The Papp coefficient values, ER, and net flux ratio of COMT inhibitors 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.
| Test Compound | 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 | ||||||||
| BIA 9-1059 | 60 | 1.29 (0.27) | 1.47 (0.18) | 1.14 | 1.22 (0.23) | 0.35 (0.07) | 0.29 | 0.25 | — | 0.24 (0.08) | 1.69 (0.44) | 7.04 | 6.18 | 0.64 |
| BIA 9-1079 | 10 | 5.23 (2.75) | 8.47 (0.91) | 1.62 | 3.47 (1.77) | 15.9 (4.19) | 4.58 | 2.83 | 0.60 | 7.14 (4.63) | 13.6 (1.74) | 1.90 | 1.17 | — |
| Entacapone | 30 | 6.33 (0.37) | 6.02 (0.39) | 0.95 | 3.51 (1.33) | 1.29 (0.36) | 0.37 | 0.39 | — | 0.98 (0.19) | 11.1 (0.92) | 11.3 | 11.9 | 1.06 |
| Nebicapone | 10 | 24.6 (1.45) | 17.6 (4.18) | 0.72 | 23.9 (7.06) | 14.3 (2.60) | 0.60 | 0.83 | — | 5.40 (0.09) | 11.6 (0.63) | 2.15 | 2.99 | 1.07 |
| Opicapone | 30 | 4.72 (2.33) | 6.08 (0.38) | 1.29 | 2.56 (1.08) | 2.50 (0.39) | 0.98 | 0.76 | — | 0.42 (0.09) | 9.73 (1.13) | 23.2 | 18.0 | 1.58 |
| Tolcapone | 10 | 26.6 (5.07) | 20.6 (3.87) | 0.77 | 24.3 (2.84) | 19.5 (3.37) | 0.80 | 1.04 | — | 28.3 (2.93) | 23.7 (1.65) | 0.84 | 1.09 | — |