WEKO3
アイテム
Synthesis and preliminary evaluation of 4-hydroxy-6-(3-[11C]methoxyphenethyl)pyridazin-3(2H)-one, a 11C-labeled d-amino acid oxidase (DAAO) inhibitor for PET imaging
https://repo.qst.go.jp/records/80122
https://repo.qst.go.jp/records/80122979406ba-944c-4206-857b-58092b3acb6c
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2020-06-29 | |||||
| タイトル | ||||||
| タイトル | Synthesis and preliminary evaluation of 4-hydroxy-6-(3-[11C]methoxyphenethyl)pyridazin-3(2H)-one, a 11C-labeled d-amino acid oxidase (DAAO) inhibitor for PET imaging | |||||
| 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 |
Deng, Xiaoyun
× Deng, Xiaoyun× Zhang, Yiding× Chen, Zhen× Kumata, Katsushi× Van, Richard× Rong, Jian× Shao, Tuo× Hatori, Akiko× Mori, Wakana× Yu, Qingzhen× Kuan, Hu× Fujinaga, Masayuki× Hsiao-Ying, Wey× Shao, Yihan× Josephson, Lee× Murtas, Giulia× Pollegioni, Loredano× Ming-Rong, Zhang× Liang, Huan× Zhang, Yiding× Kumata, Katsushi× Hatori, Akiko× Mori, Wakana× Kuan, Hu× Fujinaga, Masayuki× Ming-Rong, Zhang× Liang, Huan |
|||||
| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Selective DAAO inhibitors have demonstrated promising therapeutic effects in clinical studies, including clinically alleviating symptoms of schizophrenic patients and ameliorating cognitive function in Alzheimer’s patients with early phase. Herein we report the synthesis and preliminary evaluation of a 11C-labeled positron emission tomography ligand based on a DAAO inhibitor, DAO-1903 (8). 11C-Isotopologue of 8 was prepared in high radiochemical yield with high radiochemical purity (>99%) and high molar activity (>37 GBq/µmol). In vitro autoradiography studies indicated that the ligand possessed high in vitro specific binding to DAAO, while in vivo dynamic PET studies demonstrated that [11C]8 failed to cross the blood–brain barrier possibly due to moderate brain efflux mechanism. Further chemical scaffold optimization is necessary to overcome limited brain permeability and improve specific binding. | |||||
| 書誌情報 |
Bioorganic & Medicinal Chemistry Letters 巻 30, 号 16, 発行日 2020-06 |
|||||
| 出版者 | ||||||
| 出版者 | Elsevier | |||||
| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 0960-894X | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | 10.1016/j.bmcl.2020.127326 | |||||
| 関連サイト | ||||||
| 識別子タイプ | URI | |||||
| 関連識別子 | https://www.sciencedirect.com/science/article/abs/pii/S0960894X20304376 | |||||
