Articles producció científicaCiències Mèdiques Bàsiques

Tryptophanol-derived oxazolopiperidone lactams: Identification of a hit compound as NMDA receptor antagonist

  • Identification data

    Identifier:  PC:981
    Handle: https://hdl.handle.net/20.500.11797/PC981
    Authors:  Pereira, N.A.L.; Sureda, F.X.; Esplugas, R.; Pérez, M.; Amat, M.; Santos, M.M.M.
    Abstract:
    N-Methyl-d-aspartate receptors (NMDAR) exacerbated activation leads to neuron death through a phenomenon called excitotoxicity. These receptors are implicated in several neurological diseases (e.g., Alzheimer and Parkinson) and thus represent an important therapeutic target. We herein describe the study of enantiopure tryptophanol-derived oxazolopiperidone lactams as NMDA receptor antagonists. The most active hit exhibited an IC50 of 63.4 µM in cultured rat cerebellar granule neurons thus being 1.5 fold more active than clinically approved NMDA antagonist amantadine (IC50 = 92 µM)

  • Others:

    Link to the original source: http://www.sciencedirect.com/science/article/pii/S0960894X14006349
    Article's DOI: https://doi.org/10.1016/j.bmcl.2014.05.105
    Journal publication year: 2014
    Entity: Universitat Rovira i Virgili.
    Paper version: info:eu-repo/semantics/submittedVersion
    First page: 3333
    URV's Author/s: Nuno A. L. Pereira, Francesc X. Sureda, Roser Esplugas, Maria Pérez, Mercedes Amat and Maria M. M. Santos
    Department: Ciències Mèdiques Bàsiques
    Licence document URL: https://repositori.urv.cat/ca/proteccio-de-dades/
    Last page: 3336
    Keyword in other language: Amantadine, lactam, tryptophanol derived oxazolopiperidone lactam derivative, unclassified drug, degenerative disease
    ISSN: 0960-894X
    Author, as appears in the article.: Pereira, N.A.L., Sureda, F.X., Esplugas, R., Pérez, M., Amat, M., Santos, M.M.M.
    licence for use: https://creativecommons.org/licenses/by/3.0/es/
    Journal volume: 24
    e-ISSN: 1464-3405

  • Keywords:

    Sistema nerviós -- degeneració
    0960-894X

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