Licostinel

Licostinel
Systematic (IUPAC) name
6,7-Dichloro-5-nitro-1,4-dihydro-2,3-quinoxalinedione
Clinical data
Identifiers
153504-81-5
None
PubChem CID 5486198
ChemSpider 4588899
Chemical data
Formula C8H3Cl2N3O4
276.033 g/mol

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.[2][1][4] In clinical trials, licostinel did not produce phencyclidine-like psychotomimetic effects at the doses tested, though transient sedation, dizziness, and nausea were observed.[5][4] 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

  1. ↑ 1.0 1.1 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. ↑ 2.0 2.1 Eugene I. Gusev; Veronika I. Skvortsova (30 April 2003). Brain Ischemia. Springer Science & Business Media. pp. 249–. ISBN 978-0-306-47694-5.
  3. ↑ 3.0 3.1 3.2 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. ↑ 4.0 4.1 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.