TABLE 1

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 CompoundTransportDonor 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
CarbamazepinePT1036.5 (1.93)19.5 (0.60)0.5338.0 (2.54)20.0 (5.53)0.531.0037.3 (5.60)19.6 (3.85)0.531.00
PropranololPT1019.6 (4.99)20.0 (0.16)1.0223.8 (2.69)20.8 (1.51)0.870.8525.4 (2.51)22.4 (0.59)0.880.86
TrazodonePT1038.5 (3.30)29.4 (1.31)0.7633.0 (2.58)40.4 (3.14)1.221.6137.5 (5.03)27.4 (2.91)0.730.96
AtenololPP1000.22 (0.06)0.28 (0.03)1.270.35 (0.14)0.24 (0.04)0.690.540.14 (0.11)0.20 (0.03)1.431.13
CimetidineEffluxa300.56 (0.14)0.43 (0.03)0.750.06 (0.02)0.41 (0.05)6.408.500.890.15 (0.04)1.25 (0.08)8.3411.11.47
QuinidineEffluxb109.52 (2.53)12.5 (2.49)1.313.77 (0.91)29.1 (1.37)7.735.901.1312.0 (3.48)15.0 (0.48)1.250.95
SulfasalazineEffluxc600.81 (0.30)0.28 (0.05)0.340.30 (0.14)0.17 (0.09)0.561.640.13 (0.11)0.30 (0.05)2.316.790.92
Na-FPP1000.48 (0.09)0.09 (0.08)0.11 (0.04)
  • PP, passive paracellular; PT, passive transcellular.

  • a Efflux mediated by P-gp and BCRP.

  • b Efflux mediated by P-gp.

  • c Efflux mediated by BCRP.