Chemical Name:(RS)-1-(2-Amino-2-carboxyethyl)-3-(2-carboxybenzyl)pyri
midine-2,4-dione
Biological Activity:
Selective
and potent GLUK5 (GluR5)-subunit containing kainate receptor
antagonist (apparent KD = 1.09 μM). Displays ~ 90-fold selectivity
over AMPA receptors and recombinant human GLUK6- and GLUK2-containing
kainate receptors. Has little or no action at NMDA or group I mGlu receptors.
Selectively blocks kainate receptor-mediated LTP induction in rat hippocampal
mossy fibres.
Moreet al
(2004) Characterisation of UBP296: a novel, potent and selective kainate
receptor antagonist. Neuropharmacology 47 46. Dolmanet
al (2005) Synthesis and pharmacology of willardiine derivatives acting as
antagonists of kainate receptors. J.Med.Chem. 48 7867.