Summary of permeability (n = 3), efflux data, and unbound drug fractions in blood and brain homogenate (n = 6)
| Name | Papp, without GF120918 | Mean, with GF120918 | In Vitro Corrections | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| A-to-B | B-to-A | ER | A-to-B | B-to-A | ER | Kbb/ER | Kbba | |||||
| nm/s | ||||||||||||
| Mean | S.D. | Mean | S.D. | Mean | S.D. | Mean | S.D. | |||||
| GSK-1 | 58.1 | 12.1 | 502.3 | 28.6 | 8.7 | 168.3 | 38.1 | 227.0 | 20.5 | 1.3 | 0.351 | 3.56 |
| GSK-2 | 7.2 | 1.2 | 539.3 | 51.0 | 74.9 | 158.0 | 7.5 | 105.3 | 4.7 | 0.7 | 0.040 | 0.23 |
| GSK-3 | 9.0 | 1.8 | 606.3 | 60.1 | 67.6 | 68.7 | 2.4 | 56.7 | 14.8 | 0.8 | 0.056 | 0.41 |
| GSK-4 | 2.3 | 0.6 | 288.7 | 26.3 | 125.5 | 14.7 | 2.1 | 18.3 | 2.5 | 1.2 | 0.012 | -0.07 |
| GSK-5 | 5.0 | 1.0 | 599.7 | 65.5 | 120.7 | 41.9 | 8.1 | 49.4 | 2.6 | 1.2 | 0.048 | 0.31 |
| GSK-6 | 11.3 | 1 | 778.4 | 90.6 | 68.9 | 249.9 | 7.2 | 188.9 | 14.0 | 0.8 | 0.079 | 0.66 |
| GSK-7 | 8.3 | 0.6 | 486.3 | 57.8 | 58.8 | 71.8 | 2.0 | 100.2 | 5.3 | 1.4 | 0.020 | 0.02 |
| GSK-8 | 9.8 | 1.3 | 730.6 | 26.6 | 74.3 | 154.9 | 6.5 | 184.5 | 8.9 | 1.2 | 0.018 | -0.01 |
| GSK-9 | 47.9 | 4.4 | 633.7 | 39.8 | 13.2 | 220.0 | 21.6 | 192.6 | 43.9 | 0.9 | 0.136 | 1.27 |
| GSK-10 | 113.8 | 33 | 763.4 | 33.3 | 6.7 | 349.1 | 29.1 | 383.5 | 18.1 | 1.1 | 0.272 | 2.71 |
| GSK-11 | 103 | 8.1 | 1102.2 | 117.2 | 10.7 | 317.5 | 17.8 | 200.1 | 37.5 | 0.6 | 0.024 | 0.06 |
| GSK-40 | 4.27 | 0.39 | 35.6 | 7.8 | 8.3 | 21.8 | 1.4 | 15.7 | 1.8 | 0.7 | 0.202 | 1.97 |
| GSK-41 | 66.1 | 3.9 | 547.0 | 24.0 | 8.3 | 229.0 | 4.2 | 252.7 | 24.0 | 1.1 | 0.172 | 1.65 |
| Risperidone | 36.0 | 1.0 | 748.4 | 64.0 | 20.8 | 300.3 | 27.9 | 308.6 | 12.1 | 1.0 | 0.036 | 0.20 |
↵ a Pgp substrate correction for Kbb using the regression line derived from Fig. 4 (i.e. y = 10.707x - 0.1949 (R2 = 0.9342)), where y is taken as the Pgp-corrected Kbb and x represents the term Kbb/ER.