| 芳基、芳甲基及哌嗪基脒类化合物的设计与合成及5-HT和NE重摄取双重抑制活性 |
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| 引用本文： | 秦芳,杨静,文辉,张建军,王亚芳,冀呈雪,杨光中.芳基、芳甲基及哌嗪基脒类化合物的设计与合成及5-HT和NE重摄取双重抑制活性[J].高等学校化学学报,2009,30(5):938-944. |
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| 作者姓名： | 秦芳 杨静 文辉 张建军 王亚芳 冀呈雪 杨光中 |
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| 作者单位： | 中国协和医科大学,中国医学科学院药物研究所,北京,100050 |
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| 基金项目： | 国家自然科学基金，北京市自然科学基金 |
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| 摘 要： | 基于药效团模型和前期的研究结果, 设计合成了一类全新结构类型的芳基、芳甲基及哌嗪基脒类化合物, 通过1H NMR, HRMS对化合物结构进行了确证, 并完成了初步的体外药理活性评价. 结果表明, 这些化合物均显示出不同程度的5-HT和NE重摄取抑制活性, 其中化合物4b的活性最好, 化合物4a和8a在整体动物抗抑郁药效学实验中表现出明确的抗抑郁活性.
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| 关 键 词： | 5-羟色胺 去甲肾上腺素 药效团模型 双重重摄取抑制剂 |
| 收稿时间： | 2008-09-16 |
Design,Synthesis and 5-HT/NE Dual Reuptake Inhibition Activity of Phenylbenzamidine Derivatives |
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| QIN Fang,YANG Jing,WEN Hui,ZHANG Jian-Jun,WANG Ya-Fang,JI Cheng-Xue,YANG Guang-Zhong.Design,Synthesis and 5-HT/NE Dual Reuptake Inhibition Activity of Phenylbenzamidine Derivatives[J].Chemical Research In Chinese Universities,2009,30(5):938-944. |
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| Authors: | QIN Fang YANG Jing WEN Hui ZHANG Jian-Jun WANG Ya-Fang JI Cheng-Xue YANG Guang-Zhong |
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| Institution: | Institute of Materia Medica;Chinese Academy of Medical Sciences & Peking Union Medical College;Beijing 100050;China |
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| Abstract: | Depression is a kind of common and severe mental illness.Over the past few years,a number of studies have emerged suggesting that treatment with antidepressants which simultaneously enhance both noradrenergic as well as serotonergic neurotransmission including Venlafaxine and Duloxetine may result in higher response or remission rates than treatment with antidepressants which selectively enhance serotonergic neurotransmission.Based on the pharmacophore information and the analysis of structure-activity rela... |
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| Keywords: | Serotonin Norepinephrine Pharmacophore model Dual reuptake inhibitors |
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