PSN-375963 is a selective ligand for the suggested novel cannabinoid receptor GPR119. Initial studies showed that PSN375963 has similar potency and partial efficacy compared to OEA. Further studies revealed that although OEA and PSN375963 are GPR119 agonists, they have divergent effects on insulin secretion, calcium signaling, and cAMP production. Furthermore, we have used the recombinant receptor to discover novel selective small-molecule GPR119 agonists, typified by PSN632408, which suppress food intake in rats and reduce body weight gain and white adipose tissue deposition upon subchronic oral administration to high-fat-fed rats. PSN375963 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.
|Solubility||DMSO >10 mg/mL|
Activation of GPR119 by fatty acid agonists augments insulin release from clonal β-cells and isolated pancreatic islets and improves glucose tolerance in mice.
Moran BM, et al. Biol Chem. 2014 Apr;395(4):453-64. PMID: 24323890.
Endogenous and synthetic agonists of GPR119 differ in signalling pathways and their effects on insulin secretion in MIN6c4 insulinoma cells.
Ning Y, et al. Br J Pharmacol. 2008 Dec;155(7):1056-65. PMID: 18724386.
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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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.
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