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Pharmaceuticals 2010, 3(4), 1016-1044; doi:10.3390/ph3041016
Review

Beta-Adrenergic Agonists

1,* , 2
,
2
 and
2
1 Preventive and Occupational Medicine Unit, Respiratory Pathophysiology Laboratory, University Hospital San Martino, Largo R. Benzi, 10 - 16132 Genoa, Italy 2 Respiratory Pathophysiology Unit, Department of Internal Medicine, University of Genoa, Viale Benedetto XV - 16132 Genoa, Italy
* Author to whom correspondence should be addressed.
Received: 2 February 2010 / Revised: 15 March 2010 / Accepted: 26 March 2010 / Published: 30 March 2010
(This article belongs to the Special Issue Antiasthmatic Drugs)
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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.
Keywords: β2-adrenoceptors; G-protein-coupled receptor signaling;airway smooth muscle; bronchodilation; desensitization; safety issues β2-adrenoceptors; G-protein-coupled receptor signaling; airway smooth muscle; bronchodilation; desensitization; safety issues
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Barisione, G.; Baroffio, M.; Crimi, E.; Brusasco, V. Beta-Adrenergic Agonists. Pharmaceuticals 2010, 3, 1016-1044.

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