Licostinel

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Licostinel
Licostinel.svg
Systematic (IUPAC) name
6,7-Dichloro-5-nitro-1,4-dihydro-2,3-quinoxalinedione
Identifiers
CAS Number 153504-81-5
ATC code None
PubChem CID: 5486198
ChemSpider 4588899
Chemical data
Formula C8H3Cl2N3O4
Molecular mass 276.033 g/mol
  • 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) (code name ACEA-1021) is a competitive, silent antagonist of the glycine site of the NMDA receptor (Kb = 5 nM).[1][2][3][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]

See also

References

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  3. ↑ 3.0 3.1 3.2 Lua error in package.lua at line 80: module 'strict' not found.
  4. ↑ 4.0 4.1 Lua error in package.lua at line 80: module 'strict' not found.
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