Articles producció científica> Ciències Mèdiques Bàsiques

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

  • Datos identificativos

    Identificador: PC:981
    Autores:
    Pereira, N.A.L.Sureda, F.X.Esplugas, R.Pérez, M.Amat, M.Santos, M.M.M.
    Resumen:
    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)
  • Otros:

    Autor según el artículo: Pereira, N.A.L. Sureda, F.X. Esplugas, R. Pérez, M. Amat, M. Santos, M.M.M.
    Departamento: Ciències Mèdiques Bàsiques
    e-ISSN: 1464-3405
    Autor/es de la URV: Nuno A. L. Pereira, Francesc X. Sureda, Roser Esplugas, Maria Pérez, Mercedes Amat and Maria M. M. Santos
    Resumen: 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)
    Acceso a la licencia de uso: https://creativecommons.org/licenses/by/3.0/es/
    Palabra clave otro idioma: Amantadine lactam tryptophanol derived oxazolopiperidone lactam derivative unclassified drug degenerative disease
    ISSN: 0960-894X
    Página final: 3336
    Volumen de revista: 24
    Versión del articulo depositado: info:eu-repo/semantics/submittedVersion
    Enlace a la fuente original: http://www.sciencedirect.com/science/article/pii/S0960894X14006349
    URL Documento de licencia: https://repositori.urv.cat/ca/proteccio-de-dades/
    DOI del artículo: https://doi.org/10.1016/j.bmcl.2014.05.105
    Entidad: Universitat Rovira i Virgili.
    Año de publicación de la revista: 2014
    Página inicial: 3333
  • Palabras clave:

    Sistema nerviós -- degeneració
    0960-894X
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