English   español  
Por favor, use este identificador para citar o enlazar a este item: http://hdl.handle.net/10261/141535
COMPARTIR / IMPACTO:
Estadísticas
logo share SHARE logo core CORE   Add this article to your Mendeley library MendeleyBASE

Visualizar otros formatos: MARC | Dublin Core | RDF | ORE | MODS | METS | DIDL
Exportar a otros formatos:
Título

1,3-diphenylpropan-1-ones as allosteric modulators of α7 nACh receptors with analgesic and antioxidant properties

AutorCriado, Manuel; Balsera, Beatriz; Mulet Soler, José; Sala, Salvador; Torre-Martínez, Roberto de la; Fernández-Carvajal, Asia; Ferrer-Montiel, Antonio; Moreno-Fernández, Silvia; Miguel, Marta ; Pérez de Vega, M. Jesús; González-Muñiz, Rosario
Palabras claveAlpha7 nAChR
Pain
Inflammation
Antioxidant
Positive allosteric modulator
Fecha de publicación2016
EditorFuture Science
CitaciónFuture Medicinal Chemistry 8: 731-749 (2016)
ResumenNicotine acethylcholine receptors (nAChRs) play critical roles in cognitive processes, neuroprotection and inflammation. Results: According to their substituents, 1,3-diphenylpropan-1-one derivatives act as α7 nAChRs negative allosteric modulators (NAM, OMe) or Type I positive allosteric modulators (PAMs, OH). Compounds 7 and 31 were the most effective (989 and 666% enhancement of ACh-induced currents) and potent (EC: 12.9 and 6.85 μM) PAMs. They exhibited strong radical scavenging values. Compound 31, selective over other neuronal nAChR subtypes and with acceptable pharmacokinetic profile, showed antinociceptive effects in a model of inflammatory pain. Conclusion: Compound 31 is a novel, potent and selective α7 nAChR PAM, displaying antioxidant and analgesic activities. The 1,3-diphenylpropan-1-one scaffold could be the base toward more advanced type I PAMs for the treatment of nAChR-mediated diseases.
Versión del editorhttp://dx.doi.org/10.4155/fmc-2015-0001
URIhttp://hdl.handle.net/10261/141535
DOI10.4155/fmc-2015-0001
Identificadoresdoi: 10.4155/fmc-2015-0001
issn: 1756-8919
e-issn: 1756-8927
Aparece en las colecciones: (IQM) Artículos
(IBMCP) Artículos
Ficheros en este ítem:
Fichero Descripción Tamaño Formato  
Future Med Chem_Gonzalez-Muñiz R1F-1 (2).pdf1,03 MBAdobe PDFVista previa
Visualizar/Abrir
Mostrar el registro completo
 

Artículos relacionados:


NOTA: Los ítems de Digital.CSIC están protegidos por copyright, con todos los derechos reservados, a menos que se indique lo contrario.