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[11C]BCTC: Radiosynthesis and In Vivo Binding to Transient Receptor Potential Vanilloid Subfamily Member 1 (TRPV1) Receptor in the Mouse Trigeminal Nerve
https://repo.qst.go.jp/records/48390
https://repo.qst.go.jp/records/483900dc2d1b3-71bc-4c18-9492-e65d5d05cc33
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2017-11-30 | |||||
| タイトル | ||||||
| タイトル | [11C]BCTC: Radiosynthesis and In Vivo Binding to Transient Receptor Potential Vanilloid Subfamily Member 1 (TRPV1) Receptor in the Mouse Trigeminal Nerve | |||||
| 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 |
Kumata, Katsushi
× Kumata, Katsushi× Yui, Joji× Zhang, Yiding× Kurihara, Yusuke× Ogawa, Masanao× Mori, Wakana× Fujinaga, Masayuki× Zhang, Ming-Rong× 熊田 勝志× 由井 譲二× 張 一鼎× 栗原 雄祐× 小川 政直× 森 若菜× 藤永 雅之× 張 明栄 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | The purpose of this study was to synthesize a new positron emission tomography radiotracer, N-(4-tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine-1(2H)-[11C]carboxamide ([11C]BCTC, [11C]1), and assess its in vivo binding to the transient receptor potential vanilloid subfamily member 1 (TRPV1) receptor in mice. [11C]BCTC was synthesized by reacting the hydrochloride of 4-tertiarybutylaniline (2•HCl) with [11C]phosgene ([11C]COCl2) to give isocyanate [11C]4, followed by reaction with 4-(3-chloropyridin-2-yl)tetrahydropyrazine (3). [11C]BCTC was obtained at a 16–20% radiochemical yield, based on the cyclotron-produced [11C]CO2 (decay-corrected to the end of bombardment), with > 98% radiochemical purity and 65–110 GBq/μmol specific activity at the end of synthesis. An ex vivo biodistribution study in mice confirmed the specific binding of [11C]BCTC to TRPV1 in the trigeminal nerve, which is a tissue with high TRPV1 expression. | |||||
| 書誌情報 |
Bioorganic & Medicinal Chemistry Letters 巻 27, 号 19, p. 4521-4524, 発行日 2017-09 |
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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 | 0960-894X | |||||
| PubMed番号 | ||||||
| 識別子タイプ | PMID | |||||
| 関連識別子 | 28888821 | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | 10.1016/j.bmcl.2017.08.061 | |||||
