The biosynthesis of cannabigerol begins by loading hexanoyl-CoA onto a polyketide synthase assembly protein and subsequent condensation with three molecules of malonyl-CoA. This polyketide is cyclized to olivetolic acid via olivetolic acid cyclase, and then prenylated with a ten carbon isoprenoid precursor, geranyl pyrophosphate, using an aromatic prenyltransferase enzyme, geranyl-pyrophosphate—olivetolic acid geranyltransferase, to biosynthesize cannabigerolic acid, which can then be decarboxylated to yield cannabigerol.
Cannabigerol is under laboratory research to determine its pharmacological properties and potential effects in disease conditions. Contrary to the major psychoactive cannabinoid THC, cannabigerol antagonizes CB1 receptors and is both an alpha2-adrenoceptor agonist and moderate 5HT1A receptor antagonist. Cannabigerol displays CB1 and CB2 binding affinity, and has been evaluated in laboratory models of colitis.