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. Author manuscript; available in PMC: 2013 Sep 1.
Published in final edited form as: Neurochem Int. 2012 Jan 17;61(4):581–592. doi: 10.1016/j.neuint.2012.01.004

Table 1.

Pharmacological data for the activity of compounds on NMDAR subtypes

Compound GluN1/GluN2A GluN1/GluN2B GluN1/GluN2C GluN1/GluN2D
L-Glutamate Binding Site D-AP5a 0.28 ± 0.02 0.46 ± 0.14 1.64 ± 0.14 3.71 ± 0.67
CPPa 0.041 ± 0.003 0.27 ± 0.02 0.63 ± 0.05 1.99 ± 0.20
UBP141b 44.1 ± 1.7 10.4 ± 2.1 3.22 ± 0.31 2.57 ± 0.16
UBP145b 16.1 ± 2.3 6.32 ± 0.20 2.22 ± 0.55 0.94 ± 0.34
NVP-AAM077c 0.0054 ± 0.0004 0.067 ± 0.003 0.012 ± 0.001 0.037 ± 0.004
Channel Blocker Memantined 13.4 ± 1.3 10.4 ± 0.4 1.61 ± 0.06 1.76 ± 0.06
NTD binding Ifenprodile 40 0.11 29 76
Ro 25-6981f 52 0.009
Allosteric Modulators TCN 201g 0.16 >50 >30 >30
QNZ46h 182 ± 24 193 ± 45 7.1 ± 0.4 3.9 ± 0.2
UBP512i ≫300i ≫300 51 ± 11j 46 ± 6j
UBP608j 18.6 ± 1.4 90 ± 4 68 ± 9 426 ± 40
UBP618j 1.8 ± 0.2 2.4 ± 0.1 2.0 ± 0.1 2.4 ± 0.3
UBP710k (24 ± 1)l (51 ± 3) (3.6 ± 1.5) (2.6 ± 1.4)
UBP551 9.7 ± 0.2j 9.4 ± 0.6j 15 ± 6j (50 ± 4)k
UBP646k (32 ± 10) (34 ± 9) (22 ± 8) (45 ± 8)
CIQm >10 >10 (2.7) (2.8)
a

Data represents Ki values (μM) ± s.e.m., (Feng et al., 2005)

b

Data represents KB values (μM) ± s.e.m., (Costa et al., 2009)

c

Data represents Ki values (μM) ± s.e.m., (Feng et al., 2004; therein referred to as PEAQX). Schild plot KB values: GluN1/GluN2A 0.015 μM; GluN1/GluN2B, 0.078 μM (Frizelle et al., 2006)

d

Data represents IC50 values (μM) ± s.e.m, obtained in the presence of 1 mM Mg2+, Kotermanski and Johnson, 2009

e

Data represents IC50 values (μM) at human receptors, Hess et al., 1996

f

Data represents IC50 values (μM), Fischer et al., 1997

g

Data represents IC50 values (μM), Bettini et al., 2010

h

Data represents IC50 values (μM) ± s.e.m, Hansen and Traynelis, 2011

i

UBP512 is a weak potentiator of agonist-induced effects on GluN1/GluN2A and inactive at GluN1/GluN2B when tested at 100–300 μM.

j

Data represents IC50 values (μM) ± s.e.m, Costa et al., 2010

k

Data represents % potentiation ± s.e.m. of agonist-induced responses by 100 μM compound, Costa et al., 2010

l

Potentiation of responses are indicated by values in parentheses.

m

Data represents EC50 values (μM), Mullasseril et al., 2010