Cannabinoid or Related Molecule | PPARα | PPARβ/δ | PPARγ |
---|---|---|---|
μM | |||
Palmitoyl ethanolamide | 3a | >30a | >30a; >60b |
Stearoyl ethanolamide | >30a | N.D. | N.D. |
Oleoyl ethanolamide | 0.12c; 0.12d | 1c | >10c |
Anandamide | >10c; 10 to 30e | N.D. | 8b; 10f |
2-AG | N.D. | >1g | 10f; ∼30h |
Noladin ether | 10 to 30e | N.D. | ∼30h |
Virodhamine | 10 to 30e | N.D. | N.D. |
R-(+)-WIN55212 | 20e | N.D. | N.D. |
Δ9-THC | >100e | N.D. | ∼0.3i |
Cannabidiol | N.D. | N.D. | 5j |
Ajulemic acid | >50j | >50j | 0.6j; 13k |
Rimonabant | Activationl | N.D. | 10l |
AM251 | Activationl | N.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).