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Licostinel

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
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
PubChemCID
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 codeACEA-1021) is acompetitive,silent antagonist of theglycine site of theNMDA receptor (Kb = 5 nM).[1][2][3] It was under investigation by Acea Pharmaceuticals as aneuroprotective agent for the treatment ofcerebral ischemia associated withstroke andhead injuries but was ultimately never marketed.[1][2][4] Inclinical trials, licostinel did not producephencyclidine-likepsychotomimetic effects at the doses tested, though transientsedation,dizziness, andnausea were observed.[4][5] In addition to its actions at the NMDA receptor, licostinel also acts as an antagonist of theAMPA andkainate receptors at high concentrations (Kb = 0.9 μM and 2.5 μM, respectively).[3]

See also

[edit]

References

[edit]
  1. ^abSmall 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. ^abGusev EI, Skvortsova VI (30 April 2003)."Primary Neuroprotection".Brain Ischemia. Springer Science & Business Media. pp. 249–.ISBN 978-0-306-47694-5.
  3. ^abWilding 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. ^abBoyce 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.
AMPARTooltip α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor
KARTooltip Kainate receptor
NMDARTooltip N-Methyl-D-aspartate receptor
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