repo.qst.go.jp:00047422,
 author = {Fujinaga, Masayuki and Yamasaki, Tomoteru and Nengaki, Nobuki and Ogawa, Masanao and Kumata, Katsushi and Shimoda, Yoko and Yui, Joji and Xie, Lin and Zhang, Yiding and Kawamura, Kazunori and Zhang, Ming-Rong and 藤永 雅之 and 山崎 友照 and 念垣 信樹 and 小川 政直 and 熊田 勝志 and 下田 陽子 and 由井 譲二 and 謝 琳 and 張 一鼎 and 河村 和紀 and 張 明栄},
 issue = {2},
 journal = {Bioorganic & medicinal chemistry letters},
 month = {Jan},
 note = {ADX88178 (1) has been recently developed as a potent positive allosteric modulator for metabotropic glutamate receptor 4 (mGluR4). The aim of this study was to develop [(11)C]1 as a novel positron emission tomography ligand and to evaluate its binding ability for mGluR4. Using stannyl precursor 3, [(11)C]1 was efficiently synthesized by introducing an [(11)C]methyl group into a pyrimidine ring via C-(11)C coupling and deprotection reactions, in 16±6% radiochemical yield (n=10). At the end of synthesis, 0.54-1.10GBq of [(11)C]1 was acquired with >98% radiochemical purity and 90-120GBq/μmol of specific activity. In vitro autoradiography and ex vivo biodistribution study in rat brains showed specific binding of [(11)C]1 in the cerebellum, striatum, thalamus, cerebral cortex, and medulla oblongata, which showed dose-dependent decreases by administration with multi-dose of unlabeled 1.},
 pages = {370--374},
 title = {Radiosynthesis and evaluation of 5-methyl-N-(4-[(11)C]methylpyrimidin-2-yl)-4-(1H-pyrazol-4-yl)thiazol-2-amine ([(11)C]ADX88178) as a novel radioligand for imaging of metabotropic glutamate receptor subtype 4 (mGluR4).},
 volume = {26},
 year = {2016}
}