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神经烟碱型乙酰胆碱受体作为疼痛和炎症靶点的新见解:聚焦于α7 nAChR。

New Insights on Neuronal Nicotinic Acetylcholine Receptors as Targets for Pain and Inflammation: A Focus on α7 nAChRs.

机构信息

Department of Pharmacology and Toxicology, Virginia Commonwealth University, Richmond, Virginia, United States.

Experimental Animals Breeding and Research Center, Faculty of Medicine, Uludag University, Bursa, Turkey.

出版信息

Curr Neuropharmacol. 2018;16(4):415-425. doi: 10.2174/1570159X15666170818102108.

DOI:10.2174/1570159X15666170818102108
PMID:28820052
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6018191/
Abstract

BACKGROUND

Nicotine and nicotinic acetylcholine receptors (nAChRs) have been explored for the past three decades as targets for pain control. The aim of this review is to introduce readers particularly to α7 nAChRs in a perspective of pain and its modulation.

METHODS

Developments for α7 nAChR modulators and recent animal studies related to pain are reviewed.

RESULTS

Accumulating evidences suggest that selective ligands for α7 nAChRs hold promise in the treatment of chronic pain conditions as they lack many of side effects associated with other nicotinic receptor types.

CONCLUSION

This review provides the reader recent insights on α7 nAChRs from structure and function to the latest findings on the pharmacology and therapeutic targeting of these receptors for the treatment of pain and inflammation.

摘要

背景

在过去的三十年中,尼古丁和烟碱型乙酰胆碱受体(nAChRs)一直被作为控制疼痛的靶点进行研究。本文旨在从疼痛及其调节的角度,向读者介绍α7 nAChRs。

方法

综述了α7 nAChR 调节剂的发展和最近与疼痛相关的动物研究。

结果

越来越多的证据表明,α7 nAChR 的选择性配体在治疗慢性疼痛疾病方面具有广阔的前景,因为它们缺乏与其他烟碱受体类型相关的许多副作用。

结论

本综述从结构和功能到这些受体的药理学和治疗靶点方面,为读者提供了有关α7 nAChRs 的最新见解,以治疗疼痛和炎症。

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Cell Rep. 2017 Apr 25;19(4):688-696. doi: 10.1016/j.celrep.2017.04.008.
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B-973, a novel piperazine positive allosteric modulator of the α7 nicotinic acetylcholine receptor.B-973,一种新型的α7烟碱型乙酰胆碱受体的哌嗪正变构调节剂。
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The α7 nicotinic receptor dual allosteric agonist and positive allosteric modulator GAT107 reverses nociception in mouse models of inflammatory and neuropathic pain.α7烟碱型受体双重变构激动剂和正变构调节剂GAT107可逆转炎症性疼痛和神经性疼痛小鼠模型中的伤害感受。
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