@article{oai:repo.qst.go.jp:00046536,
 author = {Fujinaga, Masayuki and Yamasaki, Tomoteru and Maeda, Jun and Yui, Joji and Xie, Lin and Nagai, Yuji and Nengaki, Nobuki and Hatori, Akiko and Kumata, Katsushi and Kawamura, Kazunori and Zhang, Ming-Rong and 藤永 雅之 and 山崎 友照 and 前田 純 and 由井 譲二 and 謝 琳 and 永井 裕司 and 念垣 信樹 and 羽鳥 晶子 and 熊田 勝志 and 河村 和紀 and 張 明栄},
 issue = {24},
 journal = {Journal of Medicinal Chemistry},
 month = {Nov},
 note = {Three novel 4-substituted benzamides have been synthesized as potential ligands for the positron emission tomography (PET) imaging of metabotropic glutamate 1 (mGlu1) receptor in the brain. Of these compounds, N-(4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl)-N,4-dimethylbenzamide (4) exhibited the highest binding affinity (Ki =13.6 nM) for mGlu1 and was subsequently labeled with carbon-11. In vitro autoradiography using rat brain sections showed that [11C]4 binding was consistent with the distribution of mGlu1, with high specific binding in the cerebellum and thalamus. PET studies with [11C]4 in monkey showed a high brain uptake and a kinetic profile suitable for quantitative analysis. Pretreatment with a mGlu1-selective ligand 16 largely decreased the brain uptake, indicating high in vivo specific binding of [11C]4 to mGlu1. In metabolite analysis, only unchanged [11C]4 was found in the brain. [11C]4 is a useful PET ligand for the imaging and quantitative analysis of mGlu1 in monkey brain and merits further evaluation in humans.},
 pages = {11042--11051},
 title = {Development of N-[4-[6-(Isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methyl-4-[(11)C]methylbenzamide for Positron Emission Tomography Imaging of Metabotropic Glutamate 1 Receptor in Monkey Brain.},
 volume = {55},
 year = {2012}
}