Inhaled beta₂‐adrenoceptor agonists (beta₂‐agonists) are among the most used substances in competitive sports. The 2020 Prohibited List issued by the World Anti‐Doping Agency restricts use of all selective and non‐selective beta₂‐agonists in‐ and out‐ of competition with few exemptions. Formoterol, salbutamol, and salmeterol are allowed by inhalation within defined dosing limits. These restrictions are in place because supratherapeutic use of beta₂‐agonist has the potential to be anabolic and to enhance performance, as well as due to potential side effects. Despite substantial documentation that beta₂‐agonists exert anabolic and lipolytic actions, these actions are not widely recognized. Furthermore, a common misconception is that the inhaled route does not exert these effects. However, given the high relative systemic bioavailability via the inhaled route, inhalation at high doses can also exert anabolic and lipolytic actions. In this review, we highlight the anabolic and lipolytic actions beta₂‐agonists can exert, regardless of the type of beta₂‐agonist and the route of administration. The doses needed to provide such effects are also associated with adverse effects and would in most cases be detected in routine doping control. Notwithstanding, the beta₂‐agonist regulations are associated with some challenges and given their ability to induce muscle growth and to enhance performance, it is important to continue developing effective detection strategies to prevent potential misuse of beta₂‐agonists while allowing treatment of asthmatic subjects without causing adverse side effects or ergogenic actions.

中文翻译：

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β2-激动剂在人类中的合成代谢和脂解作用以及反兴奋剂挑战。

吸入β ₂肾上腺素能受体兴奋剂（测试版₂激动剂）可在竞争性运动最常用的物质中。世界反兴奋剂机构发布的2020年禁用清单限制在竞争中和竞争中使用所有选择性和非选择性beta ₂激动剂，且几乎没有豁免。福莫特罗，沙丁胺醇和沙美特罗在规定的剂量范围内允许吸入。这些限制都将因为超治疗使用测试版₂激动剂必须是合成代谢和增强性能，以及由于潜在的副作用的可能性。尽管有大量的文档说明beta ₂激动剂发挥合成代谢和脂解作用，这些作用尚未得到广泛认可。此外，常见的误解是吸入途径不会发挥这些作用。但是，鉴于通过吸入途径具有较高的相对全身生物利用度，高剂量吸入也可发挥合成代谢和脂解作用。在这次审查中，我们强调的合成代谢和分解脂肪的操作测试版₂激动剂可以发挥，无论测试的类型₂激动剂和给药途径。提供这种作用所需的剂量也与副作用有关，并且在大多数情况下将在常规掺杂控制中检测到。尽管如此，测试版₂激动剂法规着一些挑战相关联，并赋予其诱导肌肉生长并提高性能的能力，继续发展有效的检测策略，以防止测试可能会被滥用是很重要的₂激动剂，同时使治疗哮喘患者，而不会引起不良副作用或人为作用。