Mechanism and prevention progress of receptor desensitization induced by β2-AR agonists in the treatment of asthma
- VernacularTitle: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
- Author:
Junya DUAN
1
;
Yan ZHANG
1
;
Guihua SONG
2
;
Xiaosong CHEN
2
;
Yanrong GUO
2
;
Xuan ZHOU
3
;
Xinying CHEN
3
Author Information
1. Dept. of Pediatrics，the First Affiliated Hospital of Henan University of Chinese Medicine，Zhengzhou 450003，China;School of Pediatrics，Henan University of Chinese Medicine，Zhengzhou 450003，China
2. Dept. of Pediatrics，the First Affiliated Hospital of Henan University of Chinese Medicine，Zhengzhou 450003，China
3. School of Pediatrics，Henan University of Chinese Medicine，Zhengzhou 450003，China
- Publication Type:Journal Article
- Keywords:
bronchial asthma;
β2-adrenergic receptor agonists;
desensitization;
mechanism of occurrence;
prevention effect
- From:
China Pharmacy
2024;35(15):1910-1914
- CountryChina
- Language:Chinese
-
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.
