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
URL Documento de licencia: https://repositori.urv.cat/ca/proteccio-de-dades/
Entidad: Universitat Rovira i Virgili.
Año de publicación de la revista: 2014
Página inicial: 3333