Table 2. Rat Pharmacokinetic Properties of 1a, 2b, 2d, 3, 5b, and 6.
compd/route/dose | Cmax (nM) | AUC0–24 (μM·h) | T1/2 (h) | Cl (mL/min/kg) | Vss (L/kg) | F (%) |
---|---|---|---|---|---|---|
1a/iv/2 mg/kg | 5.1 | 43 | 11.3 | |||
1a/po/10 mg/kg | 500 | 3.79 | 51 | |||
2b/iv/2 mg/kg | 3.6 | 31 | 5.4 | |||
2b/po/10 mg/kg | 1632 | 10.1 | 88 | |||
2d/iv/2 mg/kg | 4.5 | 25 | 7.1 | |||
2d/po/10 mg/kg | 1765 | 10.2 | 79 | |||
3/iv/2 mg/kg | 5.8 | 36 | 13.5 | |||
3/po/11.5 mg/kg | 1868 | 11.9 | 100 | |||
5b/iv/2 mg/kg | 2.7 | 75 | 10 | |||
5b/po/10 mg/kg | 720 | 3.10 | 66 | |||
6/iv/2 mg/kg | 3.7 | 157 | 20.7 | |||
6/po/13 mg/kg | 478 | 2.56 | 100 |