Licostinel

From Wikipedia, the free encyclopedia
Jump to navigation Jump to search
Licostinel
Skeletal formula
Ball-and-stick model of licostinel
Clinical data
ATC code
  • None
Identifiers
CAS Number
PubChem CID
ChemSpider
Chemical and physical data
Formula C8H3Cl2N3O4
Molar mass 276.033 g/mol
3D model (JSmol)

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[edit]

References[edit]

  1. ^ a b 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. ^ a b Eugene I. Gusev; Veronika I. Skvortsova (30 April 2003). Brain Ischemia. Springer Science & Business Media. pp. 249–. ISBN 978-0-306-47694-5. 
  3. ^ a b c 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. ^ a b 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.