TABLE 1

Concentration–response data for glycine site agonists at NMDA receptor subtypes

Concentration–response data for glycine site agonists at recombinant human and rat NMDA receptor subtypes measured using two-electrode voltage-clamp electrophysiology in the presence of 100–300 µM glutamate.

Receptor SubtypeGlycine Site AgonistsReceptor SpeciesEC50 (µM)pEC50 ± S.E.M.Rel. Imax (%)nHN
GluN1/2A
 AICPHuman0.0667.18 ± 0.02100 ± 21.315
Rat0.0367.49 ± 0.0592 ± 21.329
 GlycineHuman1.25.91 ± 0.01100 ± 11.76
d-SerineHuman1.85.75 ± 0.0299 ± 11.85
 DCSHuman22.04.65 ± 0.0290 ± 21.36
Rat18.04.75 ± 0.0191 ± 11.613
GluN1/2B
 AICPHuman0.0257.60 ± 0.1910 ± 10.79
Rat0.0147.86 ± 0.039 ± 01.114
 GlycineHuman0.586.24 ± 0.02101 ± 12.26
d-SerineHuman0.986.01 ± 0.0597 ± 21.25
 DCSHuman7.35.14 ± 0.0663 ± 21.14
Rat8.35.08 ± 0.0161 ± 01.412
GluN1/2C
 AICPHuman0.00178.77 ± 0.04353 ± 60.916
Rat0.00109.04 ± 0.03339 ± 101.017
 GlycineHuman0.336.48 ± 0.03103 ± 11.75
d-SerineHuman0.476.33 ± 0.03106 ± 11.65
 DCSHuman4.45.36 ± 0.05151 ± 51.34
Rat2.85.55 ± 0.01197 ± 21.518
GluN1/2D
 AICPHuman0.0257.61 ± 0.0327 ± 11.414
Rat0.0317.51 ± 0.0226 ± 11.511
 GlycineHuman0.146.84 ± 0.04100 ± 21.65
d-SerineHuman0.356.46 ± 0.03101 ± 12.05
 DCSHuman3.15.51 ± 0.0676 ± 31.56
Rat3.25.50 ± 0.0197 ± 01.66
  • N, number of oocytes; nH, Hill coefficient; (Rel.) Imax, fitted maximal response relative to the maximal response to glycine.