Licostinel

Licostinel (INN) (code name ACEA-1021) is a competitive, silent antagonist of the glycine site of the NMDA receptor (Kb = 5 nM).[1][2][3] 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.[1][2][4] In clinical trials, licostinel did not produce phencyclidine-like psychotomimetic effects at the doses tested, though transient sedation, dizziness, and nausea were observed.[4][5] 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]

Licostinel
Clinical data
ATC code
  • None
Identifiers
IUPAC name
  • 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)
SMILES
  • c1c2c(c(c(c1Cl)Cl)[N+](=O)[O-])[nH]c(=O)c(=O)[nH]2
InChI
  • 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

See also

References
  1. Santokh Gill; Olga Pulido (31 January 2007). Glutamate Receptors in Peripheral Tissue: Excitatory Transmission Outside the CNS. Springer Science & Business Media. pp. 36–. ISBN 978-0-306-48644-9.
  2. Eugene I. Gusev; Veronika I. Skvortsova (30 April 2003). Brain Ischemia. Springer Science & Business Media. pp. 249–. ISBN 978-0-306-47694-5.
  3. Wilding TJ, Huettner JE (1996). "Antagonist pharmacology of kainate- and alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid-preferring receptors". Mol. Pharmacol. 49 (3): 540–6. PMID 8643094.
  4. Dalip J. S. Sirinathsinghji; Ray G. Hill (1 January 2002). Nmda Antagonists As Potential Analgesic Drugs. Springer Science & Business Media. pp. 151–. ISBN 978-3-7643-6011-5.
  5. Chas Bountra; Rajesh Munglani; William K. Schmidt (28 May 2013). Pain: Current Understanding, Emerging Therapies, and Novel Approaches to Drug Discovery. CRC Press. pp. 567–. ISBN 978-0-203-91125-9.


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