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学科主题: 药学
题名:
Synthesis and analgesic evaluation of a series of proline-typed spiro cyclic quaternary ammoniums
作者: 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
发表日期: 2014-02-01
DOI: 10.1007/s00044-013-0681-6
卷: 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
所属项目编号: NSFC 20802004
项目资助者: National Science Foundation of China
WOS记录号: WOS:000330766600028
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/62586
Appears in Collections:北京大学药学院_期刊论文

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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

Recommended Citation:
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.
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