β2 -Adrenoceptor agonist profiling reveals biased signalling phenotypes for the β2 -adrenoceptor with possible implications for the treatment of asthma.

Abstract excerpt

BACKGROUND AND PURPOSE: β-Adrenoceptor agonists relieve airflow obstruction by activating β2 -adrenoceptors, which are G protein-coupled receptors (GPCRs) expressed on human airway smooth muscle (HASM) cells. The currently available β-adrenoceptor agonists are balanced agonists, however, and signal through both the stimulatory G protein (Gs )- and β-arrestin-mediated pathways. While Gs signalling is beneficial...

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