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毒蕈碱受体拮抗剂:对肺功能的影响。

Muscarinic receptor antagonists: effects on pulmonary function.

作者信息

Buels Kalmia S, Fryer Allison D

机构信息

Oregon Health and Science University, 3181 SW Sam Jackson Park Road, UHN67, Portland, OR 97239, USA.

出版信息

Handb Exp Pharmacol. 2012(208):317-41. doi: 10.1007/978-3-642-23274-9_14.

DOI:10.1007/978-3-642-23274-9_14
PMID:22222705
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4104281/
Abstract

In healthy lungs, muscarinic receptors control smooth muscle tone, mucus secretion, vasodilation, and inflammation. In chronic obstructive pulmonary disease (COPD) and asthma, cholinergic mechanisms contribute to increased bronchoconstriction and mucus secretion that limit airflow. This chapter reviews neuronal and nonneuronal sources of acetylcholine in the lung and the expression and role of M₁, M₂, and M₃ muscarinic receptor subtypes in lung physiology. It also discusses the evidence for and against the role of parasympathetic nerves in asthma, and the current use and therapeutic potential of muscarinic receptor antagonists in COPD and asthma.

摘要

在健康的肺中,毒蕈碱受体控制平滑肌张力、黏液分泌、血管舒张和炎症。在慢性阻塞性肺疾病(COPD)和哮喘中,胆碱能机制导致支气管收缩增强和黏液分泌增加,从而限制气流。本章回顾了肺中乙酰胆碱的神经元和非神经元来源,以及M₁、M₂和M₃毒蕈碱受体亚型在肺生理学中的表达和作用。它还讨论了支持和反对副交感神经在哮喘中作用的证据,以及毒蕈碱受体拮抗剂在COPD和哮喘中的当前应用和治疗潜力。

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本文引用的文献

1
Transport of ipratropium, an anti-chronic obstructive pulmonary disease drug, is mediated by organic cation/carnitine transporters in human bronchial epithelial cells: implications for carrier-mediated pulmonary absorption.溴化异丙托品作为一种治疗慢性阻塞性肺病的药物,在人支气管上皮细胞中通过有机阳离子/肉碱转运体进行转运:对载体介导的肺部吸收的影响。
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Membrane depolarization causes a direct activation of G protein-coupled receptors leading to local Ca2+ release in smooth muscle.膜去极化导致G蛋白偶联受体直接激活,进而引起平滑肌局部钙离子释放。
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Preclinical evaluation of long-acting muscarinic antagonists: comparison of tiotropium and investigational drugs.长效毒蕈碱拮抗剂的临床前评估:噻托溴铵与研究药物的比较。
J Pharmacol Exp Ther. 2009 Aug;330(2):660-8. doi: 10.1124/jpet.109.152470. Epub 2009 May 28.
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Muscarinic receptor subtypes in cilia-driven transport and airway epithelial development.纤毛驱动转运和气道上皮发育中的毒蕈碱受体亚型
Eur Respir J. 2009 May;33(5):1113-21. doi: 10.1183/09031936.00015108. Epub 2009 Feb 12.
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Etanercept prevents airway hyperresponsiveness by protecting neuronal M2 muscarinic receptors in antigen-challenged guinea pigs.依那西普通过保护抗原激发的豚鼠体内的神经元M2毒蕈碱受体来预防气道高反应性。
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Suitability of muscarinic acetylcholine receptor antibodies for immunohistochemistry evaluated on tissue sections of receptor gene-deficient mice.基于毒蕈碱型乙酰胆碱受体基因缺陷小鼠组织切片评估毒蕈碱型乙酰胆碱受体抗体用于免疫组织化学的适用性。
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Lack of specificity of commercially available antisera: better specifications needed.市售抗血清缺乏特异性:需要更好的规格说明。
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Tiotropium bromide is effective for severe asthma with noneosinophilic phenotype.噻托溴铵对非嗜酸性粒细胞型重度哮喘有效。
Eur Respir J. 2008 Jun;31(6):1379-80. doi: 10.1183/09031936.00014108.
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Muscarinic receptors mediate stimulation of collagen synthesis in human lung fibroblasts.毒蕈碱受体介导人肺成纤维细胞中胶原蛋白合成的刺激。
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