毒蕈碱受体作为抗炎治疗的靶点。

María Elena Sales
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引用次数: 0

摘要

乙酰胆碱能是神经元胆碱能系统的主要神经递质,由交感和副交感自主神经的节前纤维和节后副交感神经纤维合成。越来越多的实验证据表明乙酰胆碱在原核和真核非神经元细胞中广泛表达。神经元和非神经元胆碱能系统包括ACh,胆碱乙酰转移酶和胆碱酯酶,合成和分解ACh的酶,以及烟碱和毒蕈碱ACh受体(分别为nAChRs和mAChRs),它们是ACh作用的靶点。这篇综述分析了胆碱能系统,特别是通过mAChR参与炎症,并讨论了不同的mAChR拮抗剂的作用,这些拮抗剂已被用于治疗皮肤炎症性疾病、哮喘和COPD,以及肠道炎症和全身性炎症疾病,以评估这些化合物作为治疗工具的潜在应用。
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Muscarinic receptors as targets for anti-inflammatory therapy.

ACh, the main neurotransmitter in the neuronal cholinergic system, is synthesized by pre-ganglionic fibers of the sympathetic and parasympathetic autonomic nervous system and by post-ganglionic parasympathetic fibers. There is increasing experimental evidence that ACh is widely expressed in prokaryotic and eukaryotic non-neuronal cells. The neuronal and non-neuronal cholinergic systems comprise ACh, choline acetyltransferase and cholinesterase, enzymes that synthesize and catabolize ACh, and the nicotinic and muscarinic ACh receptors (nAChRs and mAChRs, respectively), which are the targets for ACh action. This review analyzes the participation of the cholinergic system, particularly through mAChRs, in inflammation, and discusses the role of the different mAChR antagonists that have been used to treat skin inflammatory disorders, asthma and COPD, as well as intestinal inflammation and systemic inflammatory diseases, to assess the potential application of these compounds as therapeutic tools.

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