TABLE 8

Potency of cannabinoids and endocannabinoid-like molecules at peroxisome proliferator-activated receptors (EC50 or IC50 values or effective concentrations)

Cannabinoid or Related MoleculePPARαPPARβ/δPPARγ
μM
Palmitoyl ethanolamide3a>30a>30a; >60b
Stearoyl ethanolamide>30aN.D.N.D.
Oleoyl ethanolamide0.12c; 0.12d1c>10c
Anandamide>10c; 10 to 30eN.D.8b; 10f
2-AGN.D.>1g10f; ∼30h
Noladin ether10 to 30eN.D.∼30h
Virodhamine10 to 30eN.D.N.D.
R-(+)-WIN5521220eN.D.N.D.
Δ9-THC>100eN.D.∼0.3i
CannabidiolN.D.N.D.5j
Ajulemic acid>50j>50j0.6j; 13k
RimonabantActivationlN.D.10l
AM251ActivationlN.D.10l
  • N.D., no data.

  • a EC50 reporter gene assay in HeLa cells expressing recombinant receptors (Lo Verme et al., 2005a).

  • b EC50 reporter gene assay in COS cells expressing recombinant receptors (Bouaboula et al., 2005).

  • c EC50 reporter gene assay in HeLa cells expressing recombinant receptors (Fu et al., 2003).

  • d EC50 reporter gene assay in MCF7 cells expressing recombinant receptors (Alvarado et al., 2008).

  • e IC50 competition for fluorescent ligand occupancy of ligand binding domain (Sun et al., 2007a).

  • f IC50 competition for fluorescent ligand occupancy of ligand binding domain (Bouaboula et al., 2005).

  • g EC50 reporter gene assay in human umbilical vein endothelial cells in the presence of a COX-2 inhibitor (Ghosh et al., 2007).

  • h EC50 reporter gene assay in 3T3-L1 cells expressing recombinant receptors (Rockwell et al., 2006).

  • i EC50 reporter gene assay in HEK293 cells expressing recombinant receptors (O'Sullivan et al., 2005).

  • j IC50 competition for fluorescent ligand occupancy of ligand binding domain (O'Sullivan et al., 2009b).

  • k EC50 reporter gene assay in HEK293 cells expressing recombinant receptors (Liu et al., 2003).

  • l Effective concentration in reporter gene assay in HEK293 cells expressing recombinant receptors; ligand concentration(s) for PPARα activation not published (O'Sullivan et al., 2006; Sun et al., 2007b).