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.
| Molecular Weight | 285.38 |
| Formula | C17H23N3O |
| CAS Number | 388575-52-8 |
| Solubility (25°C) | DMSO >10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
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