Medicinal chemistry of cannabinoids

Clin Pharmacol Ther. 2015 Jun;97(6):553-8. doi: 10.1002/cpt.115. Epub 2015 Apr 16.


The endocannabinoid system comprises the two well characterized Gi/o -protein coupled receptors (cannabinoid receptor 1 (CB1) and CB2), their endogenous lipid ligands, and the enzymes involved in their biosynthesis and biotransformation. Drug discovery efforts relating to the endocannabinoid system have been focused mainly on the two cannabinoid receptors and the two endocannabinoid deactivating enzymes fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MGL). This review provides an overview of cannabinergic agents used in drug research and those being explored clinically.

Publication types

  • Review

MeSH terms

  • Amidohydrolases / antagonists & inhibitors
  • Cannabinoids / therapeutic use*
  • Chemistry, Pharmaceutical
  • Drug Discovery
  • Humans
  • Monoacylglycerol Lipases / antagonists & inhibitors
  • Receptor, Cannabinoid, CB1 / agonists
  • Receptor, Cannabinoid, CB1 / antagonists & inhibitors
  • Receptor, Cannabinoid, CB1 / physiology
  • Receptor, Cannabinoid, CB2 / agonists
  • Receptor, Cannabinoid, CB2 / physiology


  • Cannabinoids
  • Receptor, Cannabinoid, CB1
  • Receptor, Cannabinoid, CB2
  • Monoacylglycerol Lipases
  • Amidohydrolases
  • fatty-acid amide hydrolase