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Mechanism and prevention progress of receptor desensitization induced by
β 2-AR agonists in the treatment of asthma- ZHONGGUO YAOFANG Vol. 35, Issue 15, Pages: 1910-1914(2024)
- 作者机构：
1.河南中医药大学第一附属医院儿科医院，郑州 450003
2.河南中医药大学儿科医学院，郑州 450003
- 作者简介：
- 基金信息：
DOI：10.6039/j.issn.1001-0408.2024.15.19
CLC： R974+.3;R562.2+5Published：15 August 2024，
Received：17 November 2023，
Revised：12 June 2024，
- 稿件说明：
扫 描 看 全 文
段俊亚,张岩,宋桂华等.哮喘治疗中β2-AR激动药诱发受体脱敏的发生机制及预防进展 Δ[J].中国药房,2024,35(15):1910-1914.
DUAN Junya,ZHANG Yan,SONG Guihua,et al.Mechanism and prevention progress of receptor desensitization induced by β2-AR agonists in the treatment of asthma[J].ZHONGGUO YAOFANG,2024,35(15):1910-1914.
段俊亚,张岩,宋桂华等.哮喘治疗中β2-AR激动药诱发受体脱敏的发生机制及预防进展 Δ[J].中国药房,2024,35(15):1910-1914. DOI： 10.6039/j.issn.1001-0408.2024.15.19.
DUAN Junya,ZHANG Yan,SONG Guihua,et al.Mechanism and prevention progress of receptor desensitization induced by β2-AR agonists in the treatment of asthma[J].ZHONGGUO YAOFANG,2024,35(15):1910-1914. DOI： 10.6039/j.issn.1001-0408.2024.15.19.
摘要
β
2
-肾上腺素受体（
β
2
-AR）激动药作为治疗支气管哮喘（以下简称“哮喘”）的一线药物，在临床中广泛应用，然而长期使用可导致
β
2
-AR脱敏，降低其临床疗效，致使部分哮喘患者症状控制欠佳。
β
2
-AR激动药引起
β
2
-AR脱敏的机制主要包括慢速脱敏（与气道黏膜
β
2
-AR密度减小有关）和快速脱敏（与刺激性G蛋白脱偶联机制有关）。环磷酸腺苷（cAMP）-蛋白激酶A和cAMP-cAMP激活的交换蛋白信号通路与
β
2
-AR脱敏过程关系密切。糖皮质激素、过氧化物酶体增殖物激活受体γ激动药、ASM-024、中药单药及成方等与
β
2
-AR激动药联合使用时能改善
β
2
-AR的敏感性，从而更好地控制哮喘症状。
Abstract
β
2
-adrenergic receptor （
β
2
-AR） agonists are widely used as first-line drugs in the treatment of bronchial asthma （hereinafter referred to as “asthma”）， but long-term use can lead to
β
2
-AR desensitization and reduce its clinical efficacy， resulting in poor symptom control of some asthma patients. The mechanism of
β
2
-AR desensitization induced by
β
2
-AR agonists mainly includes slow hyposensitization （related to the decrease of
β
2
-AR density in airway mucosa） and rapid hyposensitization （related to the mechanism of stimulatory G protein decoupling）. Cyclic adenosine monophosphate（cAMP）-protein kinase A and cAMP-exchange protein activated by cAMP signaling pathways are closely related to
β
2
-AR desensitization. Glucocorticoids， peroxisome proliferator-activated receptor-gamma agonists， ASM-024， Chinese medicine monotherapies and formulations， when combined with
β
2
-AR agonists， can improve the sensitivity of
β
2
-AR， so as to better control asthma symptoms.
关键词
支气管哮喘β2-肾上腺素受体激动药脱敏发生机制预防作用
Keywords
β2-adrenergic receptor agonistsdesensitizationmechanism of occurrenceprevention effect
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