TABLE 3

Transport and permeability of probe substrates across the MDR1-MDCKII cells


Compound

Papp A→B

Mass Balance A→B

Papp B→A

Mass Balance B→A

B→A/A→B Ratio
nm/s nm/s
Digoxina 3.07 ± 0.30b 88.5 159 ± 17 95.4 51.7
Digoxin + GF120918c 11.9 ± 0.6 81.0 15.9 ± 1.5 80.4 1.33
Prazosind 165 ± 28 98.1 482 ± 56 102 2.95
Prazosin + GF120918 273 ± 29 85.4 283 ± 25 93.4 1.04
Vinblastined 8.46 ± 3.66 121 474 ± 42 121 56.0
Vinblastine + GF120918 42.0 ± 4.2 113 97.4 ± 12.2 117 2.32
Colchicined,e 63.4 ± 1.6 107 220 ± 8 105 3.46
Colchicine + GF120918
75.1 ± 4.0
101
53.4 ± 3.0
102
0.71
  • a 0.043 μM concentration was used for probe substrate; time 90 min.

  • b Average ± SD; n ≥ 3.

  • c 5 μM concentration was used for GF120918.

  • d 1 μM concentration was used for probe substrate; time 90 min.

  • e Experiment time of 240 min was used for colchicine.