Agonist Construct | Glutamate | Aspartate | NMDA | Tet-Gly | Glycine |
---|---|---|---|---|---|
μM | |||||
Wild type | 3.5 ± 0.4 | 18.4 ± 1.4 | 47.0 ± 2.7 | 1.7 ± 0.2 | 2.6 ± 0.2 |
1.2 ± 0.1 (24) | 1.0 ± 0.1 (10) | 1.5 ± 0.1 (5) | 1.3 ± 0.2 (6) | 1.5 ± 0.2 (4) | |
H466A | 490 ± 64 | 1798 ± 391 | 3995 ± 93 | 71.1 ± 9.3 | 3.7 ± 0.2 |
1.5 ± 0.2 (7) | 1.3 ± 0.2 (9) | 2.4 ± 0.2 (6) | 1.3 ± 0.2 (10) | 1.5 ± 0.1 (4)a | |
H466F | 46.2 ± 3.2 | 229 ± 21 | |||
1.7 ± 0.2 (4) | 1.4 ± 0.2 (7) | ||||
S492A | 146 ± 7 | 4408 ± 277 | 1389 ± 157 | 35.7 ± 5.4 | 2.5 ± 0.3 |
1.2 ± 0.1 (6) | 0.9 ± 0.1 (12) | 1.4 ± 0.2 (5) | 1.1 ± 0.1 (6) | 1.3 ± 0.2 (5) | |
S492P | 68.0 ± 6.4 | 3545 ± 211 | |||
1.4 ± 0.2 (10) | 1.6 ± 0.1 (9) | ||||
T494A | 482 ± 38 | 4488 ± 382 | 552 ± 78 | 38.5 ± 4.5 | 1.5 ± 0.2 |
1.3 ± 0.1 (7) | 0.9 ± 0.1 (12) | 1.2 ± 0.2 (5) | 1.4 ± 0.2 (6) | 1.2 ± 0.2 (4) | |
S670G | 421 ± 58 | 1999 ± 114 | 544 ± 19 | 36.1 ± 3.2 | 2.3 ± 0.1 |
1.4 ± 0.2 (12) | 1.0 ± 0.1 (12) | 2.1 ± 0.2 (6) | 1.6 ± 0.2 (8) | 1.3 ± 0.1 (5) | |
T671A | 2967 ± 279 | 1851 ± 129 | 351 ± 25 | 69.6 ± 6.1 | 2.9 ± 0.2 |
1.3 ± 0.1 (5)a | 1.1 ± 0.1 (16) | 2.2 ± 0.4 (6) | 1.2 ± 0.1 (6) | 1.3 ± 0.1 (4)a | |
Fold-shift in EC50 | |||||
H466A | 140 | 98 | 85 | 42 | |
H466F | 13 | 5 | |||
S492A | 42 | 240 | 30 | 21 | |
S492P | 19 | 75 | |||
T494A | 138 | 244 | 12 | 23 | |
S670G | 120 | 109 | 12 | 21 | |
T671A | 848 | 101 | 7 | 41 |