Bidirectional Papp coefficient, ER, and net flux ratio of reference compounds across MDCK II, MDCK-MDR1, and MDCK-BCRP cell monolayers
The Papp values are indicated from the AP-BL and BL-AP compartments and are expressed as mean (S.D.) (n = 3). ERs and net flux ratios greater than 2 are marked in bold. Transport classification according to Mahar Doan et al. (2002), Pavek et al. (2005), Wang et al. (2005), Feng et al. (2008), and Urquhart et al. (2008).
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) | — | — | — | — |