Potency (IC50, micromolar) of BAY36-7620 in inhibiting the action of glutamate on the wild-type mGlu1 and various chimeric mGlu receptors. For each receptor, the origin of the ECD (from mGlu1, mGlu2, or mGlu5) and the 7TM [from mGlu1, DmGluA, mGlu2, mGlu5, or mGlu1 and mGlu5 (1/5)] are indicated. Data are means ± S.E.M. of at least three independent experiments performed in triplicate. >100 means that no significant inhibition of the Glu-induced IP formation was detected with 100 μM BAY36-7620.
| mGlu1 | mGlu1/DA | mGlu1/2 | mGlu2/1 | mGlu1/5-D | mGlu5/1-C | mGlu5/1-F | |
|---|---|---|---|---|---|---|---|
| ECD | 1 | 1 | 1 | 2 | 1 | 5 | 1 |
| 7TM | 1 | DA | 2 | 1 | 5 | 1 | 5/1 |
| IC50(μM) | 0.16 ± 0.01 | >100 | >100 | 0.14 ± 0.05 | >100 | 0.24 ± 0.01 | 0.50 ± 0.06 |