Mechanism and prevention progress of receptor desensitization induced by β2-AR agonists in the treatment of asthma
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.
bronchial asthmaβ2-adrenergic receptor agonistsdesensitizationmechanism of occurrenceprevention effect
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