Table 3.
Pharmacokinetic parameters obtained in the rat following oral administration in receptor occupancy studies and satellite oral pharmacokinetic studies
| Compound | ka (1 min−1) | kel (1 min−1) | Vd/F (L·kg−1) | Rat PPB % (Fu) |
|---|---|---|---|---|
| PF-4850890 | 0.0175 | 0.00219 | 5.09 | 99.3 (0.007) |
| PF-4734666 | 0.0381 | 0.00099 | 7.70 | 98.5 (0.015) |
| R121919 | 0.125 | 0.00646 | 25.6 | 99.8 (0.005) |
| DMP904 | 0.0628 | 0.00143 | 8.63 | 99.4 (0.006) |
Ka = absorption rate constant, kel = elimination rate constant, Vd/F = oral volume of distribution, PPB = plasma protein binding, Fu = fraction unbound in the plasma.