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Updated: Apr 28, 2026

Quantifying Agonist Activity at G Protein-coupled Receptors
Published on: December 26, 2011
Constitutive activity in cannabinoid receptors
1Forest Research Institute, Jersey City, New Jersey, USA.
Abstract:
The cannabinoid receptors are G protein-coupled receptors activated by endocannabinoids or exogenous agonist such as tetrahydrocannabinol. Upon agonist binding, cannabinoid receptors will activate G proteins of the Gi family, which in turn inhibits adenylyl cyclase. Recently, inverse agonists and neutral antagonist for cannabinoid receptors have been discovered, demonstrating constitutive activity of the cannabinoid receptors. This chapter will discuss the current state of the art and provide a framework for evaluating constitutive receptor activity and distinguishing constitutive receptor activity from constitutive endogenous agonist tone.
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