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Synthesis and analgesic activities of phenyl piperazinyl aralkyl ketone derivatives

文献类型：期刊论文

作者Xie Peng2; Wang Guan2; Zhang Guisen3; Zhang Li2; Xu Xiangqing3; Guo Lin1; Li Jianqi2
刊名Acta Pharmaceutica Sinica
出版日期2012
卷号47期号:11页码:1511-1516
关键词phenyl piperazinyl aralkyl ketone derivatives non-opioid analgesics synthesis pharmacokinetic
ISSN号0513-4870
其他题名芳烷基苯基哌嗪类衍生物的合成及镇痛活性研究
文献子类Article
英文摘要To explore novel non-opioid analgesic agents, 16 compounds were synthesized and their structures were confirmed by ~1H NMR and HR-MS. YX0611-1 was treated as the leading compound. The results of mice writhing model and hot plate model showed that compounds 2, 7, 8, 9, 11 and 15 had obvious analgesic activities in vivo. The test of affinity to mu, delta, kappa receptor displayed that active compounds didn't act on opioid receptor. The results of preliminary toxicity and pharmacokinetic tests showed that compound 7 had better safety and pharmacokinetic properties than that of YX0611-1, and it deserved further development.
资助项目"重大新药创制"国家科技重大专项[00000000]
WOS研究方向Pharmacology & Pharmacy (provided by Clarivate Analytics)
语种中文
CSCD记录号CSCD:4665968
源URL[http://119.78.100.183/handle/2S10ELR8/267816]  
专题中国科学院上海药物研究所
作者单位1.Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
2.Novel Technology Center of Pharmaceutical Chemistry, Shanghai Institute of Pharmaceutical Industry, Shanghai 200437, China.;
3.Jiangsu Nhwa Pharmaceutical Co., Ltd., Xuzhou, Jiangsu 221009, China.;
推荐引用方式
GB/T 7714		 Xie Peng,Wang Guan,Zhang Guisen,et al. Synthesis and analgesic activities of phenyl piperazinyl aralkyl ketone derivatives[J]. Acta Pharmaceutica Sinica,2012,47(11):1511-1516.
APA Xie Peng.,Wang Guan.,Zhang Guisen.,Zhang Li.,Xu Xiangqing.,...&Li Jianqi.(2012).Synthesis and analgesic activities of phenyl piperazinyl aralkyl ketone derivatives.Acta Pharmaceutica Sinica,47(11),1511-1516.
MLA Xie Peng,et al."Synthesis and analgesic activities of phenyl piperazinyl aralkyl ketone derivatives".Acta Pharmaceutica Sinica 47.11(2012):1511-1516.

入库方式： OAI收割

来源：上海药物研究所

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