TABLE 2.
Efflux ratio of [3H]prazosin, [14C]zidovudine, [3H]abacavir, and [14C]imitanib in MDCK wild-type, MDCK Bcrp1 cells, and MDCK Bcrp1 cells in the presence of the inhibitors Ko143, GF120918, nelfinavir, and Pluronic P85
Efflux ratio = Papp B-to-A transport/Papp A-to-B transport.
| MDCK WT | MDCK Bcrp1 | MDCK Bcrp1 + Ko143 (200 nM) | MDCK Bcrp1 + GF120918 (5 μM) | MDCK-Bcrp1 + Nelfinavir (25 μM) | MDCK-Bcrp1 +P85 (0.01% w/v) | |
|---|---|---|---|---|---|---|
| Prazosin | 1.3 | 10.5 | 1.4 (complete)a | 5.0 (partial)b | 9.8 (N.S.)c | 12.5 (N.S.) |
| Zidovudine | 0.9 | 10 | 0.8 (complete) | 1.3 (complete) | 1.6 (complete) | 4.4 (partial) |
| Abacavir | 1.3 | 27 | 1.1 (complete) | 1.4 (complete) | 1.5 (complete) | 7.8 (partial) |
| Imatinib (STI-571) | 1.8 | 62 | 2.2 (complete) | 27.5 (partial) | 24.7 (partial) | 57 (N.S.) |
WT, wild type; N.S., not significant.
a
Efflux ratio in the Bcrp1-transfected cells reduced by at least 85%.
b
Efflux ratio reduced by at least 50% but less than 85%.
c
No significant reduction in efflux ratio.