EC50 values for the glutamate- and LY354740 stimulated GTPγ35S binding on the HEK-293 cell membranes transfected with the mGlu2 wild-type and point-mutated receptors. Values are mean ± S.D. of the EC50 values, calculated from at least three individual experiments, performed in triplicate.
| Mutation | EC50 of GTPγ35S Binding | |
|---|---|---|
| Glutamate-Stimulated | LY354740-Stimulated | |
| μM | nM | |
| Wild-type | 3 ± 1 | 28 ± 4 |
| Y144S | 6 ± 1 | 67 ± 8 |
| Y144A | 10 ± 3 | 100 ± 19 |
| D146S | 2.8 ± 0.15 | 30 ± 3 |
| S148A | >100 | >200 |
| A166S | 6 ± 4 | 24 ± 12 |
| S167A | 10 ± 5 | 19 ± 5 |
| S169A | 1.1 ± 0.7 | 24 ± 8 |