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Development of Novel PET Probes for Central 2-Amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid (AMPA) Receptors
https://repo.qst.go.jp/records/47535
https://repo.qst.go.jp/records/47535ab264dd6-307c-4c92-a894-b8b31714a519
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2016-09-05 | |||||
| タイトル | ||||||
| タイトル | Development of Novel PET Probes for Central 2-Amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid (AMPA) Receptors | |||||
| 言語 | ||||||
| 言語 | eng | |||||
| 資源タイプ | ||||||
| 資源タイプ識別子 | http://purl.org/coar/resource_type/c_6501 | |||||
| 資源タイプ | journal article | |||||
| アクセス権 | ||||||
| アクセス権 | metadata only access | |||||
| アクセス権URI | http://purl.org/coar/access_right/c_14cb | |||||
| 著者 |
Oi, Norihito
× Oi, Norihito× Tokunaga, Masaki× Suzuki, Michiyuki× Nagai, Yuji× Nakatani, Yosuke× Yamamoto, Noboru× Maeda, Jun× Minamimoto, Takafumi× Zhang, Ming-Rong× Suhara, Tetsuya× Higuchi, Makoto× 大井 紀人× 徳永 正希× 鈴木 成教× 永井 裕司× 中谷 陽介× 前田 純× 南本 敬史× 張 明栄× 須原 哲也× 樋口 真人 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | 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. | |||||
| 書誌情報 |
Journal of Medicinal Chemistry Manuscript 巻 58, 号 21, p. 8444-8462, 発行日 2015-10 |
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| 出版者 | ||||||
| 出版者 | ACS Publications | |||||
| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 0022-2623 | |||||
| PubMed番号 | ||||||
| 識別子タイプ | PMID | |||||
| 関連識別子 | 26469379 | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | 10.1021/acs.jmedchem.5b00712 | |||||
| 関連サイト | ||||||
| 識別子タイプ | URI | |||||
| 関連識別子 | http://pubs.acs.org/doi/abs/10.1021/acs.jmedchem.5b00712 | |||||
| 関連名称 | http://pubs.acs.org/doi/abs/10.1021/acs.jmedchem.5b00712 | |||||
