Funktionelle Selektivität am Beispiel des β2-Adrenozeptors

Abstract

Originally, G protein-coupled receptors were assumed to act as on-off switches, adopting either an active (R*) or inactive (R) conformation. However, pharmacological and biophysical studies over the past 15–20 years have now unequivocally shown that receptors can exist in multiple active conformations with distinct capabilities to activate effectors. This concept is referred to as functional selectivity and has important implications for future drug design. Here, we discuss this fundamental pharmacological concept using the β2-adrenoceptor as paradigm.