TABLE 1

Km and Ki values of NSAIDs among organic anion transporters The effect of NSAIDs was examined for the uptake of ketoprofen by rOat2-LLC, and their Ki values were determined by nonlinear regression analysis using the data shown in Fig. 2. The values in each column represent the means ± computer-calculated S.D.

NSAIDs
rOat1a
rOat2
rOat3a
hOat2b
μM μM μM μM
Salicylate 2110 ± 190 399 ± 133 519 ± 132 N.D.
Diclofenac 4.56 ± 1.24 107 ± 29 3.17 ± 0.43 14.3
Sulindac 99.9 ± 18.6 537 ± 282 7.72 ± 1.32 440
Indomethacin 7.44 ± 3.88 1.25 ± 0.40 1.29 ± 0.46 64.1
Etodolac >100 344 ± 99 9.98 ± 1.48 N.D.
Tolmetin 15.4 ± 3.2 288 ± 118 8.78 ± 2.32 N.D.
Ibuprofen 4.33 ± 0.40 346 ± 100 3.57 ± 1.09 692
Ketoprofen 6.11 ± 1.66 3.31 ± 0.18* 4.31 ± 1.28 400
Naproxen 5.54 ± 0.89 >1000 19.1 ± 6.9 486
Phenylbutazone
47.9 ± 9.2
387 ± 129
8.48 ± 0.78
N.D.

  • N.D., not determined.

  • ↵ a represent the previously reported values by Nozaki et al. (2002) and Khamdang et al. (2002), respectively

  • ↵ b represent the previously reported values by Nozaki et al. (2002) and Khamdang et al. (2002), respectively

  • ↵* represents the Km value