Table 3.
compound | f u,plasma a | CLHa (mL/min/kg) | CLpa (mL/min/kg) | t1/2a (h) | Vssa (L/kg) | AUCa (h·ng/mL) | ||
---|---|---|---|---|---|---|---|---|
human | rat | human | rat | |||||
4 | 0.01 | 0.03 | 16.9 | 59.1 | 116 | 1.05 | 5.52 | 28.7 |
33 | 0.19 | 0.26 | 16.0 | 39.0 | 123 | 4.02 | 36.9 | 27.0 |
32 | 0.06 | 0.14 | 14.7 | 46.2 | ||||
29 | 0.05 | 0.15 | 17.3 | 49.2 | ||||
20 | 0.10 | 0.23 | 13.7 | 36.2 | 126 | 4.55 | 44.4 | 26.4 |
fu = Fraction unbound; equilibrium dialysis assay; CLH = hepatic clearance; CLp = plasma clearance; t1/2 = terminal phase plasma half-life; Vss = volume of distribution at steady-state; AUC = area under the curve.