Synthesis of Novel Succinamide Derivatives Having the 5,11-Dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one Skeleton as Potent and Selective M_2 Muscarinic Receptor Antagonists. I
スポンサーリンク
概要
- 論文の詳細を見る
A series of 5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one derivatives containing the succinamide skeleton has been synthesized and evaluated for M_1,M_2 and M_3 muscarinic receptor binding affinities (in vitro) and M_2 and M_3 muscarinic receptor antagonistic activities (in vivo). Some of them showed higher and more selective binding affinities for M_2 muscarinic receptors than that of AF_DX 116. Among them, 11-[3-[N-[2-(N-benzyl-N-methylamino)ethyl]-N-ethylcarbamoyl]propiony]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one (68) was found to be the most potent and selective M_2 muscarinic receptor antagonist in vitro. This compound also strongly inhibited the oxotremorine-induced bradycardia after intravenous administration and showed 130-fold selectivity for M_2 muscarinic receptors over M_3 muscarinic receptors in vivo.
- 公益社団法人日本薬学会の論文
- 1997-06-15
著者
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Takizawa Kayoko
Research Center for Pathogenic Fungi and Microbial Toxicoses, Chiba University
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渡辺 敏子
School Of Pharmaceutical Sciences Toho University
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Shibata Hiroko
Laboratory Of Pharmaceutical Proteomics National Institute Of Biomedical Innovation (nibio)
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Shibata Hiroko
医薬基盤研究所 創薬プロテオミクスプロジェクト
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SHIBATA Hiroshi
Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.
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Okazaki T
Yamanouchi Pharmaceutical Co. Ltd. Ibaraki Jpn
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Okazaki Toshio
Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.
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Watanabe Toshifumi
Pharmaceutical Research Laboratories Ii Pharmaceutical Research Division Takeda Chemical Industries
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Yanagisawa I
Yamanouchi Pharmaceutical Co. Ltd. Ibaraki Jpn
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Yanagisawa Isao
Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co.
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Yanagisawa Isao
山之内製薬
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Takizawa Kayoko
Res. Center For Pathogenic Fungi And Microbial Toxicoses Chiba Univ.
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Watanabe T
Chiba Univ. Chiba Jpn
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Shibata Hiroshi
Laboratory For Health Care Science Research Center Suntory Ltd.
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Watanabe Toshiko
Faculty Of Pharmaceutical Sciences Chiba University
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Watanabe Toshiko
Graduate School Of Pharmaceutical Sciences Chiba University
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Watanabe Toshihiro
Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.
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Shibata H
Laboratory For Health Care Science Research Center Suntory Ltd.
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Takizawa K
Res. Center For Pathogenic Fungi And Microbial Toxicoses Chiba Univ.
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Takizawa Kenji
Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.
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KAKEFUDA Akio
Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.,
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KINOYAMA Isao
Institute for Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.,
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HIRANO Seiko
Institute for Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.,
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Hirano S
The Nukada Institute For Medical And Biological Research
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Kinoyama Isao
Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co.
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Kakefuda Akio
Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.
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Shibata Hiroshi
Institute Of Health Care Science Suntory Wellness Limited
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Shibata Hiroshi
Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.:department Of Animal Scienc
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SHIBATA Hiroshi
Institute for Biomedical Research, Suntory Limited
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