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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
硕士研究生。研究方向:中医药防治儿童呼吸系统疾病。E-mail:1915672986@qq.com
副主任医师,硕士生导师,硕士。研究方向:中西医结合治疗小儿呼吸系统疾病。电话:0371-66211112。E-mail:zhangyan6905@126.com
收稿日期:2023-11-17,
修回日期:2024-07-22,
录用日期:2024-07-22,
纸质出版日期:2024-08-15
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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 [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 [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.
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。
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.
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