Methoxy- and Fluorine-Substituted Analogs of O-1302 : Synthesis and in Vitro Binding Affinity for the CB1 Cannabinoid Receptor
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概要
- 論文の詳細を見る
Methoxy and fluorine analogs substituted on the terminal carbon of the pentyl chain of N-(piperidinyl)-1-(2,4-dichlorophenyl)-4-methyl-5-(4-pentylphenyl)-1H-pyrazole-3-carboxamide (O-1302) were synthesized in a multi-step process from 5-phenyl-1-pentanol, which was based on the 1,5-diarylpyrazole core template of N-(piperidinyl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716) through condensation of the respective amine with pyrazole carboxylic acid, in order to develop tracers for medical imaging. Their potency for inhibiting the binding of the CB1 antagonist [^3H]SR141716 was evaluated with the aim of developing positron emission tomography (PET) ligands for the cerebral cannabinoid CB1 receptor. These analogs bearing a piperidinyl carboxamide at the C_3 of the pyrazole ring exhibited affinities comparable to those of the CB1 reference antagonist SR141716, which warrants further investigation using the radiolabeled form for biological imaging studies. A morpholine ring substituted at the C_3 of the pyrazole ring resulted in a reduction of the CB1 affinity.
- 社団法人日本薬学会の論文
- 2007-08-01
著者
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ISHIWATA Kiichi
Positron Medical Center, Tokyo Metropolitan Institute of Gerontology
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Murakami T
Kyoto Univ. Kyoto
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Ishiwata K
Positron Medical Center Tokyo Metropolitan Institute Of Gerontology
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Ishiwata Kiichi
東京都老人総合研究所ポジトロン医学研究施設
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Ishii Kenji
東京都老人総合研究所ポジトロン医学研究施設
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Ishiwata Kiichi
Positron Medical Center Tokyo Metropolitan Institute Of Gerontology
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Ishiwata Kiichi
筑波大学陽子線医学利用研究センター
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Ishii Kenji
Positron Medical Center Tokyo Metropolitan Institute Of Gerontology
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Murakami T
National Inst. Advanced Industrial Sci. And Technol. Ibaraki
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MUKAI Takahiro
Graduate School of Biomedical Sciences, Nagasaki University
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Tomonari Masahide
参天製薬奈良研究開発センター
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Mukai T
九州大学 大学院薬学研究院
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Mukai Takahiro
Graduate School Of Pharmaceutical Sciences Kyushu University
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Mukai Takahiro
京都大学 薬学研究科病態機能分析学
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Mukai Takahiro
Graduate School Of Medicine Kyoto University
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NOJIRI Yumiko
Graduate School of Pharmaceutical Sciences, Kyushu University
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TOBIISHI Shintaro
Graduate School of Pharmaceutical Sciences, Kyushu University
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SASADA Toru
Positron Medical Center, Tokyo Metropolitan Institute of Gerontology
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YAMAMOTO Fumihiko
Graduate School of Pharmaceutical Sciences, Kyushu University
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MAEDA Minoru
Graduate School of Pharmaceutical Sciences, Kyushu University
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SASADA Toru
Graduate School of Pharmaceutical Sciences, Kyushu University
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Sasada Toru
Positron Medical Center Tokyo Metropolitan Institute Of Gerontology
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Ishii K
Positron Medical Center Tokyo Metropolitan Institute Of Gerontology
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Mori Tomohiko
Institute Of Biomaterials And Bioengineering Tokyo Medical And Dental University
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Ishii Kentaro
Department Of Radiology Osaka City University Graduate School Of Medicine
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Nojiri Yumiko
Graduate School Of Pharmaceutical Sciences Kyushu University
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Ishii Katsumi
Department Of Radiology Kitasato University School Of Medicine
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Ishii Keizo
Tohoku Univ. Miyagi Jpn
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Tobiishi Shintaro
Graduate School Of Pharmaceutical Sciences Kyushu University
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Maeda Minoru
Optical Measurement Technology Development Co. Ltd.
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Maeda Minoru
Graduate School Of Pharmaceutical Sciences Kyushu University
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Yamamoto Fumihiko
Graduate School Of Pharmaceutical Sciences Kyushu University:crest Japan Sceicne And Technology Corp
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Yamamoto Fumihiko
Graduate School Of Pharmaceutical Sciences Kyushu University
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Ishii K
Department Of Radiology Osaka City University Graduate School Of Medicine
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Maeda M
Graduate School Of Pharmaceutical Sciences Kyushu University
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Mukuno Takashi
The Graduate School Of National Science And Technology Okayama University
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Ishikawa Kinya
Department Of Neurology Postgraduate School Of Medicine Tokyo Medical And Dental University
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Ishii Kenji
Pet Center Tokyo Metropolitan Institute Of Gerontology
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Maeda Minoru
Graduate School Of Pharmaceutical Sciences Kyushu Univ.
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Yamamoto Fumihiko
Graduate School Of Pharmaceutical Sciences Kyushu Univ.
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Yamamoto Fumihiko
Graduate School of Pharmaceutical Sciences
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Maeda Minoru
Graduate School of Pharmaceutical Sciences
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