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Muscarinic receptor antagonists, from folklore to pharmacology; finding drugs that actually work in asthma and COPD.


ABSTRACT: In the lungs, parasympathetic nerves provide the dominant control of airway smooth muscle with release of acetylcholine onto M3 muscarinic receptors. Treatment of airway disease with anticholinergic drugs that block muscarinic receptors began over 2000 years ago. Pharmacologic data all indicated that antimuscarinic drugs should be highly effective in asthma but clinical results were mixed. Thus, with the discovery of effective β-adrenergic receptor agonists the use of muscarinic antagonists declined. Lack of effectiveness of muscarinic antagonists is due to a variety of factors including unwanted side effects (ranging from dry mouth to coma) and the discovery of additional muscarinic receptor subtypes in the lungs with sometimes competing effects. Perhaps the most important problem is inef

SUBMITTER: Moulton BC 

PROVIDER: S-EPMC3085867 | biostudies-literature | 2011 May

REPOSITORIES: biostudies-literature