Synthesis and Anxiolytic Activity of N-Substituted Cyclic Imides (1R^*, 2S^*, 3R^*, 4S^*)-N-[4-[4-(2-Pyrimidinyl)-1-piperazinyl]butyl]-2,3-bicyclo[2.2.1]heptanedicarboximide (Tandospirone) and Related Compounds
スポンサーリンク
概要
- 論文の詳細を見る
A series of cyclic imides bearing a ω-(4-aryl and 4-heteroaryl-1-piperazinyl)alkyl moieties was synthesized and tested in vivo for anxiolytic activity. The in vitro binding affinities of these compounds were also examined for 5-HT_<1A> receptor sites. Structure-activity relationships within these series are discussed. One of these compounds, (1R^*, 2S^*, 3R^*, 4S^*)-N-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-2,3-bicyclo[2.2.1]heptanedicarboximide (1 : tandospirone), was found to be equipotent with buspirone in its anxiolytic activity and more anxio-selective than buspirone and diazepam. Tandospirone (1) is currently undergoing clinical evaluation as a selective anxiolytic agent.
- 公益社団法人日本薬学会の論文
- 1991-09-25
著者
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Antoku F
Sumitomo Pharmaceuticals Research Center
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安徳 富士雄
Sumitomo Pharmaceuticals Research Center
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石墨 紀久夫
Sumitomo Pharmaceuticals Research Center
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小島 淳之
Sumitomo Pharmaceuticals Research Center
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石墨 紀久夫
Research Laboratories, Sumitomo Pharmaceuticals Co.,
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小島 淳之
Research Laboratories, Sumitomo Pharmaceuticals Co.,
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安徳 富士雄
Research Laboratories, Sumitomo Pharmaceuticals Co.,
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Kojima A
Research Center Sumitomo Pharmaceuticals Co. Ltd
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小島 淳之
Research Center, Sumitomo Pharmaceuticals Co., Ltd
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