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Antidepressant
Zelquistinel
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    Zelquistinel

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    Zelquistinel
    Zelquistinel.svg
    Clinical data
    Routes of
    administration    		 By mouth
    Drug class NMDA receptor modulator
    Identifiers
    • tert-butyl (4S)-2-[(2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl]-3-oxo-2,5-diazaspiro[3.4]octane-5-carboxylate
    CAS Number
    PubChem CID
    ChemSpider
    UNII
    Chemical and physical data
    Formula C15H25N3O5
    Molar mass 327.381 g·mol−1
    3D model (JSmol)
    • C[C@H]([C@@H](C(=O)N)N1C[C@]2(C1=O)CCCN2C(=O)OC(C)(C)C)O
    • InChI=1S/C15H25N3O5/c1-9(19)10(11(16)20)17-8-15(12(17)21)6-5-7-18(15)13(22)23-14(2,3)4/h9-10,19H,5-8H2,1-4H3,(H2,16,20)/t9-,10+,15+/m1/s1
    • Key:ABAPCYNTEPGBNJ-FTGAXOIBSA-N

    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.

    See also

    External links


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