Table 1

Effects of 4-methylglutamate derivatives on radioligand binding to inotropic glutamate receptors

CompoundIC50 or EC50
[3H]Kainate[3H]AMPA[3H]CGP 39653[3H]MK-801
μM
Rat brain
 (2S,4R)-4-Methylglutamate0.032  ± 0.00326.6  ± 3.65.9  ± 0.929.6  ± 3.6
 (2R,4S)-4-Methylglutamate0.65 (2)77.8  ± 1126.7 (2) 105.2  ± 15.8
 (2R,4R)-4-Methylglutamate0.46  ± 0.1770.9  ± 1120.3  ± 0.423.1  ± 3.4
 (2S,4S)-4-Methylglutamate0.33  ± 0.0314.6  ± 0.099.6  ± 0.914.3  ± 1.7
 Glutamate0.22  ± 0.0090.266  ± 0.01 0.117 (2)0.259  ± 0.03
 Kainate0.013  ± 0.0025.1  ± 0.7
GluR6
 Kainate0.0284  ± 0.004
 (2S,4R)-4-Methylglutamate0.0186  ± 0.002

  • IC50 ([3H]kainate, [3H]AMPA and [3H]CGP 39653) and EC50 ([3H]MK-801) values represent mean ± S.E.M. of ≥3 independent determinations, except as indicated in parentheses.

  • Assay conditions are described in “Materials and Methods.”