Recent Advances in β₂-Agonists for Treatment of Chronic Respiratory Diseases and Heart Failure

β₂-Adrenoceptor (β₂-AR) agonists are widely used as bronchodilators. The emerge of ultralong acting β₂-agonists is an important breakthrough in pulmonary medicine. In this review, we will provide mechanistic insights into the application of β₂-agonists in asthma, chronic obstructive pulmonary disease (COPD), and heart failure (HF). Recent studies in β-AR signal transduction have revealed opposing functions of the β₁-AR and the β₂-AR on cardiomyocyte survival. Thus, β₂-agonists and β-blockers in combination may represent a novel strategy for HF management. Allosteric modulation and biased agonism at the β₂-AR also provide a theoretical basis for developing drugs with novel mechanisms of action and pharmacological profiles. Overlap of COPD and HF presents a substantial clinical challenge but also a unique opportunity for evaluation of the cardiovascular safety of β₂-agonists. Further basic and clinical research along these lines can help us develop better drugs and innovative strategies for the management of these difficult-to-treat diseases.