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. 2010 Dec 10;2(2):60–74. doi: 10.1021/cn1001039

Table 5. Chemical Structures and Pharmacological Profile of Isatin Oxime Analogues 5.15.3a.

graphic file with name cn-2010-001039_0008.jpg

  GluA1
GluA2 GluK1
GluK2
cmpd bind. func. bind. bind. func. bind. func.
5.1 (NS 102) b b b b 6c 1.4d b
5.2 (NS 257)e b 0.97 b b b b 2.3
5.3 ((R/S)-NS 1209) 0.12g b 0.030g 0.74g 0.63f 6.2g 65f
a

All values in [μM].

b

Not tested.

c

KB value for inhibition of Ca2+ influx in rat dorsal root ganglion (DRG) neurons; from ref (49),.

d

Displacement of [3H]KA radioligand; from ref (65).

e

IC50 values for inhibition of KA-induced depolarization in the appropriate mRNA-injected Xenopus oocytes; from ref (67).

f

IC50 values for inhibition of domoate-induced currents in HEK293 cells; from ref (68).

g

Displacement of [3H]AMPA radioligand; from ref (69).