TABLE 2

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 CompoundDonor SolutionMDCK IIMDCK-MDR1Net Flux RatioMDCK-BCRPNet Flux Ratio
Papp,AP-BL (×10−6)Papp,BL-AP (×10−6)ERPapp,AP-BL (×10−6)Papp,BL-AP (×10−6)ERWithout VerapamilWith VerapamilPapp,AP-BL (×10−6)Papp,BL-AP (×10−6)ERWithout Ko143With Ko143
μMcm/scm/scm/scm/scm/scm/s
BIA 9-1059601.29 (0.27)1.47 (0.18)1.141.22 (0.23)0.35 (0.07)0.290.250.24 (0.08)1.69 (0.44)7.046.180.64
BIA 9-1079105.23 (2.75)8.47 (0.91)1.623.47 (1.77)15.9 (4.19)4.582.830.607.14 (4.63)13.6 (1.74)1.901.17
Entacapone306.33 (0.37)6.02 (0.39)0.953.51 (1.33)1.29 (0.36)0.370.390.98 (0.19)11.1 (0.92)11.311.91.06
Nebicapone1024.6 (1.45)17.6 (4.18)0.7223.9 (7.06)14.3 (2.60)0.600.835.40 (0.09)11.6 (0.63)2.152.991.07
Opicapone304.72 (2.33)6.08 (0.38)1.292.56 (1.08)2.50 (0.39)0.980.760.42 (0.09)9.73 (1.13)23.218.01.58
Tolcapone1026.6 (5.07)20.6 (3.87)0.7724.3 (2.84)19.5 (3.37)0.801.0428.3 (2.93)23.7 (1.65)0.841.09