A Prodrug of NMDA/Glycine Site Antagonist, L-703, 717, with Improved BBB Permeability : 4-Acetoxy Derivative and Its Positron-Emitter Labeled Analog
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概要
- 論文の詳細を見る
4-Acetoxy derivative(1)of L-703, 717, a high-affinity(IC_<50>=4.5nM)antagonist for the glycine site of NMDA receptors, was synthesized and its brain uptake was examined using a carbon-11 labeled analog(|^<11>C|1). Initial radioactivity in the brain after intravenous injection of |^<11>C|1 was a 2-fold that of |^<11>C|L-703, 717 in mice. Rapid bioconversion of |^<11>C|1 into |^<11>C|L-703, 717 was demonstrated by metabolite analyses of rat brain after |^<11>C|1 injection. Ex vivo autoradiography of |^<11>C|1 in rat brain showed the same cerebellar localization of radioactivity as |^<11>C|L-703, 717. These results indicate that 1 is a promising pharmacological tool as a prodrug of L-703, 717 with improved BBB permeability.
- 社団法人日本薬学会の論文
- 2001-02-01
著者
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鈴木 和美
Showa College of Pharmaceutical Sciences
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Suzuki Kazutoshi
放射線医学総合研究所分子イメージング研究センター
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Suzuki Kazutoshi
Molecular Imaging Center National Institute Of Radiological Sciences
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Suzuki K
Pharmaceutical Frontier Research Laboratories Japan Tobacco Inc.
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Suhara Tetsuya
Clinical Neuroimaging Section Department Of Molecular Neuroimaging Molecular Imaging Center National
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Suhara Tetsuya
Division Of Advanced Technology For Medical Imaging National Institute Of Radiological Sciences
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Suzuki Kenji
Suntory Institute For Biomedical Research Wakayamadai
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Suzuki K
Noda Research Laboratories Drug Delivery System Institute Ltd.:(present Address)pharmaceutics Resear
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MAEDA Jun
Molecular Imaging Center, National Institute of Radiological Sciences
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HARADAHIRA Terushi
Division of Advanced Technology for Medical Imaging, National Institute of Radiological Sciences
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ZHANG Ming-Rong
SHI Accelerator Service
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MAEDA Jun
SHI Accelerator Service
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OKAUCHI Takashi
SHI Accelerator Service
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KIDA Takayo
SHI Accelerator Service
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KAWABE Kouichi
Core Research for Evolution Science and Technology, Japan Science and Technology Corporation
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SASAKI Sigeki
Faculty of Pharmaceutical Sciences, Kyushu University
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SUZUKI Kazutoshi
Division of Advanced Technology for Medical Imaging, National Institute of Radiological Sciences
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佐々木 茂貴
Faculty Of Pharmaceutical Sciences Kyushu University
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Maeda J
Molecular Imaging Center National Institute Of Radiological Sciences
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岡内 隆
Molecular Imaging Center National Institute Of Radiological Sciences
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Suzuki Kazutoshi
Department Of Medical Imaging National Institute Of Radiological Sciences
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Suzuki Kazutoshi
Division Of Advanced Technology For Medical Imaging National Institute Of Radiological Sciences
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Suzuki Kazutoshi
Clinical Neuroimaging Section Department Of Molecular Neuroimaging Molecular Imaging Center National
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Suzuki K
Molecular Imaging Center National Institute Of Radiological Sciences
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Kawabe K
Core Research For Evolution Science And Technology Japan Science And Technology Corporation
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Kawabe Kouichi
Core Research For Evolution Science And Technology Japan Science And Technology Corporation
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Haradahira T
Molecular Neuroimaging Group Molecular Imaging Center National Institute Of Radiological Sciences
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