Table 2. Effect of various compounds on ATP-dependent [14C]PAH transport by MRP2 and MRP4a

CompoundConcentration (μM)MRP2 (% of control)MRP4 (% of control)
a Sf9-MRP4 and Sf9-MRP2 crude membrane vesicles were incubated for 5 min with 100 μM [14C]PAH, in the absence (control) or presence of various compounds. Data are means ± SE from at least three experiments performed in triplicate. Results were tested using one-way ANOVA with Bonferroni’s correction.
*P < 0.05, **P < 0.01, ***P < 0.001 versus control (no inhibitor). Abbreviations: MK571, (E)-3-[[[3-[2-(7-chloro-2-quinolinyl)ethenyl]phenyl][[3-(dimethyl amino)-3-oxopropyl]thio]methyl]thio]-propanoic acid; PMEA, 9-(2-phosphorylmethoxyethyl) adenine; PMPA, (R)-9-(2)-phosphonylmethoxypropyl) adenine; AZTMP, 3′-azido-2′,3′-dideoxythymidine-5′-monophosphate; acyclovir, 2-amino-1,9-dihydro-9-[(2-hydroxyethoxy)methyl]-6H-purin-6-one, n.d., not determined.
b Transport rates in the absence of inhibitor: 2.5 ± 0.3 (MRP2) and 8.0 ± 0.5 pmol · mg−1 · min−1 (MRP4).
No inhibitor100b100b
MK5711051 ± 2066 ± 16
10010 ± 27**47 ± 12**
10001 ± 21***12 ± 13***
Sulfinpyrazone10178 ± 17*69 ± 6*
100119 ± 2259 ± 4***
Dipyridamole142 ± 19*103 ± 6
2568 ± 2150 ± 5***
Probenecid10170 ± 15*121 ± 8
100121 ± 18107 ± 4
100068 ± 1453 ± 2***
Uric acid1000n.d.70 ± 5*
PMPA1000n.d.88 ± 5
PMEA1000n.d.71 ± 9
AZTMP100n.d.59 ± 4***
Acyclovir100n.d.39 ± 12***
Indocyanine green100n.d.8 ± 4***