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Synthesis and analgesic evaluation of a series of proline-typed spiro cyclic quaternary ammoniums
Lin, Songwen1; Wang, Na1; Zhao, Shuo1; Sun, Qi1; Zhang, Weiwei2; Ye, Jia2; Cheng, Tieming1; Li, Runtao1
关键词Spirocyclic quaternary ammonium SAR Synthesis Analgesic activity alpha 7 nAChR
刊名MEDICINAL CHEMISTRY RESEARCH
2014-02-01
DOI10.1007/s00044-013-0681-6
23期:2页:862-869
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Chemistry, Medicinal
研究领域[WOS]Pharmacology & Pharmacy
关键词[WOS]UNIQUE SPIROCYCLOPIPERAZINIUM SALT ; NICOTINIC ACETYLCHOLINE-RECEPTORS ; COMPOUND LXM-10 ; LIGANDS ; PAIN ; MICE
英文摘要

A series of proline derivated spirocyclic quaternary ammoniums were synthesized and evaluated via in vivo analgesic activities. Compounds 9a showed the best analgesic effect with 84 % inhibition in mice. These compounds showed only micromolar Ki value by in vitro alpha 7 nAChR binding test, which may indicate the form of active metabolite play a role in their in vitro analgesic activities.

语种英语
WOS记录号WOS:000330766600028
项目编号NSFC 20802004
资助机构National Science Foundation of China
引用统计
被引频次:1[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/62586
专题北京大学药学院
北京大学药学院_化学生物学系
北京大学药学院_分子与细胞药理学系
北京大学医学图书馆_信息咨询部
北京大学第三临床医学院_儿科
作者单位1.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
2.Peking Univ, Sch Pharmaceut Sci, Dept Mol & Cellular Pharmacol, Beijing 100191, Peoples R China
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GB/T 7714
Lin, Songwen,Wang, Na,Zhao, Shuo,et al. Synthesis and analgesic evaluation of a series of proline-typed spiro cyclic quaternary ammoniums[J]. MEDICINAL CHEMISTRY RESEARCH,2014,23(2):862-869.
APA Lin, Songwen.,Wang, Na.,Zhao, Shuo.,Sun, Qi.,Zhang, Weiwei.,...&Li, Runtao.(2014).Synthesis and analgesic evaluation of a series of proline-typed spiro cyclic quaternary ammoniums.MEDICINAL CHEMISTRY RESEARCH,23(2),862-869.
MLA Lin, Songwen,et al."Synthesis and analgesic evaluation of a series of proline-typed spiro cyclic quaternary ammoniums".MEDICINAL CHEMISTRY RESEARCH 23.2(2014):862-869.
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