@article{oai:repo.qst.go.jp:00046291,
 author = {Fujinaga, Masayuki and Maeda, Jun and Yui, Joji and Hatori, Akiko and Yamasaki, Tomoteru and Kawamura, Kazunori and Kumata, Katsushi and Yoshida, Yuichirou and Nagai, Yuji and Higuchi, Makoto and Suhara, Tetsuya and Fukumura, Toshimitsu and Zhang, Ming-Rong and 藤永 雅之 and 前田 純 and 由井 譲二 and 羽鳥 晶子 and 山崎 友照 and 河村 和紀 and 熊田 勝志 and 吉田 勇一郎 and 永井 裕司 and 樋口 真人 and 須原 哲也 and 福村 利光 and 張 明栄},
 issue = {1},
 journal = {Journal of Neurochemistry},
 month = {Jul},
 note = {We developed 1-(2-[18F]fluoro-3-pyridyl)-4-(2-isopropyl-1-oxoisoindoline-
5-yl)-5-methyl-1H-1,2,3-triazole ([18F]FPIT) as a promising positron emission  tomography (PET) ligand for in vitro and in vivo imaging of metabotropic glutamate receptor type 1 (mGluR1) in rat and monkey brains. In vitro autoradiography with [18F]FPIT was used to determine the distribution of radioactivity in rat and monkey brains. In vivo experiments were performed using dissection and small-animal PET on
rats, and PET on monkey. Metabolite analysis was performed on rat plasma and brain, and monkey plasma. Autoradiography of rat and monkey brains showed that [18F]FPIT binding is aligned with the reported distribution of mGluR1 with high specific binding in the cerebellum and thalamus. PET study on rat and monkey showed high brain uptake and distribution patterns consistent with those seen in the autoradiographic studies. The radioactivity in the brain was significantly decreased
by pre-treatment with unlabeled FPIT, indicative of a specific signal for mGluR1 that was inhibited by mGluR1-selective ligand JNJ-16259865 in the brain. Metabolite analysis showed that the percentage of unchanged [18F]FPIT was 89% in the brain homogenate of rat at 90 min after injection. In the monkey plasma, the percentage of unchanged form was 50% at 90 min. [18F]FPIT produced in vitro and in vivo signals
to visualize mGluR1 expression in rat and monkey brains, suggesting the usefulness of [18F]FPIT for imaging mGluR1 in human brain.},
 pages = {115--124},
 title = {Characterization of 1-(2-[18F]fluoro-3-pyridyl)-4-(2-isopropyl-1-oxo- isoindoline-5-yl)-5-methyl-1H-1,2,3-triazole, a PET ligand for imaging the metabotropic glutamate receptor type 1 in rat and monkey brains},
 volume = {121},
 year = {2011}
}