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 |
|---|---|
| Pages (from-to) | 1016-1044 |
| Number of pages | 29 |
| Journal | Pharmaceuticals |
| Volume | 3 |
| Issue number | 4 |
| DOIs | |
| Publication status | Published - 2010 |
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Keywords
- β-adrenoceptors
- Airway smooth muscle
- Bronchodilation
- Desensitization
- G-protein-coupled receptor signaling
- Safety issues
ASJC Scopus subject areas
- Molecular Medicine
- Pharmaceutical Science
Cite this
Beta-adrenergic agonists. / Barisione, Giovanni; Baroffio, Michele; Crimi, Emanuele; Brusasco, Vito.
In: Pharmaceuticals, Vol. 3, No. 4, 2010, p. 1016-1044.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Beta-adrenergic agonists
AU - Barisione, Giovanni
AU - Baroffio, Michele
AU - Crimi, Emanuele
AU - Brusasco, Vito
PY - 2010
Y1 - 2010
N2 - 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.
AB - 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.
KW - β-adrenoceptors
KW - Airway smooth muscle
KW - Bronchodilation
KW - Desensitization
KW - G-protein-coupled receptor signaling
KW - Safety issues
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UR - http://www.scopus.com/inward/citedby.url?scp=77952156765&partnerID=8YFLogxK
U2 - 10.3390/ph3041016
DO - 10.3390/ph3041016
M3 - Article
VL - 3
SP - 1016
EP - 1044
JO - Pharmaceuticals
JF - Pharmaceuticals
SN - 1424-8247
IS - 4
ER -