The IC50 values of various NSAIDs for organic anion uptake mediated by hOAT1, hOAT2, hOAT3, and hOAT4
| Drugs | hOAT1 | hOAT2 | hOAT3 | hOAT4 |
|---|---|---|---|---|
| μM | ||||
| Hydrophilic | ||||
| Acetaminophen | 639 | 2000> | 2000> | 2000> |
| Acetylsalicylate | 769 | 2000> | 717 | 2000> |
| Salicylate | 325 | 2000> | 50.0 | 2000> |
| Hydrophobic | ||||
| Diclofenac | 4.46 | 14.3 | 7.78 | 34.5 |
| Ibuprofen | 55.6 | 692 | 6.00 | 103 |
| Indomethacin | 3.83 | 64.1 | 0.61 | 10.1 |
| Ketoprofen | 4.34 | 400 | 5.98 | 70.3 |
| Mefenamic acid | 0.83 | 21.7 | 0.78 | 61.7 |
| Naproxen | 5.67 | 486 | 4.67 | 85.4 |
| Phenacetin | 275 | 1878 | 19.4 | 2000> |
| Piroxicam | 62.8 | 70.3 | 2.52 | 84.9 |
| Sulindac | 36.2 | 440 | 3.62 | 617 |
S2 hOAT1, S2 hOAT2, S2 hOAT3, and S2hOAT4 were incubated in a solution containing either 5 μM [14C]PAH (hOAT1), 50 nM [3H]PGF2α(hOAT2), or 50 nM [3H]estrone sulfate (hOAT3 and hOAT4) in the absence or presence of various concentrations of NSAIDs for 2 min (hOAT1, hOAT3, and hOAT4) or 20 s (hOAT2). Each value represents the mean ± S.E. of six monolayers from two separate experiments.