TABLE 2.
EC50 values of methamphetamine and amphetamine for hOCT1 and hOCT2 determined by two-binding site fitting
The EC50 values were obtained by fitting inhibition data in Fig. 1 and Supplemental Fig. 2 using eq. 2 described in Materials and Methods with the fit shown in Supplemental Fig. 3. The last column lists the P values obtained by comparing eqs. 1 and 2 with an extra sum-of-squares F test. Results represent mean ± S.D. of three independent experiments each run in triplicate.
| Inhibitor |
Two-Binding Site |
Two-Binding versus One-Binding Site |
||
|---|---|---|---|---|
| Transporter |
EC50 Value |
|||
| High Affinity |
Low Affinity |
|||
| μM | μM | |||
| Methamphetamine | hOCT1 | 5.29 ± 0.66 | 400 ± 229 | P < 0.0001 |
| hOCT2 | 1.21 ± 0.19 | 58.2 ± 23.4 | P < 0.0001 | |
| Amphetamine | hOCT1 | NA | NA | P = 0.55 |
| hOCT2 | 0.72 ± 0.29 | 145 ± 104 | P < 0.0001 | |
NA, not applicable.