Articles producció científica> Ciències Mèdiques Bàsiques

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

  • Identification data

    Identifier: PC:981
    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:

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

    Sistema nerviós -- degeneració
    0960-894X
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