Antagonism of recombinant and native GluK3-containing kainate receptors.
Neuropharmacology. 2009-01-01; 56(1): 131-140
DOI: 10.1016/j.neuropharm.2008.08.002
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1. Neuropharmacology. 2009 Jan;56(1):131-40. doi: 10.1016/j.neuropharm.2008.08.002.
Epub 2008 Aug 12.
Antagonism of recombinant and native GluK3-containing kainate receptors.
Perrais D(1), Pinheiro PS, Jane DE, Mulle C.
Author information:
(1)Laboratoire Physiologie Cellulaire de la Synapse, CNRS UMR 5091, Bordeaux
Neuroscience Institute, University of Bordeaux, 33077 Bordeaux, France.
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.
DOI: 10.1016/j.neuropharm.2008.08.002
PMID: 18761361 [Indexed for MEDLINE]