Table 1.
Potencies (pEC50) of the indicated compound on mGlu2, mGlu2-4 and mGlu4 as determined using the TR-FRET-based conformational assay depicted in Figure 1, or the cAMP assay as depicted in Figure 2.
Data are means ± SEM of at least three experiments performed in triplicates.
| Receptor | ||||||
|---|---|---|---|---|---|---|
| mGlu2 | mGlu2-4 | mGlu4 | ||||
| Compound | pEC50 | Emax (%) | pEC50 | Emax (%) | pEC50 | Emax (%) |
| TR-FRET conformational sensor assay | ||||||
| Glutamate | 5.5 ± 0.04 | 100 ± 1 | 5.5 ± 0.04 | 100 ± 2 | 5.0 ± 0.05 | 100 ± 2 |
| LY354740 | 7.5 ± 0.04 | 99 ± 1 | 5.9 ± 0.4 | 59 ± 9 | – | 3 ± 1 |
| APDC | 5.4 ± 0.07 | 97 ± 3 | 4.8 ± 0.1 | 56 ± 3 | – | 10 ± 2 |
| DCGIV | 6.6 ± 0.06 | 79 ± 1 | 6.8 ± 0.2 | 27 ± 2 | 4.7 ± 0.2 | 16 ± 2 |
| L-AP4 | – | 14 ± 1 | 6.7 ± 0.1 | 48 ± 2 | 6.2 ± 0.1 | 95 ± 1 |
| LSP4-2022 | – | 3 ± 1 | 6.8 ± 0.1 | 53 ± 2 | 6.2 ± 0.05 | 91 ± 1 |
| ACPT-I | – | 7 ± 1 | 5.3 ± 0.2 | 26 ± 2 | 5.1 ± 0.1 | 74 ± 2 |
| cAMP assay | ||||||
| Glutamate | 5.6 ± 0.06 | 100 ± 1 | 5.6 ± 0.07 | 100 ± 2 | 5.1 ± 0.06 | 100 ± 2 |
| LY354740 | 7.8 ± 0.04 | 97 ± 1 | 5.3 ± 0.2 | 59 ± 6 | – | 5 ± 1 |
| APDC | 6.3 ± 0.06 | 96 ± 2 | 6.0 ± 0.1 | 50 ± 2 | – | 9 ± 3 |
| DCGIV | 6.9 ± 0.09 | 69 ± 2 | 6.6 ± 0.2 | 42 ± 3 | 5.5 ± 0.4 | −17 ± 2 |
| L-AP4 | – | 3 ± 2 | 6.6 ± 0.1 | 51 ± 1 | 6.9 ± 0.07 | 99 ± 2 |
| LSP4-2022 | – | 3 ± 1 | 6.9 ± 0.1 | 48 ± 2 | 6.9 ± 0.04 | 99 ± 1 |
| ACPT-I | – | 13 ± 7 | 5.9 ± 0.1 | 32 ± 1 | 5.7 ± 0.1 | 68 ± 3 |