10 µM REL-1017 differentially blocked heterodimeric NMDARs in the presence of extracellular 1 mM Mg2+. REL-1017 showed a preference for NMDARs containing the 2D subunit, which is blocked in the presence of either 10 μM or 1 μM L-glutamate at −30 mV or more negative voltages. Data were obtained in automated patch-clamp platform. Every data point represents mean ± SEM (n = 4) of normalized current elicited by 10 mM L-glutamate at indicated voltage, measured during a hyperpolarizing ramp, in the absence (○) or presence (●) of 10 µM REL-1017. Statistical results of one-way analysis of variance (ANOVA) followed by Tukey’s multiple comparisons test also reported p < 0.05 (*), p < 0.01 (**), p < 0.001 (***), and p < 0.0001 (****). Glu is glutamate.