PSN632408 is a novel, selective and small-molecule agonist of human and mouse GPR119 with EC50 values of 5.6±0.99 μM and 7.9±0.7 μM, respectively [1].
PSN632408 has been reported to activate human and mouse GPR119 in a yeast fluorimetric assay with EC50 of 5.6±0.99 μM and 7.9±0.7 μM, respectively. In HEK-OSGPR116 cells, cAMP level was dose-dependently increased by PSN632408 with an EC50 of 1.9±0.14 μM.. In vivo, PSN632408 induced food intake reduction by using a rat feeding model and acute hypophagic effects in dose-dependence [1].
References:
[1] Overton HA1, Babbs AJ, Doel SM, Fyfe MC, Gardner LS, Griffin G, Jackson HC, Procter MJ, Rasamison CM, Tang-Christensen M, Widdowson PS, Williams GM, Reynet C.Deorphanization of a G protein-coupled receptor for oleoylethanolamide and its use in the discovery of small-molecule hypophagic agents. Cell Metab. 2006 Mar;3(3):167-75