TABLE 11.

Equilibrium dissociation constants in micromolar for NMDA receptor competitive antagonists

Data presented as K_i except where indicated as K_B or K_d.

Competitive Antagonist	Site	GluN2A	GluN2B	GluN2C	GluN2D
		μM
7-CKAa	GluN1	0.6	0.2
5,7-DCKAb	GluN1	0.03	0.05	0.17	0.09
CGP-61594 (KB)b	GluN1	0.43	0.045	0.16	0.34
CGP-58411 (KB)c	GluN1	0.24	0.13
GV150,526Ad	GluN1	0.08	0.08	0.11	0.05
GV196,771Ad	GluN1	0.48	0.22	0.18	0.15
MDL105,519d	GluN1	0.012	0.015	0.012	0.018
ACEA-1011 (KB)e	GluN1	0.33	0.46	0.21	0.74
ACEA-1021f	GluN1	0.004	0.004	0.003	0.011
L-689,560 (KB)c	GluN1	0.004	0.02
L-701,324a	GluN1	0.005	0.005
(R)-AP5g	GluN2	0.28	0.46	1.6	3.7
(R)-AP7g	GluN2	0.49	4.1	6.4	17
PMPAg	GluN2	0.84	2.7	3.5	4.2
(R)-CPPg	GluN2	0.041	0.27	0.63	1.99
NVP-AAM077 (KB)h	GluN2	0.015	0.078
PPDAi	GluN2	0.55	0.31	0.096	0.13
(R)-α-AAi	GluN2	6.5	25	44	110
PBPDi	GluN2	16	5.0	8.9	4.3
UBP141j	GluN2	14	19	4.2	2.8
CGS-19755 (selfotel)g	GluN2	0.15	0.58	0.58	1.1
CGP-43487 (KB)c	GluN2	0.28	1.6
CGP-40116 (KB)c	GluN2	0.04	0.03
Con-Brk	GluN2	0.68	0.14	4.9	0.31
Con-Gl	GluN2	>10	0.1	1	1
Con-Pr1l	GluN2	>10	0.2	>10	1
Con-Pr2l	GluN2	>10	0.5	>10	1
Con-Pr3l	GluN2	>10	0.5	>10	8
Con-Rl	GluN2	1	1	7	>10
Con-T (Kd)m	GluN2	3.2	2.9

α-AA, α-aminoadipate; 5,7-DCKA, 5,7-dichlorokynurenic acid; 7-CKA, 7-chlorokynurenic acid; ACEA-1011, 5-chloro-7-trifluoromethyl-1,4-dihydro-2,3-quinoxalinedione; ACEA-1021, licostinel; AP5, 2-amino-5-phosphonopentanoate; AP7, 2-amino-7-phosphonopentanoate; CGP-61594, (±)-trans-4-[2-(4-azidophyenyl)acetylamino]-5,7-dichloro-1,2,3,4-tetrahydroquinoline-2-carboxylic acid; CGP-40116, d-(E)-2-amino-4-methyl-5-phosphono-3-pentenoic acid; CGP-43487, d-(E)-2-amino-4-methyl-5-phosphono-3-pentenoic acid methyl ester; CGP-58411, 7-chloro-4-hydroxy-3-phenyl-1H-quinolin-2-one. CGS-19755, (2R,4S)-4-(phosphonomethyl)piperidine-2-carboxylic acid; CPP, 4-(3-phosphonopropyl) pizerazine-2-carboxylic acid; GV150,526A, gavestinel; GV196,771A, (E)-4,6-dichloro-3-[(2-oxo-1-phenyl-3-pyrrolidinylidene)methyl]-1H-indole-2-carboxylic acid; L-689,560, 4-trans-2-carboxy-5,7-dichloro-4-phenylaminocarbonylamino-1,2,3,4-tetrahydroquinoline; L-701,324, 7-chloro-4-hydroxy-3-(3-phenoxy)phenyl-2(1H)-quinolone; MDL105,519, (E)-3-(2-phenyl-2-carboxyethenyl)-4, 6-dichloro-1H-indole-2-carboxylic acid; PBPD, (2S,3R)-1-(biphenyl-4-carbonyl)piperazine-2,3-dicarboxylic acid; PMPA, (R,S)-4-(phosphonomethyl)-piperazine-2-carboxylic acid; PPDA, (2S,3R)-1-(phenanthren-2-carbonyl)piperazine-2,3-dicarboxylic acid.

^a K_B values are from the Cheng-Prusoff correction of IC₅₀ values measured for inhibition of glycine-activated currents in mouse L(tk−) cells (Priestley et al., 1995).

^b Hess et al. (1998).

^c Hess et al. (1996).

^d Chopra et al. (2000).

^e Woodward et al. (1995a).

^f Woodward et al. (1995b).

^g Feng et al. (2005).

^h Frizelle et al. (2006).

ⁱ Feng et al. (2004).

^j Morley et al. (2005).

^k Twede et al. (2009).

^l Teichert et al. (2007).

^m K_d was calculated from on and off rates (Sheng et al., 2007).