Abstract
Twenty-four 4-alkylidene glutamic acids were synthesised and tested as potential subtype selective GluR5 and 6 ligands. It was found that a critical size of alkylidene group gave potent and selective GluR5 receptor agonists. LY339624 had Kis of 0.0326 and >100 microM on GluR5 and 6 receptors, respectively.
MeSH terms
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Animals
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Cell Line
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Cells, Cultured
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Ganglia, Spinal / cytology
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GluK2 Kainate Receptor
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Humans
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Kidney / cytology
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Kidney / embryology
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Ligands
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Molecular Structure
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Neurons, Afferent / metabolism
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Pyrrolidonecarboxylic Acid / analogs & derivatives*
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Pyrrolidonecarboxylic Acid / chemical synthesis
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Pyrrolidonecarboxylic Acid / chemistry
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Pyrrolidonecarboxylic Acid / metabolism
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Pyrrolidonecarboxylic Acid / pharmacology
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Radioligand Assay
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Rats
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Receptors, Kainic Acid / agonists*
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Receptors, Kainic Acid / metabolism
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Structure-Activity Relationship
Substances
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Gluk1 kainate receptor
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Ligands
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Receptors, Kainic Acid
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Pyrrolidonecarboxylic Acid