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dc.contributor.authorPérez-Faginas, Paulaes_ES
dc.contributor.authorAranda, M. Teresaes_ES
dc.contributor.authorTorre-Martínez, Roberto de laes_ES
dc.contributor.authorQuirce, Susanaes_ES
dc.contributor.authorFernández-Carvajal, Asiaes_ES
dc.contributor.authorFerrer-Montiel, Antonioes_ES
dc.contributor.authorGonzález-Muñiz, Rosarioes_ES
dc.date.accessioned2016-12-16T11:47:24Z-
dc.date.available2016-12-16T11:47:24Z-
dc.date.issued2016-01-14-
dc.identifier.citationRSC Advances 6 : 6868-6877 (2016)es_ES
dc.identifier.issn2046-2069-
dc.identifier.urihttp://hdl.handle.net/10261/141530-
dc.descriptionElectronic supplementary information (ESI) available: Protocol for the evaluation of compound 4b in the CFA-induced paw inflammation model and obtained results. See DOI: 10.1039/c5ra25709ces_ES
dc.description.abstractA high throughput screening campaign identified nine b,g-diamino ester derivatives as TRP modulators. A discrete library of new derivatives (23 components) was prepared in a one-pot two step reductive amination reaction, and evaluated for their ability to block the agonist-induced calcium influx in cells expressing human TRPV1, TRPM8 and TRPA1 channels. Selective antagonists for each channel, as well as dual TRPV1/TRPM8 and TRPM8/TRPA1 ligands, were obtained after subtle modification of this linear scaffold. SAR studies revealed the preferred substituents for the selective blockade of the three TRP channels under study. The most potent TRPV1 antagonists displayed submicromolar IC50 valueses_ES
dc.description.sponsorshipThis work was supported by the Spanish MINECO: CSD2008- 00005, The Spanish Ion Channel Initiative-CONSOLIDER INGENIO 2010, and BFU2012-39092-C02.es_ES
dc.language.isoenges_ES
dc.publisherRoyal Society of Chemistryes_ES
dc.relation.isversionofPostprintes_ES
dc.rightsclosedAccessen_EN
dc.titleNew transient receptor potential TRPV1, TRPM8 and TRPA1 channel antagonists from a single linear β,γ-diamino ester scaffoldes_ES
dc.typeartículoes_ES
dc.identifier.doi10.1039/c5ra25709c-
dc.description.peerreviewedPeer reviewedes_ES
dc.relation.publisherversionhttp://dx.doi.org/10.1039/c5ra25709ces_ES
dc.embargo.terms2017-01-30es_ES
dc.contributor.funderMinisterio de Economía y Competitividad (España)es_ES
dc.relation.csices_ES
oprm.item.hasRevisionno ko 0 false*
dc.identifier.funderhttp://dx.doi.org/10.13039/501100003329es_ES
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