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学科主题: 药学
题名:
Antinociception of spirocyclopiperazinium salt compound LXM-10-M targeting alpha 7 nicotinic receptor and M4 muscarinic receptor and inhibiting CaMKII alpha/CREB/CGRP signaling pathway in mice
作者: Wan, Dan1; Wang, Ding1; Sun, Qi2; Song, Yan1; Jiang, YiMin3; Li, RunTao2; Ye, Jia1
关键词: Spirocyclopiperazinium salt compound ; LXM-10-M ; Antinociception ; alpha 7 nicotinic receptor ; M4 muscarinic receptor ; CaMKII alpha/CREB/CGRP signaling pathway
刊名: EUROPEAN JOURNAL OF PHARMACOLOGY
发表日期: 2016-01-05
DOI: 10.1016/j.ejphar.2015.11.056
卷: 770, 页:92-98
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Pharmacology & Pharmacy
研究领域[WOS]: Pharmacology & Pharmacy
关键词[WOS]: DEPENDENT PROTEIN-KINASE ; ELEMENT-BINDING PROTEIN ; GENE-RELATED PEPTIDE ; INFLAMMATORY PAIN ; RATS ; MODELS ; PHOSPHORYLATION ; ACTIVATION ; BEHAVIOR ; NUCLEUS
英文摘要:

The present study was designed to investigate the antinociception of spirocyclopiperazinium salt compound LXM-10-M (2,4-dimethyl-9-beta m-hydroxyphenylethyl-3-oxo-6, 9-diazaspiro [5.5] undecane chloride) in thermal and chemical pain models, and further to explore the molecular target and potential signal pathway. We assessed the antinociception of LXM-10-M in hot-plate test, formalin test and acetic acid writhing test in mice. The possible changes of calcium/calmodulin-dependent protein kinase II alpha (CaMKII alpha)/cAMP response element-binding protein (CREB)/calcitonin gene related peptide (CGRP) signaling pathway were detected by Western Blot in mice. Administration of LXM-10-M produced significant antinociception in hot-plate test, formalin test and acetic acid writhing test in mice, with no obvious toxicity. The antinociceptive effects were blocked by pretreatment with methyllycaconitine citrate (MLA, alpha 7 nicotinic receptor antagonist) or tropicamide (TRO, M4 muscarinic receptor antagonist). Western blot analysis showed that the upregulations of p-CaMKII alpha, p-CREB and CGRP in the spinal cord were reduced by LXM-10-M in chemical pain model in mice, and the effects were blocked by MLA or TRO pretreatment. This is the first paper to report that LXM-10-M exerted significant antinociception, which may be attributed to the activation of alpha 7 nicotinic receptor and M4 muscarinic receptor and thereby triggering the inhibition of CaMKII alpha/CREB/CGRP signaling pathway in mice. (C)) 2015 Elsevier By. All rights reserved.

语种: 英语
所属项目编号: 81470050 ; 7122097
项目资助者: National Natural Science Foundation of China, China ; Beijing Municipal Natural Science Foundation, China
WOS记录号: WOS:000367230700013
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/56792
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, Dept Mol & Cellular Pharmacol, Beijing 100871, Peoples R China
2.Peking Univ, Sch Pharmaceut Sci, Dept Biol Chem, Beijing 100871, Peoples R China
3.Peking Univ, Med & Hlth Anal Ctr, Beijing 100871, Peoples R China

Recommended Citation:
Wan, Dan,Wang, Ding,Sun, Qi,et al. Antinociception of spirocyclopiperazinium salt compound LXM-10-M targeting alpha 7 nicotinic receptor and M4 muscarinic receptor and inhibiting CaMKII alpha/CREB/CGRP signaling pathway in mice[J]. EUROPEAN JOURNAL OF PHARMACOLOGY,2016,770:92-98.
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