Table 5. Pharmacokinetics in Rat.
| IV |
PO |
|||||||
|---|---|---|---|---|---|---|---|---|
| compd | cLogP | Cl (L/h/kg) | Vss (L/kg) | T1/2 (h) | Cmax (ng/mL) | AUClast (ng/mL·h) | T1/2 (h) | F (%) |
| 4a | 2.24 | 3.9 | 5.42 | 2.4 | 175 | 880 | 2.8 | 35 |
| 9b | 1.90 | 3.67 | 2.78 | 0.8 | 86 | 249 | 1.5 | 12 |
| 10a | 2.40 | 5.44 | 5.89 | 1.2 | 198 | 896 | 3.3 | 48 |
| 18a | 1.68 | 5.04 | 4.55 | 1.1 | 291 | 541 | 1.6 | 28 |
| 27c | 2.48 | 2.40 | 6.17 | 1.83 | 1250 | 3980 | 2.4 | 97 |
| 29d | 3.26 | 2.16 | 12.2 | 4.72 | 256 | 1610 | 4.4 | 89 |
| 30d | 0.2 | 1.65 | 1.02 | 2.48 | 3.52 | 19.5 | 1.9 | <1 |
| 31a | 1.11 | 4.39 | 4.22 | 0.8 | 103 | 209 | 3.7 | 9 |
Dose: po at 10 mg/kg; iv at 5 mg/kg (n = 3).
Dose: po at 8 mg/kg; iv at 4 mg/kg (n = 3).
Dose: po at 10 mg/kg; iv at 10 mg/kg (n = 3).
Dose: po at 4 mg/kg; iv at 2 mg/kg (n = 3).