Kynurenic Acid - Mechanism of Action

Mechanism of Action

KYNA has been proposed to act on four targets:

  • As an antagonist at ionotropic AMPA, NMDA and Kainate glutamate receptors in the concentration range of 0.1-2.5 mM
  • As a noncompetitive antagonist at the glycine site of the NMDA receptor.
  • As an antagonist of the α7 nicotinic acetylcholine receptor. However, recently (2011) direct recording of α7 nicotinic acetylcholine receptor currents in adult (noncultured) hippocampal interneurons by the Cooper laboratory validated a 2009 study that failed to find any blocking effect of kynurenic acid across a wide range of concentrations, thus suggesting that in noncultured, intact preparations from adult animals there is no effect of kynurenic acid on α7 nicotinic acetylcholine receptor currents
  • As a ligand for the orphan G protein-coupled receptor GPR35. Another tryptophan metabolite, 5-hydroxyindoleacetic acid exerts its effects via the orphan G protein-coupled receptor GPR35

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