Molecular mechanisms of beta(2)-adrenergic receptor function, response, and regulation

J Allergy Clin Immunol. 2006 Jan;117(1):18-24; quiz 25. doi: 10.1016/j.jaci.2005.11.012.


The human beta(2)-adrenoceptor is a member of the 7-transmembrane family of receptors, encoded by a gene on chromosome 5, and widely distributed in the respiratory tract. Intracellular signaling after beta(2)-adrenoceptor activation is largely affected through cyclic adenosine monophosphate and protein kinase A. Differences in the mechanism of interaction of short- and long-acting beta(2)-agonists and the beta(2)-receptor are reflected in the kinetics of airway smooth muscle relaxation and the onset and duration of bronchodilation in asthmatic patients. beta-Adrenoceptor desensitization associated with prolonged beta(2)-agonist activation differs depending on the cell type and is reflected in different profiles of clinical tolerance to chronic beta(2)-agonist therapy. A number of genetic polymorphisms of the beta(2)-receptor have been described that appear to alter the behavior of the receptor, including the response to beta(2)-agonists. The synergy between the beta(2)-receptor and the glucocorticoid receptor functions has implications for the combined use of beta(2)-agonists and corticosteroids in the treatment of respiratory disease.

Publication types

  • Review

MeSH terms

  • Adrenergic beta-Agonists / pharmacology
  • Amino Acid Sequence
  • Animals
  • Humans
  • Molecular Sequence Data
  • Polymorphism, Genetic
  • Receptors, Adrenergic, beta-2 / analysis
  • Receptors, Adrenergic, beta-2 / chemistry
  • Receptors, Adrenergic, beta-2 / genetics
  • Receptors, Adrenergic, beta-2 / physiology*
  • Signal Transduction


  • Adrenergic beta-Agonists
  • Receptors, Adrenergic, beta-2