The Cannabinoid Receptors

Part of the series The Receptors pp 3-19

Structure–Activity Relationships of Classical Cannabinoids

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In this chapter an overview of the more recent developments in the structure–activity relationships (SARs) of classical cannabinoids is discussed, especially the profound pharmacological effects produced by various chemical entities in the side chain at C-3, the hydroxyl at C-1, C-11, and hydroxyalkyl chains at C-6. Also cardiovascular studies point to the presence of a novel cannabinoid subtype receptor and the antagonist activity of cannabidiol has opened up new areas for research. Ligands, which had either a unique pharmacological profile, were potent agonists, partial agonists/antagonists, or were CB2 selective, were identified, generating leads with the potential to be drugs in the treatment of various diseases.


Classical cannabinoids Tetrahydrocannabinols Structure activity relationships Endocannabinoid system Cannabinoid receptors Vanilloid receptors Pharmacological activity Cannabinol Cannabidiol Cardiovascular activity