The effect of mutations on mGlu5-mediated of agonist-induced [Ca2+]i response
EC50, Hill coefficient (nH), and relative efficacy (Emax) values for the quisqualate- and glutamate-induced [Ca2+]i response in the HEK-293 cells transiently transfected with the rmGlu5a WT and mutated receptors. For quisqualate, the data are presented as mean ± S.E. of five to eight dose-response measurements; for glutamate, they represent mean ± S.E. of two to five dose-response measurements from two or three independent transfections.
| rmGlu5a Receptor | Quisqualate | Glutamate | ||||
|---|---|---|---|---|---|---|
| EC50 | nH | Relative Emax | EC50 | nH | Relative Emax | |
| nM | nM | |||||
| WT | 11.9 ± 1.6 | 2.3 ± 0.3 | 100 | 540 ± 80 | 2.2 ± 0.2 | 100 |
| R647A | 44 ± 2.8 | 1.5 ± 0.1 | 44.1 ± 3.5 | 1302 ± 52 | 2.8 ± 0.9 | 42.6 ± 4.2 |
| P654S | 19 ± 3 | 1.6 ± 0.2 | 121.8 ± 9.8 | 793 ± 61 | 1.7 ± 0.1 | 124.4 ± 16.2 |
| S657C | 15.5 ± 2.5 | 1.7 ± 0.1 | 100.8 ± 8.4 | 606 ± 94 | 1.9 ± 0.5 | 102.1 ± 5.7 |
| P654S/S657C | 30 ± 2.4 | 1.8 ± 0.1 | 105.5 ± 2.5 | 1107 ± 20 | 1.7 ± 0.2 | 104.5 ± 3.8 |
| Y658V | 46.7 ± 14.5 | 1.4 ± 0.2 | 75.1 ± 12.1 | 847 ± 58 | 5.5 ± 4 | 69.0 ± 14.8 |
| Y658F | 19.5 ± 4.5 | 2.2 ± 0.2 | 132.3 ± 7.2 | 761 ± 237 | 2.1 ± 0.3 | 114.8 ± 10.4 |
| N733A | 33 ± 8.5 | 2 ± 0.1 | 115.8 ± 14.6 | 712 ± 29 | 2.1 ± 0.1 | 109.1 ± 12.7 |
| L743V | 31 ± 5 | 1.9 ± 0.6 | 77.4 ± 6.0 | 1007 ± 178 | 2.1 ± 0.4 | 78.9 ± 5.2 |
| L743A | 12 ± 4.3 | 2 ± 0.1 | 94.1 ± 31.2 | 559 ± 216 | 2.2 ± 0.2 | 103.9 ± 41.1 |
| T780A | 23 ± 5 | 1.3 ± 0.1 | 81.1 ± 6.4 | 813 ± 185 | 1.9 ± 0.4 | 93.0 ± 13.8 |
| W784F | 24.5 ± 2.5 | 3.3 ± 0.4 | 108.3 ± 38.1 | 842 ± 172 | 2.7 ± 0.1 | 98.5 ± 32.6 |
| W784A | 25 ± 2 | 2.3 ± 0.1 | 106.1 ± 36.3 | 1268 ± 132 | 1.8 ± 0.2 | 105.9 ± 40.1 |
| F787A | 24.5 ± 0.5 | 2.3 ± 0.5 | 171.4 ± 62.9 | 919 ± 24 | 2.3 ± 0.3 | 167.4 ± 60.6 |
| V788M | 34 ± 16 | 2.1 ± 0.1 | 91.3 ± 12.4 | 713 ± 54 | 1.9 ± 0.3 | 86.3 ± 10.2 |
| Y791A | 19.3 ± 5.8 | 1.4 ± 0.3 | 51.6 ± 5.9 | 720 ± 86 | 1.5 ± 0.6 | 52.3 ± 8.8 |
| M801T | 20 ± 4 | 1.8 ± 0.1 | 69.5 ± 18.5 | 720 ± 126 | 1.7 ± 0.2 | 64.4 ± 13.9 |
| A809V | 45.5 ± 14.5 | 1.5 ± 0.4 | 87.8 ± 3.1 | 867 ± 84 | 4.5 ± 2.5 | 88.8 ± 16.0 |