Table 1.

Subunit-selectivity of compounds acting on recombinant NMDA receptors

Compound	GluN2A	GluN2B	GluN2C	GluN2D	Ref
Competitive Antagonists	Ki (μM)	Ki (μM)	Ki (μM)	Ki (μM)
APV, (R)-AP5	0.28	0.46	1.6	3.7	[55]
Selfotel (CGS-19755)	0.15	0.58	0.58	1.1	[55]
(R)-CPP	0.041	0.27	0.63	1.99	[55]
NVP-AAM077	0.015	0.078	--	--	[44]
UBP-141	14	19	4.2	2.8	[56]
Conantokin-G	10	0.1	1	1	[57]
Conantokin-R	1	1	7	10	[57]
7-Cl-kynurenatea	0.6	0.2	--	--	[58]
Channel blockers	IC50 (μM)	IC50 (μM)	IC50 (μM)	IC50 (μM)
Argiotoxin636	0.009	0.005	0.46	--	[59]
(+)MK-801	0.015	0.009	0.024	0.038	[53]
Memantineb	13	10	1.6	1.8	[60]
Ketamineb	5.4	5.1	1.2	2.9	[60]
Phencyclidine	0.82	0.16	0.16	0.22	[53]
Dextrorphan	1.3	0.33	0.15	0.74	[53]
CNS-1102 (aptiganel)	0.13	0.068	0.087	0.14	[53]
Noncompetitive Antagonists	IC50 (μM)	IC50 (μM)	IC50 (μM)	IC50 (μM)
Ifenprodil	39	0.15	29	76	[61]
Ro 25-6981	52	0.0090	--	--	[62]
CP-101,606	>100	0.039	>100	>100	[63]
QNZ46	229	>300	6	3	[5]
DQP-1105	206	121	9	3	[9]
TCN 201	0.109	>30	--	>30	[7]
UBP-618	1.8	2.4	2.0	2.4	[8]
Dynorphin A (1–13)	19	29	228	57	[64]
Pregnanolone sulfate (3α5βS)	50	44	26	30	[65]
Allosteric Potentiators	EC50 (μM)	EC50 (μM)	EC50 (μM)	EC50 (μM)
CIQ	NE	NE	2.8	3	[6]
Spermine	NEc	163	NE	NE	[66,67,21]
Pregnenolone sulfate	21	33	NEc	NEc	[26]
UBP-710	>30	>30	NEc	NEc	[8]

NE indicates no detectable effect, and -- indicates that data is not available.

^aK_B values calculated from Cheng-Prusoff correction of IC₅₀ values.

^bIC₅₀ values determined in extracellular Mg²⁺, which alters subunit selectivity.

^cPartially inhibits with IC₅₀ value of 100 μM or greater.