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Imaging the trace amine-associated receptor 1 by positron emission tomography
https://repo.qst.go.jp/records/82773
https://repo.qst.go.jp/records/8277393a0e72a-c039-4f31-8499-1ecad3fd8416
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2021-03-18 | |||||
| タイトル | ||||||
| タイトル | Imaging the trace amine-associated receptor 1 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 |
Sun, Jiyun
× Sun, Jiyun× Chen, Jiahui× Katsushi, Kumata× Xiao, Zhiwei× Rong, Jiang× Haider, Ahmed× Shao, Tuo× Lu, Wang× Xu, Hao× Zhang, Ming-Rong× Liang, Huan× Katsushi, Kumata× Lu, Wang× Zhang, Ming-Rong× Liang, Huan |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Trace amine-associated receptor 1 (TAAR1) has been implicated in drug addiction, schizophrenia, depression and Parkinson’s disease (PD). To date, there are no reports on TAAR1-targeted probes for non-invasive quantification of receptor density in vivo. Herein, we report the synthesis of a 11C-labeled TAAR1 high-affinity antagonist N-(3-methoxyphenyl)-6-(pyrrolidin-1-yl)-5-(trifluoromethyl)nicotinamide [11C]4 (also named [11C]TAAR1-1911), as well as its physicochemical and preclinical evaluations for positron emission tomography (PET) imaging. This PET ligand was afforded using [11C]CH3I with the base NaOH in good radiochemical yield (non-decay corrected 14% relative to starting [11C]CO2), excellent radiochemical purities (> 99%) and high molar activities (> 37 GBq/µmol). Despite promising in vitro performance characteristics, [11C]4 did not exhibit in vivo specificity, potentially owing to fast metabolic degradation. Further studies are warranted to identify a suitable TAAR1 PET tracer, which would ultimately aid the development of TAAR1-directed therapeutic agents. | |||||
| 書誌情報 |
Tetrahedron Letters 巻 70, p. 153007, 発行日 2021-03 |
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| 出版者 | ||||||
| 出版者 | ELSEVIER | |||||
| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 0040-4039 | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | 10.1016/j.tetlet.2021.153007 | |||||
| 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/S0040403921002033 | |||||
