| 芳烷醇哌啶类化合物的合成及抗抑郁活性研究 |
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| 引用本文： | 郑永勇,高凯,翁志洁,李建其. 芳烷醇哌啶类化合物的合成及抗抑郁活性研究[J]. 药学学报, 2010, 45(3): 324-329 |
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| 作者姓名： | 郑永勇 高凯 翁志洁 李建其 |
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| 作者单位： | (1. 上海医药工业研究院创新药物与制药工艺国家重点实验室, 上海 200040; 2. 江苏惠中医药科技有限公司, 江苏 南京 210009) |
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| 基金项目： | 国家自然科学基金资助项目(30772623) |
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| 摘 要： | 为寻找新型具有抗抑郁活性的单胺递质再摄取抑制剂, 设计合成了15个芳烷醇哌啶类未见文献报道的新化合物, 结构经1H NMR及HR-MS分析确证。大鼠脑突触体对5-HT、NA和DA再摄取抑制作用体外活性测试结果表明, 化合物4、5和8对5-HT、NA和DA再摄取抑制作用较强。小鼠强迫游泳实验发现, 化合物4、5和13具有显著的体内抗抑郁效果, 化合物4和5值得进一步研究。
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| 关 键 词： | 芳烷醇哌啶类化合物 单胺递质再摄取抑制剂 合成 抗抑郁活性 |
Synthesis and antidepressant activities of aryl alkanol piperidine derivatives |
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| ZHENG Yong-yong,GAO Kai,WENG Zhi-jie,LI Jian-qi. Synthesis and antidepressant activities of aryl alkanol piperidine derivatives[J]. Acta pharmaceutica Sinica, 2010, 45(3): 324-329 |
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| Authors: | ZHENG Yong-yong GAO Kai WENG Zhi-jie LI Jian-qi |
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| Affiliation: | ZHENG Yong-yong1,GAO Kai2,WENG Zhi-jie1,LI Jian-qi1 (1. State Key Laboratory of New Drug , Pharmaceutical Process,Shanghai Institute of Pharmaceutical Industry,Shanghai 200040,China,2. Jiangsu Huizhong Pharmatech Co.,Ltd.,Nanjing 210009,China) |
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| Abstract: | To explore novel monoamine reuptake inhibitor with antidepressant activity, a series of substituted aryl alkanol piperidine derivatives were designed and synthesized. All of them were new compounds, and their structures were confirmed with 1H NMR and HR-MS. The results showed that compounds 4, 5 and 8 displayed strong 5-HT, NA and DA reuptake inhibiting activities in vitro. Among the tested compounds, 4, 5 and 13 exhibited potent antidepressant activities in the mice forced swimming test. Compounds 4 and 5 have potent antidepressant activities and are worth further development. |
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| Keywords: | aryl alkanol piperidine derivative monoamine reuptake inhibitor synthesis antidepressant activity |
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