TABLE 7.
EC50 values in micromolar for agonists binding to the GluN1 subunit of the NMDA receptor
Percentage relative efficacy (in parentheses) is the current response to a maximally effective concentration of agonist relative to the response to a maximally effective concentration of glycine. All values are from recombinant rat NMDA receptors expressed in X. laevis oocytes and coactivated by glutamate (Chen et al., 2008; Dravid et al., 2010) except HA 966 and ACBC (Priestley et al., 1995). Values are given to two significant digits.
| Glycine-Site Agonist | GluN2A | GluN2B | GluN2C | GluN2D |
|---|---|---|---|---|
| μM (%) | ||||
| Glycine | 1.1 (100) | 0.72 (100) | 0.34 (100) | 0.13 (100) |
| l-Serine | 212 (95) | 77 (98) | 27 (110) | 15 (98) |
| d-Serine | 1.3 (98) | 0.65 (96) | 0.32 (110) | 0.16 (93) |
| l-Alanine | 96 (79) | 36 (65) | 28 (92) | 13 (97) |
| d-Alanine | 3.1 (96) | 0.89 (84) | 0.56 (96) | 0.22 (99) |
| d-Cycloserine | 19 (90) | 8.2 (65) | 3.3 (190) | 2.9 (94) |
| HA 966 | 12 (12) | 4.6 (14) | ||
| β-Cl-d-Alanine | 21 (84) | 9.9 (88) | 3.7 (79) | 1.7 (81) |
| β-F-dl-Alanine | 11 (92) | 0.98 (88) | 0.40 (84) | 0.40 (91) |
| tri-F-dl-Alanine | 1.3 (130) | 0.65 (64) | 0.32 (110) | 0.16 (93) |
| ACPC | 1.3 (79) | 0.65 (89) | 0.35 (88) | 0.083 (89) |
| ACBC | 45 (13) | 6.6 (33) | ||
ACBC, 1-aminocyclobutane-1-carboxylic acid; ACPC, 1-aminocyclopropane-1-carboxylic acid; HA 966, (+)-(1-hydroxy-3-aminopyrrolidine-2-one).