Beta-adrenergic agonists

Giovanni Barisione, Michele Baroffio, Emanuele Crimi, Vito Brusasco

Research output: Contribution to journalArticlepeer-review


Inhaled β2-adrenoceptor (β2-AR) agonists are considered essential bronchodilator drugs in the treatment of bronchial asthma, both as symptoms-relievers and, in combination with inhaled corticosteroids, as disease-controllers. In this article, we first review the basic mechanisms by which the β2-adrenergic system contributes to the control of airway smooth muscle tone. Then, we go on describing the structural characteristics of β2-AR and the molecular basis of G-protein-coupled receptor signaling and mechanisms of its desensitization/ dysfunction. In particular, phosphorylation mediated by protein kinase A and β-adrenergic receptor kinase are examined in detail. Finally, we discuss the pivotal role of inhaled β2-AR agonists in the treatment of asthma and the concerns about their safety that have been recently raised.

Original languageEnglish
Pages (from-to)1016-1044
Number of pages29
Issue number4
Publication statusPublished - 2010


  • β-adrenoceptors
  • Airway smooth muscle
  • Bronchodilation
  • Desensitization
  • G-protein-coupled receptor signaling
  • Safety issues

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmaceutical Science


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