Mean Glu or FP0429 EC50 values and FP0429 Emax values (%Glu max) for wt and mutant mGlu4 and mGlu8 receptors
All dose-response curves were fitted using Prism 4. At least three independent experiments performed in triplicates were used to determine mean EC50 values and Emax values.
Receptor | mGlu4wt | mGlu4SA | mGlu4AG | mGlu4AA | mGlu8wt | mGlu8SA | mGlu8AG | mGlu8SG |
|---|---|---|---|---|---|---|---|---|
| Glu EC50 (μM) | 3.0 ± 0.3 | 3.8 ± 0.3 | 3.2 ± 0.4 | 2.8 ± 0.5 | 1.3 ± 0.5 | 0.8 ± 0.1 | 0.9 ± 0.1 | 1.1 ± 0.2 |
| FP0429 EC50 (μM) | 48.3 ± 5.2 | 40.1 ± 3.8 | 48.9 ± 8.3 | 79.6 ± 14.3 | 56.2 ± 14.6 | 47.3 ± 5.1 | 71.2 ± 14.2 | 50.8 ± 5.7 |
| FP0429 Emax (%Glu max) | 75 ± 6 | 45 ± 4 | 76 ± 4 | 52 ± 9 | 36 ± 7 | 52 ± 8 | 70 ± 11 | 90 ± 16 |