Abstract
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 language | English |
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Pages (from-to) | 1016-1044 |
Number of pages | 29 |
Journal | Pharmaceuticals |
Volume | 3 |
Issue number | 4 |
DOIs | |
Publication status | Published - 2010 |
Keywords
- β-adrenoceptors
- Airway smooth muscle
- Bronchodilation
- Desensitization
- G-protein-coupled receptor signaling
- Safety issues
ASJC Scopus subject areas
- Molecular Medicine
- Pharmaceutical Science