Potencies of various antagonists at the group III mGluRs as assessed using the GIRK thallium flux assay
Potencies of compounds are shown in micromolar concentrations for IC50 values.
Antagonist | mGluR4 | mGluR7 L-AP4 | mGluR8 | ||||
|---|---|---|---|---|---|---|---|
| L-AP4 | Glutamate | L-AP4 | Glutamate | ||||
| LY341495 | 27.0 ± 11.6 | 14.3 ± 4.3 | 3.2 ± 0.33 | 0.21 ± 0.10 | 0.20 ± 0.02 | ||
| MSOP | >1000 | >300 | >1000 | >300 | >300 | ||
| CPPG | >300 | 167.2 ± 50 | >300 | 5.7 ± 2.3 | 3.7 ± 0.4 | ||
| UBP1112 | >300 | >300 | >1000 | 50.8 ± 22.9 | 34.2 ± 7.0 | ||
| MPPG | >300 | 167.7 ± 2.1 | >300 | 28.7 ± 10.0 | 25.8 ± 4.4 | ||
| (S)-MAP4 | >1000 | >300 | >1000 | >300 | >300 | ||
| MSPG | IA | IA | IA | >300 | >300 | ||
IA, inactive.