WEKO3
アイテム
Radiosynthesis and preliminary evaluation of 4-[18F]fluoro-N-[4-[6-(isopropylamino) pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide as a new positron emission tomography ligand for metabotropic glutamate receptor subtype 1
https://repo.qst.go.jp/records/46088
https://repo.qst.go.jp/records/4608885c55848-6588-4716-b223-1a10dae6a132
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2011-06-02 | |||||
| タイトル | ||||||
| タイトル | Radiosynthesis and preliminary evaluation of 4-[18F]fluoro-N-[4-[6-(isopropylamino) pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide as a new positron emission tomography ligand for metabotropic glutamate receptor subtype 1 | |||||
| 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 |
Yamasaki, Tomoteru
× Yamasaki, Tomoteru× Fujinaga, Masayuki× Yoshida, Yuichiro× Kumata, Katsushi× Yui, Joji× Kawamura, Kazunori× Hatori, Akiko× Fukumura, Toshimitsu× Zhang, Ming-Rong× 山崎 友照× 藤永 雅之× 吉田 勇一郎× 熊田 勝志× 由井 譲二× 河村 和紀× 羽鳥 晶子× 福村 利光× 張 明栄 |
|||||
| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | The purpose of this study was to develop 4-[18F]fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide ([18F]FITM, [18F]4) as a new PET ligand for imaging metabotropic glutamate receptor subtype 1 (mGluR1). [18F]4 was synthesized by [18F]fluorination of a novel nitro precursor 3 with [18F]KF in the presence of Kryptofix 222. At the end of synthesis, 429-936 MBq (n = 8) of [18F]4 was obtained with >99% radiochemical purity and 204-559 GBq/mumol specific activity starting from 6.7 to 13.0 GBq of [18F]F;. The brain distribution of [18F]4 was determined by the in vitro and ex vivo autoradiography using rat brain sections. The in vitro and in vivo specific binding of [18F]4 to mGluR1 was detected in the cerebellum, thalamus, hippocampus, and striatum. These results suggest that [18F]4 is a promising PET ligand for the in vivo evaluation of mGluR1. | |||||
| 書誌情報 |
Bioorganic & Medicinal Chemistry Letters 巻 21, 号 10, p. 2998-3001, 発行日 2011-05 |
|||||
| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 0960-894X | |||||
