Table 2. Pharmacokinetic Parameters of Compounds 3 and 4.
| compd | rat iv PKa |
rat po PKa |
mouse po PKb |
||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| dosec (mg/kg) | CL (L/h/kg) | Vss (L/kg) | t1/2 (h) | dosed (mg/kg) | Cmax (μM) | t1/2 (h) | AUC (μM·h) | F (%) | dosee (mg/kg) | Cmax (μM) | t1/2 (h) | AUC (μM·h) | |
| 3 | 0.5 | 0.52 | 2.32 | 4.3 | 2.0 | 0.37 | 4.6 | 2.71 | 29 | 30 | 7.88 | 3.7 | 63.3 |
| 4 | 0.5 | 0.75 | 2.85 | 3.6 | 2.0 | 0.45 | 2.9 | 1.98 | 33 | 30 | 6.09 | 3.5 | 36.3 |
a
Pharmacokinetic parameters following administration of compounds 3 or 4 in male Sprague–Dawley rats: 2 animals per study.
b
Pharmacokinetic parameters following administration of compound 3 or 4 in male Mouse_CD1: 3 animals per study.
c
Dosed as a solution in DMSO.
d
Dosed in 1% Tween 80/2% HPMC/97% water/MSA pH 2.2.
e
Dosed in 10.0% Pluronic F68/30.0% HPBCD/60.0% water/MSA pH 2.5.