Related Experiment Video
Updated: Aug 17, 2026

Quantifying Agonist Activity at G Protein-coupled Receptors
Published on: December 26, 2011
Mechanisms of inverse agonism at G-protein-coupled receptors
1School of Animal and Microbial Sciences, University of Reading, Whiteknights, RG6 6AJ, Reading, UK. p.g.strange@reading.ac.uk
Abstract:
Many drugs with important therapeutic actions that had been assumed to be antagonists at G-protein-coupled receptors (GPCRs) have been shown to be inverse agonists. For both basic pharmacology and drug design it is important to understand the mechanisms whereby these drugs achieve their effects. It had been assumed that these drugs achieved their effects by stabilizing an inactive state of the receptor (R) at the expense of a partially activated state (R*). In this article, I consider this and other mechanisms that could explain inverse agonist actions, and conclude that more than one mechanism can apply to inverse agonism at GPCRs.
More Related Videos
Related Concept Videos
G-protein Coupled Receptors
G-protein Coupled Receptors
G Protein-coupled Receptors
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
Activation and Inactivation of G Proteins
GPCRs Regulate Adenylyl Cylase Activity
Two...
Transducer Mechanism: G Protein–Coupled Receptors
GPCRs are also called heptahelical, 7TM, or...

