GPR119 (previously designated SNORF25) is an orphan G protein-coupled receptor expressed predominantly in the pancreas and gastrointestinal tract in humans and in the brain, pancreas, and gastrointestinal tract in rodents. It mediates a reduction in food intake and body weight gain in rats upon treatment with oleoyl ethanolamide (OEA), an endogenous, potent agonist for PPARα.1,2 PSN375963 is a potent and selective agonist of GPR119 that shows similar potency to OEA at both recombinant murine and human GPR119 receptors, exhibiting EC50 values of 8.4 and 7.9 µM, respectively (EC50 values for OEA are 3.2 and 2.9 µM, respectively).2 These data suggest that PSN375963 may be useful as a therapeutic agent for the treatment of obesity.
1
Fu, J., Gaetani, S., Oveisi, F., et al. Oleylethanolamide regulates feeding and body weight through activation of the nuclear receptor PPAR-α. Nature42590-93(2003).
2
Overton, H.A., Babbs, A.J., Doel, S.M., et al. Deorphanization of a G protein-coupled receptor for oleoylethanolamide and its use in the discovery of small-molecule hypophagic agents. Cell Metab3167-175(2006).
Room temperature
in continental US; may vary elsewhere
SMILES
Copy SMILES to clipboard
CCCCC1CCC(CC1)c1onc(n1)c1ccncc1
Background Reading
Overton, H.A., Babbs, A.J., Doel, S.M., et al. Deorphanization of a G protein-coupled receptor for oleoylethanolamide and its use in the discovery of small-molecule hypophagic agents. Cell Metab3167-175(2006).
Fu, J., Gaetani, S., Oveisi, F., et al. Oleylethanolamide regulates feeding and body weight through activation of the nuclear receptor PPAR-α. Nature42590-93(2003).
PSN375963 is available in the following screening
library: