New 5-HT_3 (Serotonin-3) Receptor Antagonists. IV. Synthesis and Structure-Activity Relationships of Azabicycloalkaneacetamide Derivatives
スポンサーリンク
概要
- 論文の詳細を見る
The synthesis and structure-activity relationships of a series of new azabicycloalkanes as 5-HT_3 (serotonin-3) receptor antagonists are described. Our study on the azabicycloalkaneacetamide derivatives showed that 2,3-dihydroindole as the aromatic ring moiety afforded potent 5-HT_3 receptor antagonist activity, as judged by blockade of bradycardia induced by i.v. injection of 2-methylserotonin in anesthetized rats. 7-Azaindole as the aromatic moiety afforded weak 5-HT_3 receptor antagonists activity. The best 5-HT_3 antagonists in this study were endo-3,3-diethyl- (9k) and 3,3-dimethyl-2,3-dihydro-1-[(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)acetyl-1H-indole (9d), being approximately 10-fold more potent than ondansetron (1). This study shows that the azabicycloalkaneacetyl group is a new pharmacophoric element as a basic nitrogen and a linking carbonyl moiety.
- 社団法人日本薬学会の論文
- 1995-08-15
著者
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伊藤 清隆
New Drug Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
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高杉 寿
New Drug Research Laboratories Fujisawa Pharmaceutical Co., Ltd.,
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西野 重孝
New Drug Research Laboratories
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高杉 寿
New Drug Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
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加藤 眞行
New Drug Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
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加藤 昌子
Div. Of Chemistry Fac. And Graduate School Of Sci. Hokkaido Univ.
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山国 尚志
New Drug Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.,
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Takasugi H
New Drug Research Laboratories Fujisawa Pharmaceutical Co. Ltd
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Takasugi H
New Drug Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
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西野 重孝
New Drug Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
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Nishino S
Fujisawa Pharmaceutical Co. Ltd. Osaka Jpn
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山国 尚志
New Drug Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
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Kato M
Department Of Pharmacotherapeutics Showa Pharmaceutical University
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Kako M
Suzuka Univ. Medical Sci. And Technol. Mie Jpn
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