Agathadiol, a labdane diterpenoid from juniper berries, is a positive allosteric modulator of CB1R

Fitoterapia. 2021 Nov:155:105059. doi: 10.1016/j.fitote.2021.105059. Epub 2021 Oct 9.


The neutral fraction of a juniper (Juniperus communis L.) berries acetone extract could positively modulate the activity of type 1 - cannabinoid receptor (CB1R). Bioactivity-directed fractionation identified the labdane diterpenoid agathadiol (4) as a positive allosteric modulator of CB1R, while closely related analogues were inactive. Agathadiol (4) is a minor constituent of juniper, but could be more conveniently obtained by semisynthesis from agathic acid (8), a major constituent of Manila copal.

Keywords: Agathadiol; Allosteric ligands; Cannabinoid receptor-1; Juniperus communis; Labdane diterpenoids.

MeSH terms

  • Cannabinoid Receptor Agonists / pharmacology*
  • Dicarboxylic Acids
  • Diterpenes / pharmacology*
  • Fruit / chemistry
  • Juniperus / chemistry*
  • Molecular Structure
  • Receptor, Cannabinoid, CB1
  • Tetrahydronaphthalenes


  • Cannabinoid Receptor Agonists
  • Dicarboxylic Acids
  • Diterpenes
  • Receptor, Cannabinoid, CB1
  • Tetrahydronaphthalenes
  • labdane
  • agathic acid