Effect of mutations on inhibition of quisqualate-induced [Ca2+]i response by MPEP
IC50 and Hill coefficient (nH) values for the inhibition by MPEP of quisqualate (10 nM)-evoked [Ca2+]i response in the HEK-293 cells transiently transfected with the rmGlu5a WT and mutated receptors. Data are presented as means ± S.E. of the five to eight dose-response measurements from a minimum of three independent transfections. The affected mutants are shown in boldface type.
| rmGlu5a Receptor | Position in the 7TMD | IC50 MPEP | IC50 (mutant)/IC50 (WT) | nH |
|---|---|---|---|---|
| nM | ||||
| WT | 13.0 ± 1.5 | 1.5 ± 0.1 | ||
| R647A | 3.29 | 3.0 ± 0.1 | 0.2 | 1.8 ± 0.2 |
| P654S | 3.36 | 190.0 ± 27.5 | 15.0 | 2.0 ± 0.4 |
| S657C | 3.39 | 18.0 ± 3.4 | 1.4 | 1.6 ± 0.4 |
| P654S/S657C | 3.36,3.39 | 106.0 ± 12.0 | 8.2 | 1.4 ± 0.3 |
| Y658V | 3.40 | 707.0 ± 167.0 | 54.0 | 1.3 ± 0.3 |
| Y658F | 3.40 | 8.7 ± 2.7 | 0.7 | 1.4 ± 0.7 |
| N733A | 45.51 | 15.7 ± 1.8 | 1.2 | 1.5 ± 0.2 |
| L743V | 5.47 | 41.0 ± 4.7 | 3.2 | 1.7 ± 0.3 |
| L743A | 5.47 | 68.4 ± 6.0 | 5.3 | 1.5 ± 0.3 |
| T780A | 6.44 | 119.0 ± 37.0 | 9.2 | 1.4 ± 0.5 |
| W784F | 6.48 | 25.3 ± 4.7 | 2.0 | 1.2 ± 0.3 |
| W784A | 6.48 | 270.0 ± 64.4 | 21.0 | 0.8 ± 0.4 |
| F787A | 6.51 | 130.0 ± 45.0 | 10.0 | 1.7 ± 0.5 |
| V788M | 6.52 | 22.0 ± 2.5 | 1.7 | 1.7 ± 0.2 |
| Y791A | 6.55 | 291.0 ± 102.0 | 22.4 | 1.5 ± 0.3 |
| M801T | 7.39 | 26.0 ± 5.2 | 2.0 | 1.2 ± 0.2 |
| A809V | 7.47 | 583.0 ± 187.0 | 45.0 | 1.4 ± 0.6 |