@article{oai:repo.qst.go.jp:00047535,
 author = {Oi, Norihito and Tokunaga, Masaki and Suzuki, Michiyuki and Nagai, Yuji and Nakatani, Yosuke and Yamamoto, Noboru and Maeda, Jun and Minamimoto, Takafumi and Zhang, Ming-Rong and Suhara, Tetsuya and Higuchi, Makoto and 大井 紀人 and 徳永 正希 and 鈴木 成教 and 永井 裕司 and 中谷 陽介 and 前田 純 and 南本 敬史 and 張 明栄 and 須原 哲也 and 樋口 真人},
 issue = {21},
 journal = {Journal of Medicinal Chemistry Manuscript},
 month = {Oct},
 note = {We document the development of PET probes for central AMPA receptors and their application to in vivo imaging of animals. Initial screening of perampanel derivatives was performed to identify probe candidates. Despite the high autoradiographic contrast yielded by several radioligands, rat PET scans did not support their in vivo suitability. Further focused derivatization and second screening by ex vivo LC-MS measurements led to the selection of 2-[1-(3-methylaminophenyl)-2-oxo-5-(pyrimidin-2-yl)-1,2-dihydropyridin-3-yl]benzonitrile, 21a, and its analogs as candidates. [11C]21a was shown by autoradiography to specifically bind to the neocortex and hippocampus, consistent with AMPA receptor localization. PET imaging with [11C]21a demonstrated moderate uptake of radioactivity in rat and monkey brains, with the retention of radiosignals being consistent with autoradiograms, and the uptake was blocked by pretreatment with unlabeled 21a in a dose-dependent manner. The current approach has facilitated the discovery of a PET probe potentially suitable for translational research and development focused on AMPA receptors.},
 pages = {8444--8462},
 title = {Development of Novel PET Probes for Central 2-Amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid (AMPA) Receptors},
 volume = {58},
 year = {2015}
}