Reference Compound | Transport | Donor Solution | MDCK II | MDCK-MDR1 | Net Flux Ratio | MDCK-BCRP | Net Flux Ratio | ||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Papp,AP-BL (×10−6) | Papp,BL-AP (×10−6) | ER | Papp,AP-BL (×10−6) | Papp,BL-AP (×10−6) | ER | Without Verapamil | With Verapamil | Papp,AP-BL (×10−6) | Papp,BL-AP (×10−6) | ER | Without Ko143 | With Ko143 | |||
μM | cm/s | cm/s | cm/s | cm/s | cm/s | cm/s | |||||||||
Carbamazepine | PT | 10 | 36.5 (1.93) | 19.5 (0.60) | 0.53 | 38.0 (2.54) | 20.0 (5.53) | 0.53 | 1.00 | — | 37.3 (5.60) | 19.6 (3.85) | 0.53 | 1.00 | — |
Propranolol | PT | 10 | 19.6 (4.99) | 20.0 (0.16) | 1.02 | 23.8 (2.69) | 20.8 (1.51) | 0.87 | 0.85 | — | 25.4 (2.51) | 22.4 (0.59) | 0.88 | 0.86 | — |
Trazodone | PT | 10 | 38.5 (3.30) | 29.4 (1.31) | 0.76 | 33.0 (2.58) | 40.4 (3.14) | 1.22 | 1.61 | — | 37.5 (5.03) | 27.4 (2.91) | 0.73 | 0.96 | — |
Atenolol | PP | 100 | 0.22 (0.06) | 0.28 (0.03) | 1.27 | 0.35 (0.14) | 0.24 (0.04) | 0.69 | 0.54 | — | 0.14 (0.11) | 0.20 (0.03) | 1.43 | 1.13 | — |
Cimetidine | Effluxa | 30 | 0.56 (0.14) | 0.43 (0.03) | 0.75 | 0.06 (0.02) | 0.41 (0.05) | 6.40 | 8.50 | 0.89 | 0.15 (0.04) | 1.25 (0.08) | 8.34 | 11.1 | 1.47 |
Quinidine | Effluxb | 10 | 9.52 (2.53) | 12.5 (2.49) | 1.31 | 3.77 (0.91) | 29.1 (1.37) | 7.73 | 5.90 | 1.13 | 12.0 (3.48) | 15.0 (0.48) | 1.25 | 0.95 | — |
Sulfasalazine | Effluxc | 60 | 0.81 (0.30) | 0.28 (0.05) | 0.34 | 0.30 (0.14) | 0.17 (0.09) | 0.56 | 1.64 | — | 0.13 (0.11) | 0.30 (0.05) | 2.31 | 6.79 | 0.92 |
Na-F | PP | 100 | 0.48 (0.09) | — | — | 0.09 (0.08) | — | — | — | — | 0.11 (0.04) | — | — | — | — |