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[11C]Sorafenib: Radiosynthesis and preliminary PET study of brain uptake in P-gp/Bcrp knockout mice
https://repo.qst.go.jp/records/46041
https://repo.qst.go.jp/records/4604154ae55a0-f145-453c-9869-f2a01f3357ac
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2011-05-20 | |||||
| タイトル | ||||||
| タイトル | [11C]Sorafenib: Radiosynthesis and preliminary 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 |
Asakawa, Chiharu
× Asakawa, Chiharu× Ogawa, Masanao× Kumata, Katsushi× Fujinaga, Masayuki× Kato, Koichi× Yamasaki, Tomoteru× Yui, Joji× Kawamura, Kazunori× Hatori, Akiko× Fukumura, Toshimitsu× Zhang, Ming-Rong× 浅川 千春× 小川 政直× 熊田 勝志× 藤永 雅之× 加藤 孝一× 山崎 友照× 由井 譲二× 河村 和紀× 羽鳥 晶子× 福村 利光× 張 明栄 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Sorafenib (Nexavar, BAY43-9006, 1) is a second-generation, orally active multikinase inhibitor that is approved for the treatment of some cancers in patients. In this Letter, we developed [11C]1 as a novel positron emission tomography (PET) probe, and evaluated the influence of ABC transporters-mediated efflux on brain uptake using PET with [11C]1 in P-glycoprotein (P-gp)/breast cancer resistance protein (Bcrp) knockout mice versus wild-type mice. [11C]1 was synthesized by the reaction of hydrochloride of aniline 2 with [11C]phosgene ([11C]COCl2) to give isocyanate [11C]6, followed by reaction with another aniline 3. Small-animal PET study with [11C]1 indicated that the radioactivity level (AUC0–60 min, SUV x min) in the brains of P-gp/Bcrp knockout mice was about three times higher than in wild-type mice. |
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| 書誌情報 |
Bioorganic & Medicinal Chemistry Letters 巻 21, 号 8, p. 2220-2223, 発行日 2011-04 |
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| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 0960-894X | |||||
