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

Beta-Adrenergic Agonists

1,* , 2
, 2
 and 2
Received: 2 February 2010; in revised form: 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 which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

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

AMA Style

Barisione G, Baroffio M, Crimi E, Brusasco V. Beta-Adrenergic Agonists. Pharmaceuticals. 2010; 3(4):1016-1044.

Chicago/Turabian Style

Barisione, Giovanni; Baroffio, Michele; Crimi, Emanuele; Brusasco, Vito. 2010. "Beta-Adrenergic Agonists." Pharmaceuticals 3, no. 4: 1016-1044.


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