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Development of a 18F-Labelled Radiotracer with Improved Brain Kinetics for Positron Emission Tomography Imaging of Translocator Protein (18 kDa) in Ischemic Brain and Glioma
https://repo.qst.go.jp/records/48072
https://repo.qst.go.jp/records/4807260037185-eeef-49c1-a898-b252195679dd
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2017-06-21 | |||||
| タイトル | ||||||
| タイトル | Development of a 18F-Labelled Radiotracer with Improved Brain Kinetics for Positron Emission Tomography Imaging of Translocator Protein (18 kDa) in Ischemic Brain and Glioma | |||||
| 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 |
Fujinaga, Masayuki
× Fujinaga, Masayuki× Luo, Rui× Kumata, Katsushi× Zhang, Yiding× Hatori, Akiko× Yamasaki, Tomoteru× Xie, Lin× Mori, Wakana× Kurihara, Yusuke× Ogawa, Masanao× Nengaki, Nobuki× Wang, Feng× Ming-Rong, Zhang× Fujinaga, Masayuki× Kumata, Katsushi× Zhang, Yiding× Hatori, Akiko× Yamasaki, Tomoteru× Xie, Lin× Mori, Wakana× Kurihara, Yusuke× Ogawa, Masanao× Nengaki, Nobuki× Ming-Rong, Zhang |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | We designed four novel acetamidobenzoxazolone compounds 7a–d as candidates of positron emission tomography (PET) radiotracers for imaging translocator protein (18 kDa, TSPO) in ischemic brain and glioma. Among these compounds, 2-(5-(6-fluoropyridin-3-yl)-2-oxobenzo[d]oxazol-3(2H)-yl)-N-methyl-N-phenylacetamide (7d) exhibited high binding affinity (Ki = 13.4 nM) with TSPO and moderate lipophilicity (cLogD: 1.92). [18F]7d was radiosynthesized by [18F]fluorination of the bromopyridine precursor 7h with [18F]F- at 9 ± 3% radiochemical yield (n = 15, decay-corrected). In vitro autoradiography and PET studies for ischemic rat brains showed significantly increased binding with TSPO on the ipsilateral side compared to the contralateral side. PET with [18F]7d showed improved brain kinetics than our radiotracers developed until now. Metabolite study of [18F]7d showed 93% of unchanged form in the ischemic brain at 30 min after radiotracer injection. Moreover, PET study with [18F]7d provided a clear tumor image in a glioma-bearing rat model. We demonstrated that [18F]7d is a useful PET radiotracer for visualization of not only neuroinflammation but also glioma and will translate this radiotracer to “first-in-human” study in our facility. | |||||
| 書誌情報 |
Journal of Medicinal Chemistry 巻 60, 号 9, p. 4047-4061, 発行日 2017-04 |
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| 出版者 | ||||||
| 出版者 | ELSEVIER | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | 10.1021/acs.jmedchem.7b00374. | |||||
