TABLE 2

Inhibitory effect of YM90K on organic anion uptake by hOATs and on organic cation uptake by hOCTs




Substrate

Percentage of Control Uptake at 300 μM YM90Ka

IC50

Ki
μM
hOAT1 PAH 2.3 ± 0.1*** 3.8 5.8c
hOAT2 PGF 63.6 ± 3.3*** >300 ND
hOAT3 ES 10.8 ± 0.0*** 4.4 3.4b
hOAT4 ES 77.0 ± 0.8*** >300 ND
hOCT1 TEA 89.6 ± 5.5 >300 ND
hOCT2
TEA
95.4 ± 2.5
>300
ND
  • ND, not determined.

  • a Each value represents the mean ± S.E. of three determinations. ***P < 0.001.

  • b Competitive inhibition.

  • c Noncompetitive inhibition.