TABLE 3

Plasma, brain, and CSF AUC and their unbound ratios (mean and S.D.) after cassette dosing in wild-type and Mdr1a knockout rats from study 2

Wild-Type RatsMdr1a Knockout Rats
CompoundAUCpAUCbAUCCSFKp,uu,brainKp,uu,CSFCub/CCSFAUCpAUCbAUCCSFKp,uu,brainKp,uu,CSFCub/CCSF
ng⋅h/mlng⋅h/ml
Amprenavir2676.347.270.0160.270.062 36610811.70.200.310.65
 S.D.374.982.890.0140.120.05581234.20.080.140.30
Citalopram43.12338.130.720.810.8850.788020.32.31.71.3
 S.D.10.2461.760.230.260.2710.01207.40.60.70.5
Digoxin158041.529.30.0150.0650.2318708531780.2550.3310.772
 S.D.32030.96.70.0110.0210.18380105540.0670.1270.255
Elacridar0.8861.28BLLOQ0.39NANA0.3722.60BLLOQ1.9NANA
 S.D.0.2890.26NA0.30NANA0.1741.13NA1.7NANA
Imatinib1266.701.340.140.540.2615125.53.210.441.10.41
 S.D.422.240.480.070.260.13243.40.900.090.30.13
Ko143BLLOQBLLOQBLLOQNANANABLLOQBLLOQBLLOQNANANA
 S.D.NANANANANANANANANANANANA
Loperamide38.63.590.2040.0130.120.1130.038.61.020.180.790.23
 S.D.5.61.120.2800.0050.170.154.74.50.310.040.280.08
Prazosin14026.54.080.0920.130.7117060.112.70.170.330.51
 S.D.325.41.420.0300.050.29225.92.90.030.090.14
Quinidine14829.98.850.0380.220.17182198047.42.00.942.14
 S.D.235.02.680.0130.070.073223012.20.70.300.81
Sulfasalazine393BLLOQBLLOQNANANA437BLLOQBLLOQNANANA
 S.D.47NANANANANA101NANANANANA
Verapamil15574.35.540.180.590.31182162018.53.41.72.0
 S.D.2116.81.920.050.220.13323307.61.00.80.9
  • BLLOQ, below the lower limit of quantitation; NA, not applicable.