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

Mechanism and prevention progress of receptor desensitization induced by β2-AR agonists in the treatment of asthma

段俊亚 ¹张岩 ¹宋桂华 ²陈小松 ²郭彦荣 ²周璇 ³陈新颖³

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作者信息

1. 河南中医药大学第一附属医院儿科医院,郑州 450003;河南中医药大学儿科医学院,郑州 450003
2. 河南中医药大学第一附属医院儿科医院,郑州 450003
3. 河南中医药大学儿科医学院,郑州 450003
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摘要

β2-肾上腺素受体(β2-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β2-AR脱敏,降低其临床疗效,致使部分哮喘患者症状控制欠佳.β2-AR激动药引起β2-AR脱敏的机制主要包括慢速脱敏(与气道黏膜β2-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β2-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β2-AR激动药联合使用时能改善β2-AR的敏感性,从而更好地控制哮喘症状.

Abstract

β2-adrenergic receptor(β2-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 β2-AR desensitization and reduce its clinical efficacy,resulting in poor symptom control of some asthma patients.The mechanism of β2-AR desensitization induced by β2-AR agonists mainly includes slow hyposensitization(related to the decrease of β2-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 β2-AR desensitization.Glucocorticoids,peroxisome proliferator-activated receptor-gamma agonists,ASM-024,Chinese medicine monotherapies and formulations,when combined with β2-AR agonists,can improve the sensitivity of β2-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

Key words

bronchial asthma/β2-adrenergic receptor agonists/desensitization/mechanism of occurrence/prevention effect

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基金项目

国家自然科学基金面上项目(81873338)

河南省医学科技攻关计划联合共建项目(LHGJ20230687)

河南省"双一流"创建学科中医学科学研究专项(HSRP-DFCTCM-2023-8-26)

出版年

2024

中国药房

中国医院协会,中国药房杂志社

中国药房

CSTPCD北大核心

影响因子：0.956

ISSN：1001-0408

参考文献量15

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