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Potent and selective GluR5-containing kainate receptor antagonist (IC50 = 7 nM) that displays selectivity over GluR6-containing kainate, NMDA, AMPA and group I mGlu receptors. Reversibly blocks induction of NMDA recptor-independent long term potentiation (LTP) in vitro at nanomolar concentrations.
Dolman et al (2007) Synthesis and pharmacological characterisation of N3-substituted willardiine derivatives: role of the substituent at the 5-position of the uracil ring in the development of highly potent and selective GLUK5 kainate receptor antagonists. J.Med.Chem. 50 1558. Dargan et al (2009) ACET is a highly potent and specific kainate receptor antagonist: Characterisation and effects on hippocampal mossy fibre function. Neuropharmacology 56 121.
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