神经病理性疼痛和炎症性疼痛中的烟碱型乙酰胆碱受体。
Nicotinic acetylcholine receptors in neuropathic and inflammatory pain.
机构信息
Department of Biology, University of Utah, Salt Lake City, UT, USA.
Department of Psychiatry, University of Utah, Salt Lake City, UT, USA.
出版信息
FEBS Lett. 2018 Apr;592(7):1045-1062. doi: 10.1002/1873-3468.12884. Epub 2017 Oct 27.
Abstract
Nicotinic acetylcholine receptors (nAChRs) are actively being investigated as therapeutic targets for the treatment of pain and inflammation, but despite more than 30 years of research, there are currently no FDA-approved analgesics that are specific for these receptors. Much of the initial research effort focused on the α4β2 nAChR subtype, but more recently, additional subtypes have been identified as promising new leads and include α6β4, α7, and α9-containing nAChRs. This Review will focus on the distribution of these nAChRs in the cell types involved in neuropathic pain and inflammation and the activity of currently available nicotinic ligands.
摘要
烟碱型乙酰胆碱受体（nAChRs）作为治疗疼痛和炎症的治疗靶点正在被积极研究，但尽管经过了 30 多年的研究，目前还没有获得 FDA 批准的针对这些受体的镇痛药。最初的研究工作主要集中在α4β2 nAChR 亚型上，但最近，其他亚型被确定为有前途的新靶点，包括含有α6β4、α7 和α9 的 nAChRs。本综述将重点介绍这些 nAChRs 在涉及神经性疼痛和炎症的细胞类型中的分布，以及目前可用的烟碱配体的活性。
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