Constitutive Activity at the α 1 ‐Adrenoceptors: Past and Future Implications

This chapter contains sections titled: Introduction The α1-Adrenoceptors: Main Structure–Functional Features The Discovery of Constitutively Activating Mutations and its Implications Theoretical and Experimental Approaches for Study of Constitutive GPCR Activity Theoretical Analysis of CAM GPCR Pharmacology Computational Modeling of the α1BAR Measuring Constitutive Activity of the α1AR Subtypes Constitutively Activating Mutations of the α1AR Subtypes Where the Mutations have been Found Constitutive Activation of Multiple Signaling Pathways A Putative Model of Receptor Activation for the α1BAR Constitutive Activity of Wild-type α1ARs and Inverse Agonism Constitutive Activity of Wild-type α1AR Subtypes Inverse Agonism at the α1ARs Receptor Regulation and Constitutive Activity of the α1ARs Conclusions