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Synthesis and characterization of 11C-labeled benzyl amidine derivatives as PET radioligands for GluN2B subunit of the NMDA receptors
https://repo.qst.go.jp/records/49349
https://repo.qst.go.jp/records/49349f9e37d90-5e92-4e6b-8fc1-8e2330eaa9da
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2018-11-19 | |||||
| タイトル | ||||||
| タイトル | Synthesis and characterization of 11C-labeled benzyl amidine derivatives as PET radioligands for GluN2B subunit of the NMDA 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 |
Fuchigami, Takeshi
× Fuchigami, Takeshi× Fujimoto, Noriko× Haradahira, Terushi× Nojiri, Yumiko× Okauchi, Takashi× Maeda, Jun× Suhara, Tetsuya× Yamamoto, Fumihiko× Nakayama, Morio× Maeda, Minoru× Mukai, Takahiro× Maeda, Jun× Suhara, Tetsuya |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | GluN2B-containing NMDA receptors (NMDARs) play fundamental roles in learning and memory, although they are also associated with various brain disorders. In this study, we synthesized and evaluated three 11 C-labeled N-benzyl amidine derivatives 2-[11 C]methoxybenzyl) cinnamamidine ([11 C]CBA), N-(2-[11 C]methoxybenzyl)-2- naphthamidine ([11 C]NBA) and N-(2-[11 C]methoxybenzyl)quinoline-3-carboxamidine ([11 C]QBA) as PET radioligands for these receptors. The 11 C-benzyl amidines were synthesized via conventional methylation of corresponding des-methyl precursors with [11 C]CH3 I. In vitro binding characteristics were examined in brain sagittal sections using various GluN2B modulators and off-target ligands. Further, in vivo brain distribution studies were performed in normal mice. The 11 C-labeled benzyl amidines showed high specific binding to the GluN2B subunit at in vitro. In particular, the quinoline derivative [11 C] QBA had the best binding properties in terms of high brain localization to GluN2B-rich regions and specificity to the GluN2B subunit. Conversely, these 11 C-radioligands showed the brain distributions were inconsistent with GluN2B expression in biodistribution experiments. The majority of the radiolabeled compounds were identified as metabolized forms, of which amido derivatives seemed to be the major species. Although these 11 C-ligands had high specific binding to the GluN2B subunit, significant improvement in metabolic stability is necessary for successful PET imaging of the GluN2B subunit of NMDARs. | |||||
| 書誌情報 |
Journal of Labelled Compounds and Radiopharmaceuticals 巻 61, 号 14, p. 1095-1105, 発行日 2018-11 |
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| 出版者 | ||||||
| 出版者 | Wiley | |||||
| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 0362-4803 | |||||
| PubMed番号 | ||||||
| 識別子タイプ | PMID | |||||
| 関連識別子 | 30375667 | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | 10.1002/jlcr.3691 | |||||
| 関連サイト | ||||||
| 識別子タイプ | URI | |||||
| 関連識別子 | https://onlinelibrary.wiley.com/doi/full/10.1002/jlcr.3691 | |||||
