Ki andKm | ||||
---|---|---|---|---|
CP (PCG) | CP (PAH) | rOat3 (PCG) | rOat1 (PAH) | |
μM | ||||
Estrone sulfate | 22.3 ± 18.3 | 34.8 ± 10.6 | 9.10 ± 5.23 | N.D. |
Cimetidine | 44.4 ± 9.4 | 51.0 ± 7.0 | 46.8 ± 15.1 | >1000 |
Probenecid | 2.29 ± 0.66 | 3.29 ± 0.30 | 4.43 ± 0.89 | 31.0 ± 7.91-a |
E217βG | 33.0 ± 6.8 | 26.8 ± 6.8 | 35.6 ± 18.3 | >3001-a |
PAH | 406 ± 184 | 354 ± 841-b | 398 ± 154 | 47.0 ± 5.21-b |
PCG | 111 ± 191-b | 69.6 ± 21.1 | 82.6 ± 31.51-b | 800 ± 361 |
The effect of estrone sulfate, cimetidine, probenecid, E217βG, PAH and PCG was examined on the uptake of PCG and PAH by isolated rat CP, and PCG and PAH by rOat3 and rOat1. TheseK i and K m values were determined by nonlinear regression analysis as described underExperimental Procedures. Data are taken from Figures 4to 6 and from Sugiyama et al. (2001). Values represent the mean ± S.D. (n = 3).