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. 2023 Feb 13;14(5):917–935. doi: 10.1021/acschemneuro.2c00779

Figure 2.

Figure 2

Inhibition of NMDA receptors by EU93-108. (A) Current response time course for maximal receptor activation by 100 μM l-glutamate and 100 μM glycine (GG) and then in the continuous presence of 100 μM l-glutamate and glycine plus increasing concentrations of EU93-108 at 0.03, 0.1, 0.3, 1, 3, and 10 μM is shown for each receptor subunit combination. The receptors tested are diheteromeric rat GluN1/GluN2Ac1/GluN2Ac2 (r2Ac1/r2Ac2), triheteromeric rat GluN1/GluN2Ac1/GluN2Bc2 (r2Ac1/r2Bc2), diheteromeric rat GluN1/GluN2Bc1/GluN2Bc2 (r2Bc1/r2Bc2), and diheteromeric human GluN1/GluN2B/GluN2B (h2B/h2B). All currents were normalized to the maximal response in 100 μM glutamate and glycine, set as 100%. The mean ± SEM for maximal current sizes for r2Ac1/r2Ac2 receptors was 295 ± 44 nA (n = 6), for r2Ac1/r2Bc2 receptors 278 ± 39 nA (n = 12), for r2Bc1/r2Bc2 receptors 353 ± 77 nA (n = 8), and for h2B/h2B receptors 276 ± 63 nA (n = 10). (B) Concentration–effect curve for inhibition by EU93-108 for all four receptor subunit combinations, with the same symbols as in (A). The mean ± SEM values are plotted for r2Ac1/r2Ac2 receptors (open triangles, n = 6), r2Ac1/r2Bc2 receptors (closed circles, n = 12), r2Bc1/r2Bc2 receptors (open circles, n = 8), and h2B/h2B receptors (open squares, n = 10) with increasing concentrations of EU93-108 applied in the presence of 100 μM glutamate and 100 μM glycine at −40 mV as described in the Materials and Methods section.