The transient receptor potential vanilloid 1: role in airway inflammation and disease

Eur J Pharmacol. 2006 Mar 8;533(1-3):207-14. doi: 10.1016/j.ejphar.2005.12.063. Epub 2006 Feb 7.


The transient receptor potential vanilloid 1 (TRPV1) is an excitatory cation channel, rather selectively expressed in a subpopulation of nociceptive, primary sensory neurons that promote neurogenic inflammation via neuropeptide release. TRPV1 is activated by noxious temperature, low extracellular pH and diverse lipid derivatives, and is uniquely sensitive to vanilloid molecules, including capsaicin. TRPV1 expression and sensitivity is highly regulated by diverse G protein-coupled and tyrosine kinase receptors. Other exogenous or endogenous chemical agents, including reactive oxygen species, ethanol and hydrogen sulphide sensitize/activate TRPV1. In the airways, TRPV1 agonists cause cough, bronchoconstriction, microvascular leakage, hyperreactivity and hypersecretion. Patients with asthma and chronic obstructive pulmonary disease are more sensitive to the tussive effect of TRPV1 agonists and TRPV1 activation may contribute to respiratory symptoms caused by acidic media present in the airways during asthma exacerbation, gastroesophageal reflux induced asthma or in other conditions. TRPV1 antagonists may be useful in the treatment of these diseases.

Publication types

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

MeSH terms

  • Animals
  • Asthma / drug therapy
  • Asthma / metabolism*
  • Cough / metabolism
  • Cough / prevention & control
  • Humans
  • Ligands
  • Neurogenic Inflammation / drug therapy
  • Neurogenic Inflammation / metabolism*
  • Neurons / drug effects
  • Neurons / metabolism
  • Pulmonary Disease, Chronic Obstructive / drug therapy
  • Pulmonary Disease, Chronic Obstructive / metabolism*
  • Respiratory System / drug effects
  • Respiratory System / innervation
  • Respiratory System / metabolism
  • Respiratory System Agents / pharmacology
  • Respiratory System Agents / therapeutic use
  • TRPV Cation Channels / antagonists & inhibitors
  • TRPV Cation Channels / metabolism*


  • Ligands
  • Respiratory System Agents
  • TRPV Cation Channels
  • TRPV1 receptor