English   español  
Please use this identifier to cite or link to this item: http://hdl.handle.net/10261/90619
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 | DATACITE
Exportar a otros formatos:


Cannabinoid agonists showing BuChE inhibition as potential therapeutic agents for Alzheimer's disease

AuthorsGonzález-Naranjo, Pedro ; Pérez-Macias, N.; Campillo, Nuria E. ; Pérez, C.; Arán, Vicente J. ; Girón, Rocío; Sánchez-Robles, E.; Martín, M. Isabel ; Gómez-Cañas, María; García-Arencibia, M.; Fernández-Ruiz, Javier; Páez, Juan A.
Issue Date2014
CitationEuropean Journal of Medicinal Chemistry 73: 56- 72 (2014)
AbstractDesigning drugs with a specific multi-target profile is a promising approach against multifactorial illnesses as Alzheimer's disease. In this work, new indazole ethers that possess dual activity as both cannabinoid agonists CB2 and inhibitors of BuChE have been designed by computational methods. On the basis of this knowledge, the synthesis, pharmacological evaluation and docking studies of a new class of indazoles has been performed. Pharmacological evaluation includes radioligand binding assays with [3H]-CP55940 for CB1R and CB2R and functional activity for cannabinoid receptors on isolated tissue. Additionally, in vitro inhibitory assays of AChE/BuChE and the corresponding competition studies have been carried out. The results of pharmacological tests have revealed that three of these derivatives behave as CB2 cannabinoid agonists and simultaneously show BuChE inhibition. In particular, compounds 3 and 24 have emerged as promising candidates as novel cannabinoids that inhibit BuChE by a non-competitive or mixed mechanism, respectively. On the other hand, both molecules show antioxidant properties. © 2013 Elsevier Masson SAS. All rights reserved.
Identifiersdoi: 10.1016/j.ejmech.2013.11.026
issn: 0223-5234
e-issn: 1768-3254
Appears in Collections:(IQM) Artículos
Files in This Item:
File Description SizeFormat 
accesoRestringido.pdf15,38 kBAdobe PDFThumbnail
Show full item record
Review this work

WARNING: Items in Digital.CSIC are protected by copyright, with all rights reserved, unless otherwise indicated.