TABLE 3

Inhibitory effects of anions and cations on the uptake of [3H]bumetanide by MCT6

Uptake rate of 0.1 μM [3H]bumetanide inMCT6-expressing oocytes or uninjected oocytes was measured at room temperature and pH 7.4 or pH 6.0 for 30 min in the presence or absence of inhibitor. MCT6-specific uptake was obtained by subtracting the uptake amount of uninjected oocytes from that of MCT6-expressing oocytes. The results are shown as percentages of control uptake measured in the absence of inhibitor. Each value represents the mean ± S.E.M. (n = 4–10).


Inhibitor

Concentration

MCT6-Specific Uptake
pH 7.4
pH 6.0
mM % of control
l-Lactic acid 5 123.8 ± 11.4 76.8 ± 11.7
Pyruvic acid 5 95.1 ± 12.4 75.7 ± 5.6
Succinic acid 5 101.8 ± 14.2 73.0 ± 7.3
Citric acid 5 128.2 ± 8.9 99.2 ± 0.5
Choline 5 126.4 ± 14.1 76.3 ± 6.2
Cimetidine 5 40.4 ± 2.6* 58.1 ± 7.9*
p-Aminohippuric acid 5 30.9 ± 7.7* 83.9 ± 1.9
Estrone-3-sulfate 5 11.6 ± 4.0* 21.3 ± 8.1*
Chlorothiazide 0.5 52.0 ± 6.7* 77.5 ± 9.7
Hydrochlorothiazide 0.5 71.0 ± 5.1* 68.6 ± 5.1*
Trichlormethiazide 0.5 20.7 ± 2.6* 64.2 ± 5.5*
Probenecid 0.5 46.3 ± 2.4* 82.6 ± 14.2
Glibenclamide 0.1 31.3 ± 4.3* 56.3 ± 9.4*
Nateglinide
0.001
40.8 ± 2.5*
47.1 ± 10.3*
  • * p < 0.05 vs. control.