The therapeutic applications of cannabinoid agonists and antagonists

Abstract

To date, two subtypes of cannabinoid receptors, CB1 and CB2, have been described. They have been identified in both central and peripheral nervous systems. CB1 receptors are coupled to Gi or Go leading to inhibition of adenylyl cyclase and Ca2+ channels. CB2 receptors are also negatively coupled to adenylyl cyclase. To date, three classes of agonist ligands have been identified: natural cannabinoids and structurally-related compounds, aminoalkylindoles and arachidonyl acid derivatives. Antagonists have now also been described for both receptor subtypes. Cannabinoid receptors are involved in analgesia, cognition, memory, locomotor activity, control of appetite and vomiting, regulation of intestinal, bronchial and uterine contraction, control of intra-ocular pressure and regulation of inflammatory and immune responses. Both natural and synthetic cannabinoids with agonistic or antagonistic properties have promising therapeutic effects and will undoubtedly lead to the emergence of new pharmacological tools and useful drugs.