Potencies of various mGlu5 antagonists on inhibition of quisqualate-induced [Ca2+]i response IC50 and Hill coefficient (nH) values for the inhibition of quisqualate (20 nM)-evoked [Ca2+]i response in the HEK-293 cells stably expressing the hmGlu5a receptor. Data are means ± S.E. of the three to six dose-response measurements (each performed in triplicate).
Compound | IC50 | nH | |
|---|---|---|---|
| μM | |||
| SIB-1757 | 1.1 ± 0.06 | 2.3 ± 0.3 | |
| SIB-1893 | 0.8 ± 0.09 | 1.4 ± 0.1 | |
| MPEP | 0.028 ± 0.003 | 1.9 ± 0.2 | |
| Fenobam | 0.058 ± 0.002 | 1.7 ± 0.1 | |
| S-4-CPG | 1971 ± 205 | 1.3 ± 0.2 | |