Title : Salmeterol Efficacy and Bias in the Activation and Kinase-Mediated Desensitization of β2-Adrenergic Receptors.

Pub. Date : 2015 Jun

PMID : 25784721






5 Functional Relationships(s)
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1 Salmeterol is a long-acting beta2-adrenergic receptor (beta2AR) agonist that is widely used as a bronchodilator for the treatment of persistent asthma and chronic obstructive pulmonary disease in conjunction with steroids. Salmeterol Xinafoate adrenoceptor beta 2 Homo sapiens
2 Salmeterol is a long-acting beta2-adrenergic receptor (beta2AR) agonist that is widely used as a bronchodilator for the treatment of persistent asthma and chronic obstructive pulmonary disease in conjunction with steroids. Salmeterol Xinafoate adrenoceptor beta 2 Homo sapiens
3 Previous studies demonstrated that salmeterol showed weak efficacy for activation of adenylyl cyclase; however, its efficacy in the complex desensitization of the beta2AR remains poorly understood. Salmeterol Xinafoate adrenoceptor beta 2 Homo sapiens
4 In this work, we provide insights into the roles played by the G protein-coupled receptor kinase/arrestin and protein kinase A in salmeterol-mediated desensitization through bioluminescence resonance energy transfer (BRET) studies of liganded-beta2AR binding to arrestin and through kinetic studies of cAMP turnover. Salmeterol Xinafoate adrenoceptor beta 2 Homo sapiens
5 First, BRET demonstrated a much reduced efficacy for salmeterol recruitment of arrestin to beta2AR relative to isoproterenol. Salmeterol Xinafoate adrenoceptor beta 2 Homo sapiens