PSN632408, a selective, orally active GPR119 agonist, shows similar potency to OEA at both recombinant mouse and human GPR119 receptors (EC50=5.6 and 7.9 uM, respectively). PSN632408 can stimulate β-cell replication and improve islet graft function. PSN632408 has the potential for the research of obesity and related metabolic disorders[1][2].
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].
PSN632408 (100 mg/kg; p.o.; daily for 14 days) suppresses food intake in rats and reduce body weight gain and white adipose tissue deposition upon subchronic oral administration to high-fat-fed rats[1].
| Animal Model: | Diet-induced obese (DIO) rats[1] |
| Dosage: | 100 mg/kg |
| Administration: | P.o.; daily for 14 days |
| Result: | The mean daily food intake was decreased by 10% during the first week of dosing and 15% during the second week. Body weight gain was significantly attenuated from day 6 onward with some evidence of weight loss.
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[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
