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Antinociceptive mechanism of the spirocyclopiperazinium compound LXM-10 in mice and rats
Xiong, Yulan1,4; Zhao, Xia2; Sun, Qi3; Li, Runtao3; Li, Changling2; Ye, Jia1,2
关键词Antinociception Alpha 7 Nicotinic Acetylcholine Receptor M4 Muscarine Acetylcholine Receptor Lxm-10
刊名PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR
2010-04-01
DOI10.1016/j.pbb.2010.01.004
95期:2页:192-197
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Behavioral Sciences ; Neurosciences ; Pharmacology & Pharmacy
资助者National Science Foundation of China ; National Science Foundation of China
研究领域[WOS]Behavioral Sciences ; Neurosciences & Neurology ; Pharmacology & Pharmacy
关键词[WOS]MUSCARINIC RECEPTOR SUBTYPES ; ACETYLCHOLINE-RECEPTORS ; CHOLINERGIC MODULATION ; SYNAPTIC-TRANSMISSION ; INFLAMMATORY PAIN ; GLUTAMATE RELEASE ; KNOCKOUT MICE ; SPINAL-CORD ; ANALGESIA ; AGONIST
英文摘要

Drugs typically used to treat pain are limited by their undesirable side effects, which has prompted a search for mechanistically different analgesic agents. We report the antinociception effect of the spirocyclopiperazinium compound LXM-10 via activation of peripheral alpha 7 nicotinic and muscarinic acetylcholine receptors in mice. This effect was attenuated by hexamethonium, atropine methylnitrate, methyllycaconitine citrate, tropicamide, bicuculline, and phaclofen. Competition receptor-binding assays in vitro showed that LXM-10 binds with high affinity a7 nAchR and with low affinity M4 receptors. Our findings show that the antinociception signaling pathway of LXM-10 underlies activation of peripheral a7 nicotinic and possibly of M4 muscarinic receptors, which activate GABA(A) and GABA(B) receptors, resulting in antinociceptive effects without obvious side effects. (C) 2010 Elsevier Inc. All rights reserved.

语种英语
所属项目编号NSFC 20772009
资助者National Science Foundation of China ; National Science Foundation of China
WOS记录号WOS:000276146500008
Citation statistics
Cited Times:7[WOS]   [WOS Record]     [Related Records in WOS]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/50459
Collection北京大学药学院
作者单位1.Peking Univ, 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
3.Peking Univ, Sch Pharmaceut Sci, Dept Biol Chem, Beijing 100191, Peoples R China
4.Peking Univ, Inst Mental Hlth, Beijing 100191, Peoples R China
Recommended Citation
GB/T 7714
Xiong, Yulan,Zhao, Xia,Sun, Qi,et al. Antinociceptive mechanism of the spirocyclopiperazinium compound LXM-10 in mice and rats[J]. PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR,2010,95(2):192-197.
APA Xiong, Yulan,Zhao, Xia,Sun, Qi,Li, Runtao,Li, Changling,&Ye, Jia.(2010).Antinociceptive mechanism of the spirocyclopiperazinium compound LXM-10 in mice and rats.PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR,95(2),192-197.
MLA Xiong, Yulan,et al."Antinociceptive mechanism of the spirocyclopiperazinium compound LXM-10 in mice and rats".PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR 95.2(2010):192-197.
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