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Radiosynthesis of [13N]dantrolene, a positron emission tomography probe for breast cancer resistant protein, using no-carrier-added [13N]ammonia
https://repo.qst.go.jp/records/46274
https://repo.qst.go.jp/records/462740cd1d252-5298-4e0a-827f-f0a968deeb44
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2012-02-24 | |||||
| タイトル | ||||||
| タイトル | Radiosynthesis of [13N]dantrolene, a positron emission tomography probe for breast cancer resistant protein, using no-carrier-added [13N]ammonia | |||||
| 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× Ogawa, Masanao× Takei, Makoto× Fujinaga, Masayuki× Yoshida, Yuichirou× Nengaki, Nobuki× Fukumura, Toshimitsu× Suzuki, Kazutoshi× Zhang, Ming-Rong× 熊田 勝志× 小川 政直× 藤永 雅之× 吉田 勇一郎× 念垣 信樹× 福村 利光× 鈴木 和年× 張 明栄 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Dantrolene (1) is a substrate for breast cancer resistant protein, which is widely distributed in the blood–brain-barrier, intestine, gall bladder, and liver. PET study with 1 labeled with a positron emitter can be used to visualize BCRP and to elucidate the effect of BCRP on the pharmacokinetics of drugs. The objective of this study was to label 1 using nitrogen-13 (13N, a positron emitter; half-life:9.9 min). Using no-carrier-added [13N]NH3 as the labeling agent, we synthesized [13N]dantrolene ([13N]1) for the first time. The reaction of carbomyl chloride 2b with [13N]NH3 gave an unsymmetrical urea [13N]3, followed by cyclization of [13N]3 to afford [13N]1. Due to its instability, 2b was prepared in situ by treating amine 5 with triphosgene in a ratio of 4 to 1 and used for subsequent [13N]ammonolysis without purification. |
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| 書誌情報 |
Bioorganic & Medicinal Chemistry 巻 20, 号 1, p. 305-310, 発行日 2012-01 |
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| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 0968-0896 | |||||
