TABLE 1

Mean EC50 values, Hill slopes, and shifts in potency for wild-type NR1/NR2A NMDA receptors and receptors carrying mutations in the S1 and S2 ligand binding domains

For each receptor, the EC50 is given on the first line and the nH on the second. The number of oocytes studied is given in parentheses.

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
  • a Values reported in Anson et al. (1998).