TB-1-099 noncompetitively inhibits [3H]5-HT uptake Uptake binding surfaces were generated as described under Materials and Methods in the absence and presence of the indicated concentrations of TB-1-099. The data of three experiments (132 data points) were pooled and fit to the one-component uptake equation for the best-fit estimates of the Vmax and Km. The two [3H]5-HT experiments were run several months apart, each with its own control. Each value is ±S.D., n = 3.
Condition | Vmax | Apparent Km |
|---|---|---|
| fmol / mg protein / min | nM | |
| [3H]5-HT | ||
| Experiment 1 | ||
| Control | 300 ± 13 | 8.7 ± 0.4 |
| TB-1-099 (50 μM) | 140 ± 13* | 12.7 ± 0.9* |
| Experiment 2 | ||
| Control | 453 ± 47 | 13.4 ± 0.83 |
| Indatraline (8 nM) | 486 ± 83 | 63.6 ± 2* |
| [3H]DA | ||
| Control | 5187 ± 173 | 50.4 ± 2.0 |
| TB-1-099 (300 nM) | 4907 ± 320 | 87.5 ± 4.5* |
↵* P < 0.01 (F-test)