Chemistry:Licostinel
From HandWiki
Short description: Chemical compound
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| Formula | C8H3Cl2N3O4 |
| Molar mass | 276.03 g·mol−1 |
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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]
See also
References
- ↑ 1.0 1.1 "Glutamate Receptor Pharmacology: Lessons Learned from the Last Decade of Stroke Trials". Glutamate Receptors in Peripheral Tissue: Excitatory Transmission Outside the CNS. Springer Science & Business Media. 31 January 2007. pp. 36–. ISBN 978-0-306-48644-9. https://books.google.com/books?id=wcjiZ58mypIC&pg=PA36.
- ↑ 2.0 2.1 "Primary Neuroprotection". Brain Ischemia. Springer Science & Business Media. 30 April 2003. pp. 249–. ISBN 978-0-306-47694-5. https://books.google.com/books?id=TLla0xisFkoC&pg=PA249.
- ↑ 3.0 3.1 "Antagonist pharmacology of kainate- and alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid-preferring receptors". Molecular Pharmacology 49 (3): 540–546. March 1996. PMID 8643094. http://molpharm.aspetjournals.org/cgi/pmidlookup?view=long&pmid=8643094.
- ↑ 4.0 4.1 "Behavioural studies on the potential of NMDA receptor antagonists as analgesics". NMDA Antagonists As Potential Analgesic Drugs. Springer Science & Business Media. 1 January 2002. pp. 151–. ISBN 978-3-7643-6011-5. https://books.google.com/books?id=pIDGlb1ISCgC&pg=PA151.
- ↑ "N-Methyl-D-Aspartate (NMDA) Receptors as Target for Pain Therapy". Pain: Current Understanding, Emerging Therapies, and Novel Approaches to Drug Discovery. CRC Press. 28 May 2013. pp. 567–. ISBN 978-0-203-91125-9. https://books.google.com/books?id=anRzslvfcUwC&pg=PA567.
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