Zelquistinel (original) (raw)
Zelquistinel (GATE-251, formerly AGN-241751) is an orally active small-molecule NMDA receptor modulator which is under development for the treatment of major depressive disorder (MDD) by Gate Neurosciences, and previously by Allergan. Zelquistinel acts through a unique binding site on the NMDA receptor, independent of the glycine site, to modulate receptor activity and enhance NMDAR-mediated synaptic plasticity. Its mechanism of action is similar to that of rapastinel. However, unlike rapastinel, zelquistinel is orally bioavailable, exhibits increased potency, and has improved drug properties.
| Property | Value |
|---|---|
| dbo:abstract | Zelquistinel (GATE-251, formerly AGN-241751) is an orally active small-molecule NMDA receptor modulator which is under development for the treatment of major depressive disorder (MDD) by Gate Neurosciences, and previously by Allergan. Zelquistinel acts through a unique binding site on the NMDA receptor, independent of the glycine site, to modulate receptor activity and enhance NMDAR-mediated synaptic plasticity. Its mechanism of action is similar to that of rapastinel. However, unlike rapastinel, zelquistinel is orally bioavailable, exhibits increased potency, and has improved drug properties. On July 23, 2018, the U.S. FDA granted Fast Track designation to the development of zelquistinel as an investigational new treatment for major depressive disorder. As of August 2019, the drug had completed a phase IIa clinical trial. (en) |
| dbo:casNumber | 2151842-64-5 |
| dbo:class | dbr:NMDA_receptor_modulator |
| dbo:fdaUniiCode | 387WYR6N95 |
| dbo:pubchem | 132155398 |
| dbo:thumbnail | wiki-commons:Special:FilePath/Zelquistinel.svg?width=300 |
| dbo:wikiPageExternalLink | https://adisinsight.springer.com/drugs/800031388 |
| dbo:wikiPageID | 57708479 (xsd:integer) |
| dbo:wikiPageLength | 5153 (xsd:nonNegativeInteger) |
| dbo:wikiPageRevisionID | 1113271459 (xsd:integer) |
| dbo:wikiPageWikiLink | dbr:FDA_Fast_Track_Development_Program dbr:List_of_investigational_antidepressants dbc:Experimental_drugs dbr:Oral_administration dbr:Apimostinel dbr:Major_depressive_disorder dbr:Clinical_trial dbc:NMDA_receptor_modulators dbc:Antidepressants dbr:Rapastinel dbr:Mechanism_of_action dbr:Phases_of_clinical_research dbr:NMDA_receptor_modulator dbr:Small-molecule |
| dbp:c | 15 (xsd:integer) |
| dbp:casNumber | 2151842 (xsd:integer) |
| dbp:chemspiderid | 81367638 (xsd:integer) |
| dbp:class | dbr:NMDA_receptor_modulator |
| dbp:h | 25 (xsd:integer) |
| dbp:iupacName | tert-butyl -2-[-1-amino-3-hydroxy-1-oxobutan-2-yl]-3-oxo-2,5-diazaspiro[3.4]octane-5-carboxylate (en) |
| dbp:n | 3 (xsd:integer) |
| dbp:o | 5 (xsd:integer) |
| dbp:pubchem | 132155398 (xsd:integer) |
| dbp:routesOfAdministration | dbr:Oral_administration |
| dbp:smiles | C[C@H]O (en) |
| dbp:stdinchi | 1 (xsd:integer) |
| dbp:stdinchikey | ABAPCYNTEPGBNJ-FTGAXOIBSA-N (en) |
| dbp:unii | 387 (xsd:integer) |
| dbp:wikiPageUsesTemplate | dbt:Drugbox dbt:Ionotropic_glutamate_receptor_modulators dbt:Nervous-system-drug-stub dbt:Reflist dbt:Fdacite |
| dcterms:subject | dbc:Experimental_drugs dbc:NMDA_receptor_modulators dbc:Antidepressants |
| rdf:type | owl:Thing dul:ChemicalObject dbo:ChemicalSubstance wikidata:Q8386 dbo:Drug |
| rdfs:comment | Zelquistinel (GATE-251, formerly AGN-241751) is an orally active small-molecule NMDA receptor modulator which is under development for the treatment of major depressive disorder (MDD) by Gate Neurosciences, and previously by Allergan. Zelquistinel acts through a unique binding site on the NMDA receptor, independent of the glycine site, to modulate receptor activity and enhance NMDAR-mediated synaptic plasticity. Its mechanism of action is similar to that of rapastinel. However, unlike rapastinel, zelquistinel is orally bioavailable, exhibits increased potency, and has improved drug properties. (en) |
| rdfs:label | Zelquistinel (en) |
| owl:sameAs | wikidata:Zelquistinel https://global.dbpedia.org/id/7boPW |
| prov:wasDerivedFrom | wikipedia-en:Zelquistinel?oldid=1113271459&ns=0 |
| foaf:depiction | wiki-commons:Special:FilePath/Zelquistinel.svg |
| foaf:isPrimaryTopicOf | wikipedia-en:Zelquistinel |
| is dbo:wikiPageRedirects of | dbr:AGN-241751 dbr:AGN-241,751 dbr:AGN241751 dbr:AGN_241,751 dbr:AGN_241751 |
| is dbo:wikiPageWikiLink of | dbr:AGN-241751 dbr:AGN-241,751 dbr:AGN241751 dbr:AGN_241,751 dbr:AGN_241751 |
| is foaf:primaryTopic of | wikipedia-en:Zelquistinel |
