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 AgonistGluN2AGluN2BGluN2CGluN2D
μM (%)
Glycine1.1 (100)0.72 (100)0.34 (100)0.13 (100)
l-Serine212 (95)77 (98)27 (110)15 (98)
d-Serine1.3 (98)0.65 (96)0.32 (110)0.16 (93)
l-Alanine96 (79)36 (65)28 (92)13 (97)
d-Alanine3.1 (96)0.89 (84)0.56 (96)0.22 (99)
d-Cycloserine19 (90)8.2 (65)3.3 (190)2.9 (94)
HA 96612 (12)4.6 (14)
β-Cl-d-Alanine21 (84)9.9 (88)3.7 (79)1.7 (81)
β-F-dl-Alanine11 (92)0.98 (88)0.40 (84)0.40 (91)
tri-F-dl-Alanine1.3 (130)0.65 (64)0.32 (110)0.16 (93)
ACPC1.3 (79)0.65 (89)0.35 (88)0.083 (89)
ACBC45 (13)6.6 (33)
  • ACBC, 1-aminocyclobutane-1-carboxylic acid; ACPC, 1-aminocyclopropane-1-carboxylic acid; HA 966, (+)-(1-hydroxy-3-aminopyrrolidine-2-one).