Experiments were conducted using whole-cell patch-clamp electrophysiology at a −70 mV holding potential. Concentrations of (±)-ketamine able to inhibit 75% of the current elicited by 10 µM glutamate and glycine each were applied to a cell line expressing heterodimeric NR1-2C NMDARs to carry out kinetic studies. These experiments showed that 10 µM REL-1017 and 1 µM (±)-ketamine elicited similar current blockade of approximately 75%. Control current (100%) was induced by 10 µM L-glutamate and 10 µM glycine, respectively, and resulted in −594.2 ± 103.7 pA (mean ± SEM, n = 28). 10 µM REL-1017 and 10 µM, 3 µM, 1 µM, and 0.3 µM (±)-ketamine reduced L-glutamate/glycine–elicited current by 74.6 ± 1.9% (n = 12), 97.2 ± 0.3% (n = 3), 89.7 ± 0.6% (n = 3), 74.6 ± 2.2% (n = 3), and 44.2 ± 3.0% (n = 7), respectively.