Table 1.
Compound | Exp. | ERTRQ(‐) | ERTRQ(+) | ERTRQ(‐) ‐ ERTRQ(+) | REF | Kp,uu,brain,pred(method 1) |
Kp,uu,brain,obs (CI95%) |
P/O | |
---|---|---|---|---|---|---|---|---|---|
Individual | Mean ± SD | ||||||||
Verapamil | 1 | 2.94 | 0.76 | 2.18 | 2.20 | 0.17 | 0.17 ± 0.03 | 0.16 (0.13–0.20) | 1.02 |
2 | 2.97 | 0.76 | 2.21 | 2.39 | 0.16 | ||||
3 | 3.59 | 0.71 | 2.88 | 2.37 | 0.13 | ||||
4 | 3.73 | 0.83 | 2.90 | 1.32 | 0.21 | ||||
N‐desmethyl loperamide | 1 | 18.28 | 0.86 | 17.42 | 0.97 | 0.056 | 0.043 ± 0.018 | 0.046 (0.035–0.057) | 0.92 |
2 | 26.21 | 0.82 | 25.39 | 1.83 | 0.021 | ||||
3 | 55.00 | 0.98 | 54.02 | 0.30 | 0.058 | ||||
4 | 119.43 | 0.82 | 118.61 | 0.23 | 0.035 | ||||
Metoclopramide | 1 | 1.87 | 0.70 | 1.17 | 0.30 | 0.74 | 0.74 ± 0.08 | 0.57 (0.46–0.67) | 1.30 |
2 | 1.79 | 0.92 | 0.87 | 0.36 | 0.76 | ||||
3 | 3.56 | 1.03 | 2.53 | 0.24 | 0.63 | ||||
4 | 2.98 | 1.68 | 1.30 | 0.18 | 0.81 |
CI95%, 95% confidence interval; ER, efflux ratio; Exp., experiment; Kp,uu,brain, unbound brain‐to‐plasma concentration ratio; P/O, predicted/observed Kp,uu,brain ratio; REF, relative expression factor (measured by targeted proteomics); TRQ, tariquidar.