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Title

Chalcones as positive allosteric modulators of α7 nicotinic acetylcholine receptors: A new target for a privileged structure

AuthorsBalsera, Beatriz; Mulet Soler, José; Fernández-Carvajal, Asia; Torre-Martínez, Roberto de la; Ferrer-Montiel, Antonio; Hernández-Jiménez, José G.; Estévez-Herrera, Judith; Borges, Ricardo; Freitas, Andiara E.; López, Manuela G.; García-López, M. Teresa ; González-Muñiz, Rosario ; Pérez de Vega, M. Jesús; Valor, Luis M.; Svobodová, Lucie; Sala, Salvador; Sala, Francisco; Criado, Manuel
Keywordsα7 Nicotinic receptor
Positive allosteric modulators
Chalcones
Neuroprotection
Analgesia
Issue Date2014
PublisherElsevier
CitationEuropean Journal of Medicinal Chemistry 86: 724-739 (2014)
AbstractThe α7 acetylcholine nicotine receptor is a ligand-gated ion channel that is involved in cognition disorders, schizophrenia, pain and inflammation among other diseases. Therefore, the development of new agents that target this receptor has great significance. Positive allosteric modulators might be advantageous, since they facilitate receptor responses without directly interacting with the agonist binding site. Here we report the search for and further design of new positive allosteric modulators having the relatively simple chalcone structure. From the natural product isoliquiritigenin as starting point, chalcones substituted with hydroxyl groups at defined locations were identified as optimal and specific promoters of α77 nicotinic function. The most potent compound (2,4,2-2,5-2-tetrahydroxychalcone, 111) was further characterized showing its potential as neuroprotective, analgesic and cognitive enhancer, opening the way for future developments around the chalcone structure.
URIhttp://hdl.handle.net/10261/115951
DOI10.1016/j.ejmech.2014.09.039
Identifiersdoi: 10.1016/j.ejmech.2014.09.039
issn: 0223-5234
e-issn: 1768-3254
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(IBMCP) Artículos
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