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Synthesis and Evaluation of Novel Radioligands for Positron Emission Tomography Imaging of Metabotropic Glutamate Receptor Subtype 1 (mGluR1) in Rodent Brain
https://repo.qst.go.jp/records/46323
https://repo.qst.go.jp/records/463238c78d5c6-5758-4dee-890b-86f04dce7710
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2012-05-14 | |||||
| タイトル | ||||||
| タイトル | Synthesis and Evaluation of Novel Radioligands for Positron Emission Tomography Imaging of Metabotropic Glutamate Receptor Subtype 1 (mGluR1) in Rodent Brain | |||||
| 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 |
Fujinaga, Masayuki
× Fujinaga, Masayuki× Yamasaki, Tomoteru× Yui, Joji× Hatori, Akiko× Xie, Lin× Kawamura, Kazunori× Asakawa, Chiharu× Kumata, Katsushi× Yoshida, Yuichiro× Ogawa, Masanao× Nengaki, Nobuki× Fukumura, Toshimitsu× Zhang, Ming-Rong× 藤永 雅之× 山崎 友照× 由井 譲二× 羽鳥 晶子× 謝 琳× 河村 和紀× 浅川 千春× 熊田 勝志× 吉田 勇一郎× 小川 政直× 念垣 信樹× 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 | We designed three novel positron emission tomography ligands, N-(4-(6-(isopropylamino)pyrimidin-4-yl)-1,3- thiazol-2-yl)-4-[11C]methoxy-N-methylbenzamide ([11C]6), 4-[18F]fluoroethoxy-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3- thiazol-2-yl]-N-methylbenzamide ([18F]7), and 4-[18F]fluoropropoxy-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]- N-methylbenzamide ([18F]8), for imaging metabotropic glutamate receptor type 1 (mGluR1) in rodent brain. Unlabeled compound 6 was synthesized by benzoylation of 4-pyrimidinyl-2-methylaminothiazole 10, followed by reaction with isopropylamine. Removal of the methyl group in 6 gave phenol precursor 12 for radiosynthesis. Two fluoroalkoxy analogues 7 and 8 were prepared by reacting 12 with tosylates 13 and 14. Radioligands [11C]6, [18F]7, and [18F]8 were synthesized by O-[11C]methylation or [18F]fluoroalkylation of 12. Compound 6 showed high in vitro binding affinity for mGluR1, whereas 7 and 8 had weak affinity. Autoradiography using rat brain sections showed that [11C]6 binding is aligned with the reported distribution of mGluR1 with high specific binding in the cerebellum and thalamus. PET study with [11C]6 in rats showed high brain uptake and a similar distribution pattern to that in autoradiography, indicating the usefulness of [11C]6 for imaging brain mGluR1. |
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| 書誌情報 |
Journal of Medicinal Chemistry 巻 55, 号 5, p. 2342-2352, 発行日 2012-02 |
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| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 0022-2623 | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | 10.1021/jm201590g | |||||
