Dissociation rates of the antagonist radioligand [3H]PSB-11 from WT and mutant receptors in the absence and presence of allosteric modulators
| k−1 | |||
|---|---|---|---|
| Control | + HMA (100 μM) | + Sodium Ions (100 mM) | |
| min −1 | |||
| WT | 0.23 ± 0.02 | 0.46 ± 0.05* | 0.10 ± 0.04* |
| D58N2.50 | 0.27 ± 0.04 | 0.52 ± 0.07* | 0.31 ± 0.04 |
| L244A6.49 | 0.22 ± 0.04 | 0.45 ± 0.10* | 0.11 ± 0.03* |
| S247A6.52 | 0.24 ± 0.03 | 0.47 ± 0.10* | 0.12 ± 0.02* |
Results were expressed as means ± S.E. from three independent experiments. The dissociation rates (k−1) were determined at 25°C. The final concentration of [3H]PSB-11 used in this experiment was 8 nM.
3-150 Significantly different from control, P < 0.05.