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Synthesis and In Vitro Evaluation of Three Novel Radiotracers for Imaging of Metabotropic Glutamate Receptor Subtype 2 in Rat Brain
https://repo.qst.go.jp/records/48069
https://repo.qst.go.jp/records/480697408afa8-90ef-49b7-8efb-fa1c0452b45b
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2017-07-04 | |||||
| タイトル | ||||||
| タイトル | Synthesis and In Vitro Evaluation of Three Novel Radiotracers for Imaging of Metabotropic Glutamate Receptor Subtype 2 in Rat Brain | |||||
| 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 |
Kumata, Katsushi
× Kumata, Katsushi× Yamasaki, Tomoteru× Hatori, Akiko× Zhang, Yiding× Mori, Wakana× Fujinaga, Masayuki× Xie, Lin× Ohkubo, Takayuki× Nengaki, Nobuki× Zhang, Ming-Rong× 熊田 勝志× 山崎 友照× 羽鳥 晶子× 張 一鼎× 森 若菜× 藤永 雅之× 謝 琳× 大久保 崇之× 念垣 信樹× 張 明栄 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | The purpose of this study was to develop three new radiotracers, 1-(cyclopropylmethyl)-4-([11C/18F]substituted-phenyl)piperidin-1-yl-2-oxo-1,2-dihydropyridine-3-carbonitrile ([11C]1, [11C]2, and [18F]4), and to examine their specific bindings with metabotropic glutamate receptor subtype 2 (mGluR2) in rat brain sections by using in vitro autoradiography. These compounds were found to possess potent in vitro binding affinities (Ki: 8.0-34.1nM) for mGluR2 in rat brain homogenate. [11C]1, [11C]2, and [18F]4 were synthesized by [11C/18F]alkylation of the corresponding phenol precursors with [11C]methyl iodide or [18F]fluoroethyl bromide with >98% radiochemical purity and 80-130GBq/μmol specific activity at the end of synthesis. In vitro autoradiography indicated that these radiotracers showed heterogeneous specific bindings in mGluR2-rich brain regions, such as the cerebral cortex, striatum, hippocampus, and granular layer of the cerebellum. | |||||
| 書誌情報 |
Bioorganic & Medicinal Chemistry Letters 巻 27, 号 14, p. 3139-3143, 発行日 2017-05 |
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| 出版者 | ||||||
| 出版者 | Elsevier | |||||
| PubMed番号 | ||||||
| 識別子タイプ | PMID | |||||
| 関連識別子 | 28571823 | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | 10.1016/j.bmcl.2017.05.029 | |||||
