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Kavalactones And The Endocannabinoid System: The Plant-Derived Yangonin Is A Novel Cb1 Receptor Ligand

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By the time it's all said and done, I bet they find cannabinoid receptor ligands in a large variety of natural sources. It makes much more sense from and evolutionary viewpoint, compared to the emphasis on cannabis. I also think the understanding that phytocannabinoids are prevalent throughout nature will help ease minds in regards to the legality of cannabis. Anyway, here's a study showing that kava contains a newly identified cannabinoid receptor ligand in a plant well know for its effects. 





To investigate the possible interactions between kavalactone-based molecules and proteins of the endocannabinoid system and provide novel and synthetically accessible structural scaffolds for the design of cannabinoid receptor ligands sharing pharmacological properties with kavapyrones, a preliminary SAR analysis was performed on five commercially available natural kavalactones and nine kavalactone-analogues properly synthesized. These compounds were investigated for assessing their cannabinoid receptor binding affinity and capability of inhibiting the activity of the two major metabolic enzymes of the endocannabinoid system, fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL). Among the molecules tested, only yangonin exhibited affinity for the human recombinant CB1 receptor with a Ki = 0.72 μM and selectivity vs. the CB2 receptor (Ki > 10 μM). None of the compounds exhibited strong inhibitory effects on the two enzymes analyzed. The CB1 receptor affinity of yangonin suggests that the endocannabinoid system might contribute to the complex human psychopharmacology of the traditional kava drink and the anxiolytic preparations obtained from the kava plant.




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