The β-adrenergic receptors (βARs) include three subtypes, β₁, β₂ and β₃. These receptors are widely expressed and regulate numerous physiological processes including cardiovascular and metabolic functions and airway tone. The βARs are also important targets in the treatment of many diseases including hypertension, heart failure and asthma. In some cases, the use of current βAR ligands to treat a disease is suboptimal and can lead to severe side effects. One strategy to potentially improve such treatments is the development of biased agonists that selectively regulate a subset of βAR signaling pathways and responses. Here we discuss the compounds identified to date that preferentially activate a G_s- or β-arrestin-mediated signaling pathway through βARs. Mechanistic insight on how these compounds bias signaling sheds light on the potential development of even more selective compounds that should have increased utility in treating disease.

β-肾上腺素能受体（βARs）包括三种亚型，β ₁、β ₂和β ₃。这些受体广泛表达并调节许多生理过程，包括心血管和代谢功能以及气道张力。βARs也是治疗高血压、心力衰竭和哮喘等多种疾病的重要靶点。在某些情况下，使用当前的 βAR 配体治疗疾病不是最理想的，并且可能导致严重的副作用。一种可能改善此类治疗的策略是开发选择性调节βAR信号通路和反应子集的偏向激动剂。在这里，我们讨论了迄今为止确定的优先激活 G _{s的化合物}- 或通过 βARs 的 β-arrestin 介导的信号通路。关于这些化合物如何偏向信号传导的机制见解揭示了更具选择性的化合物的潜在开发，这些化合物应该在治疗疾病中具有更大的效用。