Antagonism of recombinant and native GluK3-containing kainate receptors

D Perrais, PS Pinheiro, DE Jane, C Mulle

Research output: Contribution to journalArticle (Academic Journal)

50 Citations (Scopus)


A number of kainate receptor antagonists have shown selectivity for receptors containing the GluK1 subunit. Here, we analyze the effects of these GluK1 antagonists on currents mediated by recombinant homomeric GluK3 and heteromeric GluK2/3 receptors expressed in HEK 293 cells and activated by fast application of glutamate. We show that, amongst these compounds, UBP302, UBP310 and UBP316 effectively block recombinant homomeric GluK3 receptors. However, these antagonists are ineffective in blocking homomeric GluK2 or heteromeric GluK2/3 receptors. In addition, these antagonists do not affect presynaptic kainate receptors at mouse hippocampal mossy fibre synapses, which are thought to be composed of GluK2 and GluK3 subunits. Moreover, the AMPA receptor-selective non-competitive antagonist GYKI 53655 blocks, at high concentrations, GluK3-containing receptors and decreases short-term plasticity at mossy fibre synapses. These results expand the range of targets of kainate receptor antagonists and provide pharmacological tools to study the elusive mechanisms of neurotransmitter control by presynaptic kainate receptors.
Translated title of the contributionAntagonism of recombinant and native GluK3-containing kainate receptors
Original languageEnglish
Pages (from-to)131 - 140
Number of pages10
Issue number1
Publication statusPublished - Jan 2009

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