Synthesis and Evaluation of Novel 2-Oxo-1,2-dihydro-3-quinolinecarboxamide Derivatives as Serotonin 5-HT_4 Receptor Agonists
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概要
- 論文の詳細を見る
A series of N-azabicycloalkyl-1-alkyl-2-oxo-1,2-dihydro-3-quinolinecarboxamides were synthesized and tested for serotonin 5-HT_4 receptor-stimulating effects in the regulation of electrically-evoked contraction in guinea pig muscle. Among them, N-azabicycloalkyl-1-isopropyl-2-oxo-1,2-dihydro-3-quinolinecarboxamide (8c, 9c, 10c, 11c, 12c) exhibited potent serotonin 5-HT_4 receptor-stimulating activity. The most potent compound, N-(endo-8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-1-isopropyl-2-oxo-1,2-dihydro-3-quinolinecarboxamide (8c, ED_<50>=36.3 nM), was seven times as active as cisapride, while 8c had no affinity for 5-HT_<1A>, 5-HT_<1D>, D_2,muscarinic M_2 or muscarinic M_3 receptors even at 10μM. Compound 8c stimulated digestive tract motility in conscious fed dogs (1.0 mg/kg p.o.).
- 公益社団法人日本薬学会の論文
- 2000-12-01
著者
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井藤 千裕
名城大学薬学部薬化学
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Isobe Y
Research Division Discovery Research Laboratories Ii Sumitomo Pharmaceuticals Co. Ltd.
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Kaneko Tetsuo
Department Of Pharmaceutical Science Hiroshima International University
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SUZUKI MASUKO
Tohoku College of Pharmacy
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Isobe Y
Japan Energy Corp. Saitama Jpn
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MURAMATSU MAKOTO
Research Center, Taisho Pharmaceutical Co., Ltd.
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五十部 穣
Research Center Sumitomo Pharmaceuticals Co. Ltd.
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SUZUKI Masaji
Research Center Taisho Pharmaceutical Co., Ltd.
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OHUCHI Yutaka
Research Center Taisho Pharmaceutical Co., Ltd.
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ASANUMA Hajime
Research Center Taisho Pharmaceutical Co., Ltd.
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KANEKO Toshie
Research Center Taisho Pharmaceutical Co., Ltd.
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YOKOMORI Sadakazu
Research Center Taisho Pharmaceutical Co., Ltd.
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ITO Chika
Research Center Taisho Pharmaceutical Co., Ltd.
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ISOBE Yoshihiko
Research Center Taisho Pharmaceutical Co., Ltd.
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Suzuki Masuko
Department Of Microbiology Tohoku Pharmaceutical University
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Suzuki M
Unit Of Chemistry Faculty Of Engineering And High Technology Research Center Kansai University
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Kaneko T
Department Of Pharmaceutical Science Hiroshima International University
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Suzuki M
Faculty Of Pharmaceutical Sciences Toyama Medical And Pharmaceutical University
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Yokomori S
Medicinal Research Laboratories Taisho Pharmaceutical Co. Ltd.
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Ohuchi Y
Research Center Taisho Pharmaceutical Co. Ltd.
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Asanuma Hajime
Research Center Taisho Pharmaceutical Co. Ltd.
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Muramatsu M
Research Center Taisho Pharmaceutical Co. Ltd.
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Muramatsu Makoto
Research Center Taisho Pharmaceutical Co. Ltd.
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