Agonist-specific patterns of beta 2-adrenoceptor responses in human airway cells during prolonged exposure.

摘要: Background and purpose: beta(2)-Adrenoceptor agonists (beta(2)-agonists) are important bronchodilators used in the treatment of asthma chronic obstructive pulmonary disease. At molecular level, beta(2)-adrenergic agonist stimulation induces desensitization beta(2)-adrenoceptor. In this study, we have examined relationships between initial effect subsequent reduction responsiveness to restimulation for a panel beta(2)-agonists cellular vitro tissue models. Experimental approach: beta(2)-Adrenoceptor-induced responses loss receptor were studied primary human airway smooth muscle cells bronchial epithelial by measuring cAMP production. Receptor was compared at equi-effective concentrations, either after continuous incubation 24 h or 1 pulse exposure followed 23 washout. Key findings confirmed guinea pig tracheal preparations vitro. results: There differences trachea beta(2)-agonists. When occurred immediately incubation, correlated with all agonists. After exposure, emerged, example isoprenaline formoterol induced least responsiveness. High lipophilicity was, some extent, predictive responsiveness, but other factors appeared be involved determining individual Conclusions implications: clear ability different beta(2) induce concentrations.