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. 2011 Apr 15;2(7):352–362. doi: 10.1021/cn200013d

Table 1. In Vitro Binding Data for Aminocyclopentanesa.

graphic file with name cn-2011-00013d_0009.jpg

  configuration
 NR2B hERG
compd C1 C3 Ki (nM)b IP (nM)c
(R,R)-8 R R 830 15000
(R,S)-8 R S 480 20000
(S,R)-8 S R 2.8 3200
(S,S)-8 S S 3.6 22000
a

All values are the geometric mean of at least n = 4 measurements.

b

Inhibition of 3H-[(E)-N1-(2-methoxybenzyl)-cinnamamidine] binding to hNR1a/NR2B receptors expressed in Ltk- cells.43

c

Inhibition of MK-499 binding to hERG in HEK293 cells.44