4-Alkylidenyl glutamic acids, potent and selective GluR5 agonists

Bioorg Med Chem Lett. 2000 Aug 21;10(16):1807-10. doi: 10.1016/s0960-894x(00)00346-2.

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

  • Animals
  • Cell Line
  • Cells, Cultured
  • Ganglia, Spinal / cytology
  • Humans
  • Kidney / cytology
  • Kidney / embryology
  • Ligands
  • Molecular Structure
  • Neurons, Afferent / metabolism
  • Pyrrolidonecarboxylic Acid / analogs & derivatives*
  • Pyrrolidonecarboxylic Acid / chemical synthesis
  • Pyrrolidonecarboxylic Acid / chemistry
  • Pyrrolidonecarboxylic Acid / metabolism
  • Pyrrolidonecarboxylic Acid / pharmacology
  • Radioligand Assay
  • Rats
  • Receptors, Kainic Acid / agonists*
  • Receptors, Kainic Acid / metabolism
  • Structure-Activity Relationship

Substances

  • Gluk1 kainate receptor
  • Gluk2 kainate receptor
  • Ligands
  • Receptors, Kainic Acid
  • Pyrrolidonecarboxylic Acid