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A Prodrug of NMDA/Glycine Site Antagonist, L-703,717, with Improved BBB Permeability: 4-Acetoxy Derivative and Its Positron-Emitter Labeled Analog
https://repo.qst.go.jp/records/44311
https://repo.qst.go.jp/records/4431115286221-374a-4607-8d42-f25c7e2074a4
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2006-06-21 | |||||
| タイトル | ||||||
| タイトル | A Prodrug of NMDA/Glycine Site Antagonist, L-703,717, with Improved BBB Permeability: 4-Acetoxy Derivative and Its Positron-Emitter Labeled Analog | |||||
| 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 |
Haradahira, Terushi
× Haradahira, Terushi× Zhang, Ming-Rong× Maeda, Jun× Okauchi, Takashi× Kida, Takayo× Kawabe, Koichi× Sasaki, Shigeki× Suhara, Tetsuya× Suzuki, Kazutoshi× 原田平 輝志× 張 明栄× 前田 純× 岡内 隆× 佐々木 茂貴× 須原 哲也× 鈴木 和年 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | 4-Acetoxy derivative(1) of L-703,717, a high-affinity (IC50=4.5nM) antagonist for the glycine site of NMDA receptors, was synthesized and its brain uptake was examined using a carbon-11 labeled analog ([11C]1).Initial radioactivity in the brain after intravenous injection of [11C]1 was a 2-fold that of [11C]L-703,717in mice.Rapid bioconversion of[11C]1 into [11C]L-703,717 was demonstrated by metabolite analyses of rat brain after [11C]1 injection. Ex vivo autoradiography of [11C]1 in rat brain showed the same cerebellar localization of radioactivity as [11C]L-703,717.These results indicate that 1 is a promising pharmacological tool as a prodrug of L-703,717 with improved BBB permeability. | |||||
| 書誌情報 |
Chemical & Pharmaceutical Bulletin 巻 49, 号 2, p. 147-150, 発行日 2001 |
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| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 0009-2363 | |||||
