zelquistinel
Sign in to saveAlso known as AGN-241751, GATE-251
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 Syndeio Biosciences, and previously by Allergan.
Wikidata facts
- Mass
- 327.1794209
Show 4 more facts
- isomeric SMILES
- C[C@@H](O)[C@@H](C(N)=O)N1C[C@@]2(CCCN2C(=O)OC(C)(C)C)C1=O
- Commons category
- Zelquistinel
- chemical formula
- C₁₅H₂₅N₃O₅
- canonical SMILES
- CC(O)C(C(N)=O)N1CC2(CCCN2C(=O)OC(C)(C)C)C1=O
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Article
5 sectionsContents
- Pharmacology
- Clinical development
- See also
- References
- External links
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 Syndeio Biosciences, and previously by Allergan.
== Pharmacology == 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. The mean half-life of Zelquistinel is reported to be from 1.21 to 2.06 hours, reaching peak plasma concentrations 30 minutes after administration.