IC50 values for the inhibition of TEA by the phenylpyridiniums and quinoliniums in CHO cells stably transfected with hOCT2 (this study) and HeLa cells stably transfected with hOCT1 (Bednarczyk et al., 2003)
Each IC50 is the mean value of at least two experiments (described under Materials and Methods). ClogP values calculated with Daylight software using Cerius2 (Accelrys).
| Compound | IC50 | AlogP | |
|---|---|---|---|
| hOCT2 | hOCT1 | ||
| μM | |||
| 1-(2-Hydroxyethyl)-4-phenylpyridinium | 10.3 ± 1.9 | 16.2 ± 1.4 | 1.76 |
| 1-(2-Hydroxyethyl)-3-phenylpyridinium | 10 ± 2.3 | 31.1 ± 2.3 | 1.76 |
| 1-(2-Hydroxyethyl)quinolinium | 14 ± 0.9 | 80.6 ± 3.2 | 1.58 |
| 1-(Phenyl)methyl-4-phenylpyridinium | 2 ± 0.1 | 9.3 ± 0.6 | 3.88 |
| 1-(Phenyl)methyl-3-phenylpyridinium | 0.8 ± 0.1 | 5.5 ± 0.9 | 3.88 |
| 1-(Phenyl)methylquinolinium | 0.47 ± 0.06 | 14.3 ± 0.7 | 3.70 |
| 1-Ethyl-4-phenylpyridinium | 4.9 ± 0.8 | 7.1 ± 1.1 | 2.65 |
| 1-Ethyl-3-phenylpyridinium | 4.45 ± 0.7 | 28.3 ± 4.5 | 2.65 |
| 1-Ethylquinolinium | 3.3 ± 0.5 | 67.6 ± 11.2 | 2.47 |