Chemical Name:(S)-1-(2-Amino-2-carboxyethyl)-3-(2-carboxybenzyl)pyrim
idine-2,4-dione
Biological Activity:
Selective
and potent GLUK5 (GluR5)-subunit containing kainate receptor
antagonist (apparent KD = 402 nM); active enantiomer of UBP 296
(Cat. No. 2078). Displays ~ 260-fold selectivity over AMPA receptors. UBP 296
displays ~ 90-fold selectivity over recombinant human GLUK6- and GLUK2-containing
kainate receptors, has little or no action at NMDA or group I mGlu receptors
and 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.
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.