Synthesis and Evaluation of Novel 2-Oxo-1, 2-dihydro-3-quinolinecarboxamide Derivatives as Potent and Selective Serotonin 5-HT_4 Receptor Agonists
スポンサーリンク
概要
- 論文の詳細を見る
A series of 8'-substituted N-(endo-8-azabicyclo[3. 2. 1]oct-3-yl)-1-isopropyl-2-oxo-1, 2-dihydro-3-quinolinecarboxamides were synthesized. The 5-HT_4 receptor agonistic activity was evaluated using the isolated guinea pig ileum preparation. Of the compounds synthesized, N-(endo-8-(3-hydroxypropyl)-8-azabicyclo[3. 2. 1]oct-3-yl)-1-isopropyl-2-oxo-1, 2-dihydro-3-quinolinecarboxamide(15a, TS-951)exhibited the most potent serotonin 5-HT_4 receptor agonistic activity. This compound had a high affinity for the serotonin 5-HT_4 receptor although it had no affinities for other broad spectrum receptors. Furthermore, it remarkably enhanced gastrointestinal motility in conscious fed dogs without unfavorable effects that non-selective serotonin 5-HT_4 receptor agonist has. TS-951 may be useful in improving gastrointestinal dysfunction.
- 公益社団法人日本薬学会の論文
- 2001-01-01
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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