@article{oai:repo.qst.go.jp:00047557,
 author = {Shimoda, Yoko and Yamasaki, Tomoteru and Fujinaga, Masayuki and Ogawa, Masanao and Kurihara, Yusuke and Nengaki, Nobuki and Kumata, Katsushi and Yui, Joji and Hatori, Akiko and Xie, Lin and Zhang, Yiding and Kawamura, Kazunori and Zhang, Ming-Rong and 下田 陽子 and 山崎 友照 and 藤永 雅之 and 小川 政直 and 栗原 雄祐 and 念垣 信樹 and 熊田 勝志 and 由井 譲二 and 羽鳥 晶子 and 謝 琳 and 張 一鼎 and 河村 和紀 and 張 明栄},
 issue = {8},
 journal = {Journal of Medicinal Chemistry},
 month = {Apr},
 note = {We found out 3-[5-(pyridin-2-yl)-2H-tetrazol-2-yl]benzonitrile analogues as the candidate for positron emission tomography (PET) imaging agents of metabotropic glutamate receptor subtype 5 (mGluR5). Among these compounds, 3-methyl-5-(5-(pyridin-2-yl)-2H-tetrazol-2-yl)benzonitrile (10) exhibited high binding affinity (Ki = 9.4 nM) and moderate lipophilicity (cLogD, 2.4). Subsequently, [11C]10 was radiosynthesized at 25 ± 14% radiochemical yield (n = 11) via C-[11C]methylation of the arylstannyl precursor 15 with [11C]methyl iodide. In vitro autoradiography and PET assessments using [11C]10 showed high specific binding in the striatum and hippocampus, two brain regions enriched with mGluR5. Moreover, test–retest PET studies with [11C]10 indicated high reliability to quantify mGluR5 density, such as the intraclass correlation coefficient (0.90) and Pearson r (0.91) in the striatum of rat brain. We demonstrated that [11C]10 is a useful PET ligand for imaging and quantitative analysis of mGluR5. Furthermore, [11C]10 might be modified using its skeleton as a lead compound.},
 pages = {3980--3990},
 title = {Synthesis and Evaluation of Novel Radioligands Based on 3-[5-(Pyridin-2-yl)-2H-tetrazol-2-yl]benzonitrile for Positron Emission Tomography Imaging of Metabotropic Glutamate Receptor Subtype 5},
 volume = {59},
 year = {2016}
}