Canna~Fangled Abstracts

The Structure-Function Relationships of Classical Cannabinoids: CB1/CB2 Modulation.

By June 28, 2016 No Comments
2016 Jun 28;8:17-39. doi: 10.4137/PMC.S32171. eCollection 2016.


PM 1aThe cannabinoids are members of a deceptively simple class of terpenophenolic secondary metabolites isolated from Cannabis sativa highlighted by (-)-Δ(9)-tetrahydrocannabinol (THC), eliciting distinct pharmacological effects mediated largely by cannabinoid receptor (CB1 or CB2) signaling. Since the initial discovery of THC and related cannabinoids, synthetic and semisynthetic classical cannabinoid analogs have been evaluated to help define receptor binding modes and structure-CB1/CB2 functional activity relationships. This perspective will examine the classical cannabinoids, with particular emphasis on the structure-activity relationship of five regions: C3 side chain, phenolic hydroxyl, aromatic A-ring, pyran B-ring, and cyclohexenyl C-ring. Cumulative structure-activity relationship studies to date have helped define the critical structural elements required for potency and selectivity toward CB1 and CB2 and, more importantly, ushered the discovery and development of contemporary nonclassical cannabinoid modulators with enhanced physicochemical and pharmacological profiles.


Cannabis sativa; cannabidiol; classical cannabinoids; phytocannabinoids; tetrahydrocannabinol

PMID: 27398024


DOI: 10.4137/PMC.S32171
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