Pharmacokinetic Parameters of 11C-SC-62807 in Wild-Type and Bcrp–/– Mice
Pharmacokinetic parameter | Wild-type mice | Bcrp–/– mice | Ratio of Bcrp–/– to wild-type |
AUCblood,0–30 min (% dose × min/mL) | 42 ± 18 | 93 ± 19* | 2.2 ± 1.1 |
AUCliver,0–30 min (% dose × min/mL) | 369 ± 85 | 535 ± 76† | 1.5 ± 0.4 |
AUCkidney,0–30 min (% dose × min/mL) | 170 ± 36 | 1,119 ± 126‡ | 6.6 ± 1.6 |
Kp,liver,AUC (mL/g of liver) | 8.8 ± 3.0 | 5.6 ± 0.8 | 0.64 ± 0.24 |
Kp,kidney,AUC (mL/g of kidney) | 4.0 ± 1.3 | 11.7 ± 2.3* | 2.9 ± 1.1 |
Xbile,0–30 min (% dose) | 48 ± 3 | 13 ± 2‡ | 0.28 ± 0.04 |
Xurine,0–30 min (% dose) | 26 ± 5 | 3.0 ± 1.7‡ | 0.11 ± 0.07 |
CLbile,blood,0–30 min (mL/min/kg) | 48 ± 19 | 5.1 ± 1.6† | 0.11 ± 0.05 |
CLrenal,blood,0–30 min (mL/min/kg) | 25 ± 8 | 1.2 ± 0.7* | 0.046 ± 0.033 |
CLint,bile,liver (mL/min/kg) | 4.5 ± 0.8 | 1.2 ± 0.1* | 0.26 ± 0.05 |
CLint,urine,kidney (mL/min/kg) | 13 ± 2 | 0.12 ± 0.07* | 0.0088 ± 0.0051 |