Cannabinoid receptor 2 (CB2) agonists and antagonists: a patent update

Expert Opin Ther Pat. 2016 Jul;26(7):843-56. doi: 10.1080/13543776.2016.1193157. Epub 2016 Jun 7.


Introduction: Modulation of the CB2 receptor is an interesting approach for pain and inflammation, arthritis, addictions, neuroprotection, and cancer, among other possible therapeutic applications, and is devoid of central side effects.

Areas covered: This review highlights the novel scaffolds for CB2 ligands and the diverse therapeutic applications for CB2 modulators disclosed in patents published since 2012.

Expert opinion: Structural diversity of CB2 modulator scaffolds characterized the patent literature. Several CB2 agonists reached clinical Phase II for pain management and inflammation. Other therapeutic applications need to be explored such as neuroprotection and/or neurodegeneration.

Keywords: Cannabinoid receptor 2; HIV; cancer; endometriosis; inflammation; organ transplant; osteoarthritis; pain.

Publication types

  • Review

MeSH terms

  • Animals
  • Cannabinoid Receptor Agonists / adverse effects
  • Cannabinoid Receptor Agonists / pharmacology*
  • Cannabinoid Receptor Agonists / therapeutic use
  • Cannabinoid Receptor Antagonists / adverse effects
  • Cannabinoid Receptor Antagonists / pharmacology*
  • Cannabinoid Receptor Antagonists / therapeutic use
  • Drug Design*
  • Humans
  • Inflammation / drug therapy
  • Inflammation / physiopathology
  • Pain / drug therapy
  • Pain / physiopathology
  • Patents as Topic
  • Receptor, Cannabinoid, CB2 / agonists
  • Receptor, Cannabinoid, CB2 / antagonists & inhibitors


  • Cannabinoid Receptor Agonists
  • Cannabinoid Receptor Antagonists
  • Receptor, Cannabinoid, CB2