Table 4. PK Profiles of 11k–n and 12b, 12e Dosed Orally in Mice at 50 mg/kg (n = 3)a.
compd. | T1/2 (h) | Tmax (h) | Cmax (ng/mL) | AUC0-inf (h·ng/mL) | MRT (h) |
---|---|---|---|---|---|
11l | 10.66 ± 5.62* | 1.00 ± 0 | 1682 ± 307 | 24619 ± 3478** | 15.9 ± 8.66* |
11m | 3.59 ± 0.64 | 1.33 ± 0.58 | 2700 ± 933* | 28716 ± 9878* | 6.07 ± 0.35** |
11n | 3.53 ± 1.63 | 0.67 ± 0.29 | 901 ± 110 | 4871 ± 935 | 4.83 ± 0.66 |
11o | 4.68 ± 0.92* | 0.50 ± 0 | 426 ± 243* | 2599 ± 1220 | 5.80 ± 0.84* |
12b | 3.46 ± 3.23 | 0.67 ± 0.29 | 17.6 ± 5.41** | 41.8 ± 33.0** | 5.20 ± 4.50 |
12f | 3.11 ± 0.35 | 1.08 ± 0.88 | 1234 ± 159 | 6024 ± 379 | 4.00 ± 0.85 |
PBTZ169 | 2.87 ± 1.03 | 0.83 ± 0.29 | 1300 ± 422 | 5478 ± 1730 | 3.73 ± 0.94 |
Note: noncompartmental calculations gave these parameter estimates. *P < 0.05. **P < 0.01, one-tail t test compared with PBTZ169.