Table 3. Pharmacokinetic Parameters for 1 following IV and PO Administration to Male Sprague–Dawley Rats.
| route |
|||
|---|---|---|---|
| IV | PO | PO | |
| dose (mg/kg) | 3 | 11 | 27 |
| plasma half-life (h) | 7.0 ± 1.3 | 4.9, 6.1 | 7.4 ± 1.3 |
| plasma clearance (mL/(min kg)) | 147 ± 33 | NAa | NA |
| plasma volume of distribution (L/kg) | 51 ± 10 | NA | NA |
| dose excreted in urine as parent (%) | 9.2, 10.7 | NA | NA |
| blood:plasma | 2.1 | NA | NA |
| Cmax (μM) | NA | 0.07, 0.05 | 0.31 ± 0.03 |
| Tmax (h) | NA | 1.0, 0.8 | 1.0 |
| bioavailability (%) | NA | 17, 15 | 27 ± 4 |
a
NA: not applicable or not available.