PSN632408 is an optimized agonist of GPR119 receptors that shows similar potency to OEA at both recombinant mouse and human GPR119 receptors, exhibiting EC50 values of 5.6 and 7.9 µM, respectively (EC50 values for OEA are 3.2 and 2.9 µM, respectively). 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.PSN632408 may be useful as a therapeutic agent for the treatment of obesity.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Deorphanization of a G protein-coupled receptor for oleoylethanolamide and its use in the discovery of small-molecule hypophagic agents.
Overton HA, et al. Cell Metab. 2006 Mar;3(3):167-75. PMID: 16517404.
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