Beta-Adrenergic Agonists

Pharmaceuticals
Giovanni BarisioneVito Brusasco

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.

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Related Concepts

Adrenal Cortex Hormones
Asthma
Bronchodilator Agents
Phosphorylation
Protein KINASE
Beta-Adrenergic Receptor Kinases
Penicillin-Binding Proteins
Agonists
Airway Structure
Structure

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