Beta-Adrenergic Agonists

Pharmaceuticals

Giovanni Barisione¹  Michele Baroffio²  Emanuele Crimi² 

[1] Preventive and Occupational Medicine Unit, Respiratory Pathophysiology Laboratory, University Hospital San Martino, Largo R. Benzi, 10 - 16132 Genoa, Italy;Respiratory Pathophysiology Unit, Department of Internal Medicine, University of Genoa, Viale Benedetto XV - 16132 Genoa, Italy; E-Mails:

关键词: β₂-adrenoceptors;    G-protein-coupled receptor signaling;    airway smooth muscle;    bronchodilation;    desensitization;    safety issues;   

DOI  :  10.3390/ph3041016

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2010 by the authors; licensee Molecular Diversity Preservation International, Basel, Switzerland.