Chemical Name:4,6-Bis(benzoylamino)-1,3-benzenedicarboxylic acid
Biological Activity:
Selective
non-competitive kainate receptor antagonist; displays selectivity for GLUK5
subunit-containing receptors (IC50 values are 1.6 and > 30 μM for homomeric GLUK5 and
GLUK6 receptors respectively). Has minimal activity at AMPA and NMDA
receptors (IC50 >> 30 μM).
Christensenet al (2004) In vitro
characterization of 5-carboxyl-2,4-di-benzamido-benzoic acid (NS3763), a
noncompetitive antagonist of GLUK5 receptors. J.Pharmacol.Exp.Ther. 309
1003.
Displays 26-fold and > 440-fold selectivity over kainate and NMDA receptors respectively. Neuro-protective; delays neuronal death in a global ischaemia model and cerebral infarction in a focal ischaemia model.