Pharmacokinetic parameters for compound 3o and PBTZ169 in ICR mice mollowing intravenous and oral administrationa.
Parameters | 3o-IV | 3o-PO | PBTZ169-IV | PBTZ169-PO | ||||
---|---|---|---|---|---|---|---|---|
Location | Plasma | Tissue | Plasma | Tissue | Plasma | Tissue | Plasma | Tissue |
Dose (mg kg−1) | 10 | 10 | 100 | 100 | 10 | 10 | 100 | 100 |
Terminal T1/2 (h) | 2.62 | 1.75 | 2.40 | 2.84 | 2.67 | 3.16 | 2.09 | 4.23 |
T max (h) | 1.75 | 0.08 | 2.00 | 2.00 | 0.08 | 0.08 | 2.00 | 0.50 |
C max (ng mL−1) | 5674.10 | 8872.56 | 2648.48 | 4578.33 | 15 600.40 | 4208.74 | 2996.34 | 811.35 |
AUC0–∞ (ng mL−1 h) | 3035.87 | 5335.01 | 13 611.26 | 24 194.36 | 9074.85 | 15 146.56 | 18 882.08 | 7841.88 |
V ss (mL kg−1) | 4524.65 | — | — | — | 1154.42 | — | — | — |
Cl (L h−1 kg) | 3.29 | 1.87 | — | — | 1.10 | 0.66 | — | — |
MRT0–∞ (h) | 1.37 | 1.08 | 3.73 | 4.19 | 1.05 | 4.50 | 3.70 | 6.50 |
F (%) | — | — | 44.83 | 45.35 | — | — | 20.81 | 5.18 |
Values are the mean from three animals. Dash indicates that the value was not measured or was not relevant.