Cited by 79Tryptophan and brain disordersAmino Acid Enzymes and MetabolismNeuroscience and Neuropharmacology Research

Kynurenic acid antagonists and kynurenine pathway inhibitors

Stone, Trevor W·2001·Expert Opinion on Investigational Drugs

Abstract

The kynurenine pathway accounts for the metabolism of around 80% of non-protein tryptophan metabolism. It includes both an agonist (quinolinic acid) at NMDA receptors and an antagonist (kynurenic acid). Since their discovery, there has been a major development of kynurenic acid analogues as neuroprotectants for the treatment of stroke and neurodegenerative disease. Several prodrugs of kynurenic acid or its analogues that can be hydrolysed within the CNS are also available. More recently, the pathway itself has proved to be a valuable drug target, affected by agents which reduce the synthesis of quinolinic acid and increase the formation of kynurenic acid. The change in the balance of these, away from the excitotoxin and towards the neuroprotectant, has anticonvulsant and neuroprotective properties.

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Crossref · 10.1517/13543784.10.4.633

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111 of 111 references verified0 citation errors · 0 not checkable

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  • Kynurenic acid is usually neuroprotective as an NMDA receptor antagonist, whereas quinolinic acid acts as an NMDA receptor agonist and exerts neurotoxic effects.

    “As an antagonist to the N-methyl-d-aspartate (NMDA) receptor, kynurenic acid is usually neuroprotective, whereas quinolinic acid acts as an agonist to the NMDA receptor and exerts neurotoxic effects (393).”

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Authors
Stone, T. W.
Affiliations
University of Glasgow (GB)
Corresponding author
Stone, Trevor W
Venue
Expert Opinion on Investigational Drugs
Published
2001-04
Volume
10
Issue
4
Pages
633-645
ISSN
  • 1354-3784 (ISSN-L)
  • 1744-7658
OpenAlex
W2106566895
Cited by
79
References
111
Citations by year
2026: 4 · 2025: 5 · 2024: 6 · 2023: 3 · 2022: 4 · 2021: 1 · 2020: 4 · 2019: 3 · 2018: 2 · 2017: 2 · 2016: 1 · 2015: 2 · 2014: 2 · 2013: 1 · 2012: 5
FWCI
0.31
Type
journal article
Language
en
Open access
closed
Locations
  • Expert Opinion on Investigational Drugs (publishedVersion)
  • PubMed (publishedVersion)
  • ENLIGHTEN (Jurnal Bimbingan dan Konseling Islam) (submittedVersion)
Topics
  • Life Sciences › Neuroscience › Biological Psychiatry › Tryptophan and brain disorders
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Biochemistry › Amino Acid Enzymes and Metabolism
  • Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuroscience and Neuropharmacology Research
Keywords
kynurenic acid, kynurenine pathway, tryptophan metabolism, quinolinic acid, NMDA receptor antagonists, prodrugs, neuroprotection, stroke, neurodegenerative diseases, antiepileptic drugs, excitotoxicity
MeSH terms
Brain Ischemia, Epilepsy, Humans, Kynurenic Acid, Kynurenine, Parkinson Disease, Prodrugs, Schizophrenia, Quinolinic Acid, Excitatory Amino Acid Antagonists, Neuroprotective Agents

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