Succinimide Derivatives. II. Synthesis and Antipsychotic Activity of N-[4-[4-(1,2-Benzisothiazol-3-yl)-1-piperazinyl]butyl]-1,2-cis-cyclohexanedicarboximide (SM-9018) and Related Compounds
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概要
- 論文の詳細を見る
Cyclic imides bearing ω-(4-benzisothiazol-3-yl-1-piperazinyl)alkyl moieties were synthesized and tested for antipsychotic activity. The in vitro binding affinities of these compounds were examined for dopamine 2 (D_2) and serotonin 2 (5-HT_2) receptor sites. Structure-activity relationships within these series are discussed. One of these compounds, N-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]butyl]-1,2-cis-cyclohexanedicarboximide (SM-9018), was found to be more potent and more selective in vivo than tiospirone in its antipsychotic activity. SM-9018 (17) is currently undergoing clinical evaluation as a selective antipsychotic agent.
- 公益社団法人日本薬学会の論文
- 1995-12-15
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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佐治 幾太郎
Sumitomo Pharmaceuticals Research Center
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吉儀 真弓
Sumitomo Pharmaceuticals Research Center
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Kojima A
Research Center Sumitomo Pharmaceuticals Co. Ltd
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