TABLE 15.

IC₅₀ values in micromolar for uncompetitive NMDA receptor antagonists

All values were measured in 0 Mg²⁺, unless otherwise indicated. Values for memantine and (±)-ketamine are from Kotermanski and Johnson (2009) with membrane potential held at −66 mV. All remaining values are from Dravid et al. (2007) with membrane potential held at −40 mV.

Uncompetitive Antagonist	GluN2A	GluN2B	GluN2C	GluN2D
	μM
(+)-MK-801	0.015	0.009	0.024	0.038
(−)-MK-801	0.35	0.32	0.038	0.17
(−)-Ketamine	16	1.6	1.1	1.5
(±)-Norketamine	51	8.7	5.6	7.5
Dextromethorphan	11	3.7	1.1	5.4
Levomethorphan	13	2.2	1.1	2.6
Dextrorphan	1.3	0.33	0.15	0.74
Levorphanol	1.8	1.2	0.58	2.1
Phencyclidine	0.82	0.16	0.16	0.22
PCA	19	3.9	1.6	1.7
CNS-1102	0.13	0.068	0.087	0.14
Amantadine	130	70	35	38
Remacemide	81	35	92	63
Pentamidine	0.72	1.5	10	9.1
9-aminoacridine	7.8	7.5	29	38
Memantine	0.80	0.57	0.52	0.54
Memantine–1 mM Mg2+	13	10	1.6	1.8
(±)-Ketamine	0.33	0.31	0.51	0.83
(±)-Ketamine–1 mM Mg2+	5.4	5.08	1.2	2.9

CNS-1102, aptiganel; PCA, 1-phenylcyclohexylamine.