PF-04995274 is a potent partial agonist of serotonin 5HT4 receptor with Ki = 0.15 - 0.46 nM for 5-HT4 isoforms a, b, d and e. 5-HT4 agonists modulate cholinergic function are being studied as possible treatment for cognitive disorders associated with Alzheimer′s Disease. PF-04995274 is brain penetrant and was shown to increase brain acetylcholine levels and reversed scopolamine-induced learning deficits in the rat Morris water maze test.
| Molecular Weight | 432.51 |
| Formula | C23H32N2O6 |
| CAS Number | 1331782-27-4 |
| Form | Solid |
| Solubility (25°C) | DMSO: 20 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.
[1] Briana K Chen, et al. Prophylactic efficacy of 5-HT 4 R agonists against stress
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