Regulation of airway inflammation and remodeling by muscarinic receptors: perspectives on anticholinergic therapy in asthma and COPD

Life Sci. 2012 Nov 27;91(21-22):1126-33. doi: 10.1016/j.lfs.2012.02.021. Epub 2012 Mar 3.


Acetylcholine is the primary parasympathetic neurotransmitter in the airways and an autocrine/paracrine secreted hormone from non-neuronal origins including inflammatory cells and airway structural cells. In addition to the well-known functions of acetylcholine in regulating bronchoconstriction and mucus secretion, it is increasingly evident that acetylcholine regulates inflammatory cell chemotaxis and activation, and also participates in signaling events leading to chronic airway wall remodeling that is associated with chronic obstructive airway diseases including asthma and COPD. As muscarinic receptors appear responsible for most of the pro-inflammatory and remodeling effects of acetylcholine, these findings have significant implications for anticholinergic therapy in asthma and COPD, which is selective for muscarinic receptors. Here, the regulatory role of acetylcholine in inflammation and remodeling in asthma and COPD will be discussed including the perspectives that these findings offer for anticholinergic therapy in these diseases.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Asthma / drug therapy*
  • Asthma / immunology
  • Asthma / metabolism
  • Asthma / pathology
  • Humans
  • Inflammation / drug therapy
  • Inflammation / immunology
  • Inflammation / metabolism
  • Inflammation / pathology
  • Muscarinic Antagonists / pharmacology
  • Muscarinic Antagonists / therapeutic use*
  • Pulmonary Disease, Chronic Obstructive / drug therapy*
  • Pulmonary Disease, Chronic Obstructive / immunology
  • Pulmonary Disease, Chronic Obstructive / metabolism
  • Pulmonary Disease, Chronic Obstructive / pathology
  • Receptors, Muscarinic / immunology
  • Receptors, Muscarinic / metabolism*
  • Respiratory System / drug effects
  • Respiratory System / immunology
  • Respiratory System / metabolism
  • Respiratory System / pathology*


  • Muscarinic Antagonists
  • Receptors, Muscarinic