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[11C]CEP-32496: radiosynthesis, biodistribution and PET study of brain uptake in P-gp/Bcrp knockout mice
https://repo.qst.go.jp/records/47035
https://repo.qst.go.jp/records/4703552e680f5-bc42-407c-8084-99372408cdde
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2015-02-04 | |||||
| タイトル | ||||||
| タイトル | [11C]CEP-32496: radiosynthesis, biodistribution and PET study of brain uptake in P-gp/Bcrp knockout mice | |||||
| 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 |
Shimoda, Yoko
× Shimoda, Yoko× Yui, Joji× Fujinaga, Masayuki× Xie, Lin× Kumata, Katsushi× Yamasaki, Tomoteru× Hatori, Akiko× Ogawa, Masanao× Kawamura, Kazunori× Zhang, Ming-Rong× 下田 陽子× 由井 譲二× 藤永 雅之× 謝 琳× 熊田 勝志× 山崎 友照× 羽鳥 晶子× 小川 政直× 河村 和紀× 張 明栄 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | CEP-32496 is a novel, orally active serine/threonine-protein kinase B-raf (BRAF) (V600E) kinase inhibitor that is being investigated in clinical trials for the treatment of some cancers in patients. In this study, we developed [11C-carbonyl]CEP-32496 as a novel positron emission tomography (PET) probe to study its biodistribution in the whole bodies of mice. [11C]CEP-32496 was synthesized by the reaction of 5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-amine hydrochloride (1·HCl) with [11C]phosgene, followed by treatment with 3-(6,7-dimethoxyquinozolin-4-yloxy)aniline (2). Small-animal PET studies with [11C]CEP-32496 indicated that radioactivity levels (AUC0–90 min, SUV × min) accumulated in the brains of P-gp/BCRP knockout mice at a 8-fold higher rate than in the brains of wild-type mice. | |||||
| 書誌情報 |
Bioorganic & Medicinal Chemistry Letters 巻 24, 号 15, p. 3574-3577, 発行日 2014-06 |
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| 出版者 | ||||||
| 出版者 | Elsevier | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | doi:10.1016/j.bmcl.2014.05.045 | |||||
