Table 3. Pharmacokinetic Parameters for 1 and 2 after Intravenous and Oral Administration.
1 |
2 |
1 as metabolite of 2 | |||
---|---|---|---|---|---|
parameter | iv | oral | iv | oral | oral |
dose (mg/kg) | 5 | 20 | 5 | 20 | 20 of compound 2 |
Cmax (μM) | 5.98 | 3.54 | 10.4 | ||
Tmax (h) | 3 | 0.5 | 3 | ||
Vd (L/kg) | 0.81 | 11.1 | |||
apparent t1/2 (h) | 7.3 | 6.2 | 10.4 | ||
CLtotal (mL·min–1·kg–1) | 1.3 | 21.8 | |||
AUC0–∞ (min·μmol·L–1) | 8589 | 7249 | 523 | 2152 | 18430 |
bioavailability (%) | 18.4 | 93 |