TABLE 2

Effect of binding site mutations on glutamate potency NR indicates mutant receptor showed no response when tested at glutamate concentrations up to 30 mM. N.D. indicates that the ratio of EC50 for mutant to EC50 for wild-type could not be determined. Shift 2A/Shift 2D is the ratio of the EC50 Mut/WT for NR2A and EC50 Mut/WT for NR2D.


NR2A Mutation

EC50

EC50 Mut/WT

Hill Slope

n

NR2D Mutation

EC50

EC50 Mut/WT

Hill Slope

n

Shift 2A/Shift 2D
μM μM
Wild-Type NR2A 3.3 1.1 26 Wild-Type NR2D 0.49 1.5 30 0.7
H466Aa 490 140 1.5 H487A 76 150 1.2 8 0.9
H466Fa 46.2 14 1.7 H487F 2.3 4.7 2.0 7 3.0
G467V >3000 N.D. 6 G488V >3000 N.D. 6
R499A >3000 N.D. 12 R520A >3000 N.D. 6
R499K >3000 N.D. 12 R520K >3000 N.D. 12
S670A 1.6 0.5 1.2 11 S691A 0.2 0.4 1.2 8 1.3
S670Ga 421 120 1.4 S691G 46 94 1.2 6 1.3
T671Ab 2967 900 1.3 T692Ac 703 1400 1.5 0.6
Y711F 143 45 1.3 6 Y732F 0.20 0.4 1.7 12 113
D712A >3000 N.D. 6 D733A NR N.D. 8
Y742F
40
12
1.3
8
Y763F
6.1
12
2.2
6
1.0
  • Data from previous studies are included for comparison

  • a Chen et al. (2005)

  • b Anson et al. (1998)

  • c Chen et al. (2004)