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Imaging of transmembrane AMPA receptor regulatory protein by positron emission tomography
https://repo.qst.go.jp/records/86471
https://repo.qst.go.jp/records/86471cb6e170f-8195-4605-8e95-79f00ed70b1d
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2022-07-05 | |||||
| タイトル | ||||||
| タイトル | Imaging of transmembrane AMPA receptor regulatory protein by positron emission tomography | |||||
| 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 |
Qingzhen, Yu,
× Qingzhen, Yu,× Katsushi, Kumata× Jian, Rong,× Zhen, Chen,× Tomoteru, Yamasaki× Jiahui, Chen,× Zhiwei, Xiao,× Hideki, Ishii× Atsuto, Hiraishi× Tuo, Shao,× Zhang, Yiding× Kuan, Hu× Lin, Xie× Masayuki, Fujinaga× Chunyu, Zhao,× Wakana, Mori× Thomas, Collier,× Ahmed, Haider,× Susumu, Tomita,× Zhang, Ming-Rong× Steven, Liang,× Katsushi, Kumata× Tomoteru, Yamasaki× Hideki, Ishii× Atsuto, Hiraishi× Zhang, Yiding× Kuan, Hu× Lin, Xie× Masayuki, Fujinaga× Wakana, Mori× Zhang, Ming-Rong |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | ABSTRACT: The transmembrane α-amino-3-hydroxyl-5-methyl-4-isoxazolepropionic acid (AMPA) receptor regulatory protein γ-8 (TARP γ-8) constitutes an auxiliary subunit of AMPA receptors, which mediates various brain functions including learning and memory. TARP γ-8 has emerged as a promising therapeutic target for central nervous system disorders. Despite considerable efforts, previously reported TARP γ-8 PET radioligands, such as [ 11C]TARP-1903 and [11C]TARP-1811 series, were plagued by limited brain uptake and/or high nonspecific binding in vivo. Herein, we developed two novel 11C-labeled probes, [11C]8 and [11C]15 (also named as [11C]TARP2105), of which the latter exhibited a reasonable brain uptake as well as specific binding toward TARP γ-8 both in vitro and in vivo, as confirmed by blocking experiments with the commercially available TARP γ-8 inhibitor, JNJ-55511118 in the TARP γ-8-rich hippocampus. Overall, [11C]15 exhibited promising tracer characteristics and proved to be a lead positron-emission tomography ligand for the non-invasive quantification of TARP γ-8 in the mammalian brain. |
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| 書誌情報 |
Journal of Medicinal Chemistry 巻 65, 号 13, p. 9144-9158, 発行日 2022-06 |
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| 出版者 | ||||||
| 出版者 | American Chemical Society | |||||
| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 0022-2623 | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | 10.1021/acs.jmedchem.2c00377 | |||||
| 関連サイト | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | https://doi.org/10.1021/acs.jmedchem.2c00377 | |||||
