Licostinel (original) (raw)
Licostinel (INN) (code name ACEA-1021) is a competitive, silent antagonist of the glycine site of the NMDA receptor (Kb = 5 nM). 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. In clinical trials, licostinel did not produce phencyclidine-like psychotomimetic effects at the doses tested, though transient sedation, dizziness, and nausea were observed. 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).
| Property | Value |
|---|---|
| dbo:abstract | Licostinel (INN) (code name ACEA-1021) is a competitive, silent antagonist of the glycine site of the NMDA receptor (Kb = 5 nM). 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. In clinical trials, licostinel did not produce phencyclidine-like psychotomimetic effects at the doses tested, though transient sedation, dizziness, and nausea were observed. 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). (en) |
| dbo:casNumber | 153504-81-5 |
| dbo:fdaUniiCode | 3Z3037LJTC |
| dbo:pubchem | 5486198 |
| dbo:thumbnail | wiki-commons:Special:FilePath/Licostinel.svg?width=300 |
| dbo:wikiPageID | 44864713 (xsd:integer) |
| dbo:wikiPageLength | 4521 (xsd:nonNegativeInteger) |
| dbo:wikiPageRevisionID | 992416905 (xsd:integer) |
| dbo:wikiPageWikiLink | dbr:Psychotomimetic dbr:Cerebral_ischemia dbc:Chloroarenes dbc:NMDA_receptor_antagonists dbc:Nitro_compounds dbr:Competitive_antagonist dbr:Nausea dbr:Eliprodil dbr:Gavestinel dbr:Aptiganel dbr:Lubeluzole dbr:Stroke dbr:Clinical_trial dbr:Head_injury dbc:Neuroprotective_agents dbr:Kainate_receptor dbc:Quinoxalines dbr:International_Nonproprietary_Name dbr:AMPA_receptor dbc:AMPA_receptor_antagonists dbc:Kainate_receptor_antagonists dbr:Dizziness dbr:Phencyclidine dbr:Glycine_site dbr:Selfotel dbr:NMDA_receptor dbr:Sedation dbr:Silent_antagonist dbr:Neuroprotective_agent |
| dbp:alt | Skeletal formula (en) Ball-and-stick model of licostinel (en) |
| dbp:atcPrefix | None (en) |
| dbp:c | 8 (xsd:integer) |
| dbp:casNumber | 153504 (xsd:integer) |
| dbp:chemspiderid | 4588899 (xsd:integer) |
| dbp:cl | 2 (xsd:integer) |
| dbp:h | 3 (xsd:integer) |
| dbp:image | Licostinel molecule spacefill.png (en) |
| dbp:iupacName | 67 (xsd:integer) |
| dbp:n | 3 (xsd:integer) |
| dbp:o | 4 (xsd:integer) |
| dbp:pubchem | 5486198 (xsd:integer) |
| dbp:smiles | c1c2c[nH]cc[nH]2 (en) |
| dbp:stdinchi | 1 (xsd:integer) |
| dbp:stdinchikey | CHFSOFHQIZKQCR-UHFFFAOYSA-N (en) |
| dbp:unii | 3 (xsd:integer) |
| dbp:width | 180 (xsd:integer) |
| dbp:wikiPageUsesTemplate | dbt:Drugbox dbt:Ionotropic_glutamate_receptor_modulators dbt:Nervous-system-drug-stub dbt:Reflist dbt:Short_description dbt:Fdacite |
| dcterms:subject | dbc:Chloroarenes dbc:NMDA_receptor_antagonists dbc:Nitro_compounds dbc:Neuroprotective_agents dbc:Quinoxalines dbc:AMPA_receptor_antagonists dbc:Kainate_receptor_antagonists |
| gold:hypernym | dbr:Antagonist |
| rdf:type | owl:Thing dul:ChemicalObject dbo:ChemicalSubstance wikidata:Q8386 dbo:Drug |
| rdfs:comment | Licostinel (INN) (code name ACEA-1021) is a competitive, silent antagonist of the glycine site of the NMDA receptor (Kb = 5 nM). 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. In clinical trials, licostinel did not produce phencyclidine-like psychotomimetic effects at the doses tested, though transient sedation, dizziness, and nausea were observed. 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). (en) |
| rdfs:label | Licostinel (en) |
| owl:sameAs | freebase:Licostinel yago-res:Licostinel wikidata:Licostinel https://global.dbpedia.org/id/s894 |
| prov:wasDerivedFrom | wikipedia-en:Licostinel?oldid=992416905&ns=0 |
| foaf:depiction | wiki-commons:Special:FilePath/Licostinel.svg wiki-commons:Special:FilePath/Licostinel_molecule_spacefill.png |
| foaf:isPrimaryTopicOf | wikipedia-en:Licostinel |
| is dbo:wikiPageWikiLink of | dbr:ACEA dbr:Quinoxalinedione dbr:NMDA_receptor dbr:List_of_drugs:_Lf–Ln |
| is foaf:primaryTopic of | wikipedia-en:Licostinel |
