CB1 and CB2 receptor pharmacology

Abstract

This review describes compounds that are currently most widely used in preclinical research to activate or block cannabinoid CB1 and CB2 receptors. Some of these compounds are ligands that display significant selectivity as CB1 or CB2 receptor agonists or antagonists, the remainder consisting of agonists each of which exhibits more or less equal potency at CB1 and CB2 receptors. The cannabinoid receptor antagonists most often used as pharmacological tools behave as inverse agonists in at least some assay systems and possible explanations for this inverse agonism are briefly discussed. Also considered in this review are actual and potential therapeutic applications for CB1 and CB2 receptor ligands.