TABLE 1

Plasma and liver concentrations (mean ± S.D., n = 3 mice/strain/time point) and liver-to-plasma concentration ratio (Kp,liver) following an s.c. administration of the model compounds at 3 mg/kg to 4- to 6-week-old male Oatp1b2 KO and WT mice


Compound

Time

KO Concentration

KO

WT Concentration

WT
Plasma
Liver
Kp, liver
Plasma
Liver
Kp,liver
h ng/ml ng/ml ng/ml ng/ml
Rifampicin 0.5 840 ± 51 13000 ± 1800 2.5 ± 0.3* 3200 ± 872 30000 ± 4300 9.4 ± 1.3
2 6700 ± 2000 16000 ± 400 2.6 ± 0.6* 3600 ± 470 37000 ± 2300 11 ± 2
Rifamycin SV 0.5 2100 ± 480 20000 ± 2500 9.2 ± 0.7 670 ± 180 14000 ± 3600 23 ± 12
2 750 ± 21 9200 ± 4400 12 ± 6 120 ± 67 5200 ± 2700 54 ± 35
Cerivastatin 0.5 1100 ± 210 620 ± 84 0.80 ± 0.45 840 ± 250 900 ± 300 1.2 ± 0.6
2 293 ± 77 120 ± 38 0.25 ± 0.14* 300 ± 42 140 ± 79 0.47 ± 0.30
Lovastatin acid 0.5 380 ± 6 5700 ± 440 16 ± 1* 260 ± 47 6300 ± 930 25 ± 4
2 50 ± 2 1200 ± 64 22 ± 3* 35 ± 7 1200 ± 390 36 ± 6
Pravastatin 0.5 690 ± 160 2100 ± 820 3.0 ± 1.4 580 ± 71 1300 ± 530 2.3 ± 0.8
2 120 ± 11 500 ± 97 4.3 ± 0.5 340 ± 190 380 ± 53 1.7 ± 1.4
Simvastatin acid 0.5 580 ± 45 1700 ± 290 3.1 ± 0.6 650 ± 170 2600 ± 1100 4.3 ± 2.2

2
150 ± 25
600 ± 110
4.2 ± 1.2
16 ± 49
970 ± 180
5.9 ± 0.59
  • * Student's t test shows P < 0.05.