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Beta-Adrenergic Agonists

Author(s): Giovanni Barisione | Michele Baroffio | Emanuele Crimi | Vito Brusasco

Journal: Pharmaceuticals
ISSN 1424-8247

Volume: 3;
Issue: 4;
Start page: 1016;
Date: 2010;
Original page

Keywords: β2-adrenoceptors | G-protein-coupled receptor signaling | airway smooth muscle | bronchodilation | desensitization | safety issues

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.
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