IC50 values of various diuretics for organic anion uptake mediated by hOAT1, hOAT2, hOAT3, and hOAT4
S2 hOAT1, S2 hOAT2, S2 hOAT3, and S2 hOAT4 were incubated in a solution containing either 5 μM [14C]PAH (hOAT1), 50 nM [3H] PGF2α (hOAT2), or 50 nM [3H]ES (hOAT3 and hOAT4) in the absence or presence of various concentrations of diuretics for 2 min (hOAT1, hOAT3, and hOAT4) or 20 s (hOAT2). Each value represents the mean ± S.E. of eight monolayers from two separate experiments.
Diuretics | hOAT1 | hOAT2 | hOAT3 | hOAT4 | |||
---|---|---|---|---|---|---|---|
μM | |||||||
Thiazide | |||||||
Chlorothiazide | 3.78 ± 0.41 | 2205 ± 143 | 65.3 ± 4.83 | 2632 ± 132 | |||
Cyclothiazide | 84.3 ± 7.32 | 39.2 ± 4.10 | 27.9 ± 2.12 | 5000> | |||
Hydrochlorothiazide | 67.3 ± 5.32 | 1023 ± 53.2 | 942 ± 76.5 | 5000> | |||
Trichloromethiazide | 19.2 ± 1.12 | 1220 ± 101 | 71.2 ± 4.32 | 1505 ± 98.3 | |||
Loop diuretic | |||||||
Bumetanide | 7.60 ± 0.58 | 77.5 ± 5.38 | 0.75 ± 0.07 | 348 ± 23.2 | |||
Ethacrynic acid | 29.6 ± 1.63 | 121 ± 9.83 | 0.58 ± 0.08 | 8.76 ± 0.91 | |||
Furosemide | 18.0 ± 1.10 | 603 ± 46.3 | 7.31 ± 0.81 | 44.5 ± 2.53 | |||
Carbonic anhydrase inhibitor | |||||||
Acetazolamide | 75.0 ± 6.52 | 5000> | 816 ± 67.3 | 425 ± 39.3 | |||
Methazolamide | 438 ± 32.1 | 5000> | 97.5 ± 9.84 | 5000> |