TP 003 is a functionally selective GABAA receptor (α3 subtype) partial agonist. Exhibits affinity for the benzodiazepine binding site on human GABAA receptors. Potentiates the GABA (α3 subtype) response selectively with high efficacy. Produces anxiolytic-like effects in rodent behavioral models of anxiety.
| Molecular Weight | 407.39 |
| Formula | C23H16F3N3O |
| CAS Number | 628690-75-5 |
| Solubility (25°C) | DMSO 40.74 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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