Table 2.
Effect of mGlu2 NAMs on [3H]-LY354740 saturation binding at mGlu2
| Kd (nM) | Bmax (fmol·mg−1) | |
|---|---|---|
| LY354740 | 9.1 ± 0.9 | 14632 ± 151 |
| +10 nM RO4988546 | 12.3 ± 2.0 | 13540 ± 420 |
| +30 nM RO4988546 | 26.0 ± 1.5 | 13870 ± 170 |
| +100 nM RO4988546 | 39.7 ± 3.2 | 13175 ± 515 |
| +2 nM RO5488608 | 14.6 ± 1.1 | 14830 ± 410 |
| +3.16 nM RO5488608 | 11.1 ± 0.3 | 11515 ± 185 |
| +5 nM RO5488608 | 21.5 ± 1.0 | 9034 ± 150 |
| +10 nM RO5488608 | 24.1 ± 1.4 | 7465 ± 171 |
Calculated Kd and Bmax values for the saturation isotherms of [3H]-LY354740 in the absence and presence of mGlu2 NAMs shown in Figure 3. Values are mean ± SEM from individual experiments performed in duplicate (LY354740 n = 8, RO4988546 n = 2, RO5488608 3.16 nM and 10 nM n = 2, RO5488608 2 nM and 5 nM n = 3).