Synthesis and Brain Regional Distribution of [^<11>C]NPS 1506 in Mice and Rat: an N-Methyl-D-aspartate (NMDA) Receptor Antagonist(Medicinal Chemistry)

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概要

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• NPS 1506 [3-fluoro-γ-(3-fluorophenyl)-N-methylbenzenepropamine] is representative of a non-psychoto-mimetic class of N-methyl-D-aspartate (NMDA) receptor antagonists. [^<11>C]NPS 1506 was prepared at high radiochemical purity (>98%) with a specific activity of around 50 GBq/μmol at the end of synthesis by methylation of the desmethyl precursor with [^<11>C]methyl iodide in the presence of NaH. Biodistribution of [^<11>C]NPS 1506 in mice and rat demonstrated that uptake into the brain was rapid and occurred at high levels. [^<11>C]NPS 1506 showed no appreciable specific binding in rodent brains under in vivo conditions, possibly because of both a large non-specific bound fraction and low in vitro binding affinity for NMDA receptors.

• 社団法人日本薬学会の論文
• 2003-11-01

著者

• Fuchigami Takeshi

  Graduate School Of Pharmaceutical Sciences Kyushu University

• Fuchigami Takeshi

  九州大学 薬学研究院

• 鈴木 和美

  Showa College of Pharmaceutical Sciences

• 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

• Suzuki Kazutoshi

  Molecular Imaging Center National Institute Of Radiological Sciences

• YAMAMOTO Fumihiko

  Graduate School of Pharmaceutical Sciences, Kyushu University

• MAEDA Minoru

  Graduate School of Pharmaceutical Sciences, Kyushu University

• Suzuki K

  Pharmaceutical Frontier Research Laboratories Japan Tobacco Inc.

• Arai Takayuki

  Department Of Chemistry Faculty Of Engineering Gunma University

• Suhara Tetsuya

  Brain Imaging Project National Institute Of Radiological Sciences

• Suhara Tetsuya

  Clinical Neuroimaging Section Department Of Molecular Neuroimaging Molecular Imaging Center National

• Suzuki Kenji

  Suntory Institute For Biomedical Research Wakayamadai

• Suzuki K

  Noda Research Laboratories Drug Delivery System Institute Ltd.:(present Address)pharmaceutics Resear

• MAEDA Jun

  Molecular Imaging Center, National Institute of Radiological Sciences

• SASAKI Shigeki

  Graduate School of Pharmaceutical Sciences, Kyushu University

• HARADAHIRA Terushi

  Department of Medical Imaging, National Institute of Radiological Sciences

• ARAI Takuya

  Department of Medical Imaging, National Institute of Radiological Sciences

• OKAUCHI Takashi

  Brain Imaging Project, National Institute of Radiological Sciences

• MAEDA Jun

  Brain Imaging Project, National Institute of Radiological Sciences

• SUZUKI Kazutoshi

  Department of Medical Imaging, National Institute of Radiological Sciences

• 佐々木 茂貴

  Faculty Of Pharmaceutical Sciences Kyushu University

• Sasaki Shigeki

  Graduate School Of Pharmaceutical Sciences Kyushu University

• Maeda J

  Molecular Imaging Center National Institute Of Radiological Sciences

• Kato Shingo

  Research Center Hospital For Charged Particle Therapy National Institute Of Radiological Sciences

• 岡内 隆

  Molecular Imaging Center National Institute Of Radiological Sciences

• Suzuki Kazutoshi

  Department Of Medical Imaging National Institute Of Radiological Sciences

• Suzuki Kazutoshi

  Clinical Neuroimaging Section Department Of Molecular Neuroimaging Molecular Imaging Center National

• Maeda Minoru

  Optical Measurement Technology Development Co. Ltd.

• Maeda Minoru

  Graduate School Of Pharmaceutical Sciences Kyushu University

• Yamamoto Fumihiko

  Graduate School Of Pharmaceutical Sciences Kyushu University:crest Japan Sceicne And Technology Corp

• Yamamoto Fumihiko

  Graduate School Of Pharmaceutical Sciences Kyushu University

• Suzuki K

  Molecular Imaging Center National Institute Of Radiological Sciences

• Maeda M

  Graduate School Of Pharmaceutical Sciences Kyushu University

• Maeda M

  Tokyo Tanabe Co. Ltd. Tokyo Jpn

• Arai T

  Department Of Medical Imaging National Institute Of Radiological Sciences:crest Japan Science And Te

• Arai Takuya

  Department Of Chemistry For Materials Graduate School Of Engineering Mie University

• Haradahira T

  Molecular Neuroimaging Group Molecular Imaging Center National Institute Of Radiological Sciences

• Maeda Minoru

  Graduate School Of Pharmaceutical Sciences Kyushu Univ.

• Yamamoto Fumihiko

  Graduate School Of Pharmaceutical Sciences Kyushu Univ.

• Yamamoto Fumihiko

  Graduate School of Pharmaceutical Sciences

• Maeda Minoru

  Graduate School of Pharmaceutical Sciences

• SUZUKI Kazutoshi

  Department of Hospital Pharmacy, Keio University School of Medicine

• Fuchigami Takeshi

  Graduate School of Biomedical Sciences, Nagasaki University

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