Article · Wikipedia archive · Last revised Jul 23, 2026

Licostinel

Licostinel is a competitive, silent antagonist of the glycine site of the NMDA receptor. It was under investigation by Acea Pharmaceuticals as a neuroprotective agent for the treatment of cerebral ischemia associated with stroke and head injuries but was ultimately never marketed. In clinical trials, licostinel did not produce phencyclidine-like psychotomimetic effects at the doses tested, though transient sedation, dizziness, and nausea were observed. In addition to its actions at the NMDA receptor, licostinel also acts as an antagonist of the AMPA and kainate receptors at high concentrations.

Last revised
Jul 23, 2026
Read time
≈ 1 min
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302 w
Citations
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Wikipedia ↗
Licostinel
Skeletal formula
Ball-and-stick model of licostinel
Clinical data
Other namesACEA-1021
ATC code
  • None
Identifiers
  • 6,7-Dichloro-5-nitro-1,4-dihydro-2,3-quinoxalinedione
CAS Number
PubChem CID
ChemSpider
UNII
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC8H3Cl2N3O4
Molar mass276.03 g·mol−1
3D model (JSmol)
  • c1c2c(c(c(c1Cl)Cl)[N+](=O)[O-])[nH]c(=O)c(=O)[nH]2
  • InChI=1S/C8H3Cl2N3O4/c9-2-1-3-5(6(4(2)10)13(16)17)12-8(15)7(14)11-3/h1H,(H,11,14)(H,12,15)
  • Key:CHFSOFHQIZKQCR-UHFFFAOYSA-N

Licostinel (INN; development code ACEA-1021) is a competitive, silent antagonist of the glycine site of the NMDA receptor (Kb = 5 nM).123 It was under investigation by Acea Pharmaceuticals as a neuroprotective agent for the treatment of cerebral ischemia associated with stroke and head injuries but was ultimately never marketed.124 In clinical trials, licostinel did not produce phencyclidine-like psychotomimetic effects at the doses tested, though transient sedation, dizziness, and nausea were observed.45 In addition to its actions at the NMDA receptor, licostinel also acts as an antagonist of the AMPA and kainate receptors at high concentrations (Kb = 0.9 μM and 2.5 μM, respectively).3

See also

See also

References

References

  1. Small DL, Tauskela JS (31 January 2007). "Glutamate Receptor Pharmacology: Lessons Learned from the Last Decade of Stroke Trials". In Gill S, Pulido O (eds.). Glutamate Receptors in Peripheral Tissue: Excitatory Transmission Outside the CNS. Springer Science & Business Media. pp. 36–. ISBN 978-0-306-48644-9.
  2. Gusev EI, Skvortsova VI (30 April 2003). "Primary Neuroprotection". Brain Ischemia. Springer Science & Business Media. pp. 249–. ISBN 978-0-306-47694-5.
  3. Wilding TJ, Huettner JE (March 1996). "Antagonist pharmacology of kainate- and alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid-preferring receptors". Molecular Pharmacology. 49 (3): 540–546. PMID 8643094.
  4. Boyce SG, Rupniak N (1 January 2002). "Behavioural studies on the potential of NMDA receptor antagonists as analgesics". In Sirinathsinghji DJ, Hill RG (eds.). NMDA Antagonists As Potential Analgesic Drugs. Springer Science & Business Media. pp. 151–. ISBN 978-3-7643-6011-5.
  5. Chizh BA, Headly PM (28 May 2013). "N-Methyl-D-Aspartate (NMDA) Receptors as Target for Pain Therapy". In Bountra C, Munglani R, Schmidt WK (eds.). Pain: Current Understanding, Emerging Therapies, and Novel Approaches to Drug Discovery. CRC Press. pp. 567–. ISBN 978-0-203-91125-9.