Pharmacokinetic Parameters | B6 | B6 + GF120918 | Mrp2KO | Mrp2KO + GF120918 |
---|---|---|---|---|
Css, out (pmol/ml) | 329 ± 40 | 371 ± 25 | 398 ± 40* | 445 ± 15* |
Cliver (pmol/ml) | 16260 ± 1470 | 10320 ± 2590¶ | 5913 ± 259* | 4426 ± 641* |
Cliver, unbound (pmol/ml) | 2428 ± 219 | 1541 ± 387¶ | 883 ± 337* | 661 ± 96* |
Cliver, unbound/Css, out | 7.49 ± 1.43 | 4.14 ± 0.69¶ | 2.27 ± 0.97* | 1.49 ± 0.21* |
Extraction ratio | 0.34 ± 0.08 | 0.26 ± 0.05 | 0.21 ± 0.08* | 0.11 ± 0.03* |
Biliary excretion rate (pmol/min/g liver) | 122 ± 34 | 66.8 ± 7.9¶ | 18.4 ± 2.2* | 11.2 ± 1.7*¶ |
(ml/h/g liver) | 3.01 ± 0.65 | 2.70 ± 0.64 | 1.27 ± 0.31* | 1.03 ± 0.18* |