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dc.contributor.authorVidal-Mosquera, Miquel-
dc.contributor.authorFernández-Carvajal, Asia-
dc.contributor.authorMoure, Alejandra-
dc.contributor.authorValente, Pierluigi-
dc.contributor.authorPlanells-Cases, Rosa-
dc.contributor.authorGonzález-Ros, José M.-
dc.contributor.authorBujons, Jordi-
dc.contributor.authorFerrer-Montiel, Antonio-
dc.contributor.authorMesseguer Peypoch, Ángel-
dc.date.accessioned2012-04-12T08:52:12Z-
dc.date.available2012-04-12T08:52:12Z-
dc.date.issued2011-
dc.identifier.citationJournal of Medicinal Chemistryes_ES
dc.identifier.issn0022-2623-
dc.identifier.urihttp://hdl.handle.net/10261/48156-
dc.description.abstractThe thermosensory transient receptor potential vanilloid 1 channel (TRPV1) is a polymodal receptor activated by physical and chemical stimuli. TRPV1 activity is drastically potentiated by proinflammatory agents released upon tissue damage. Given the pivotal role of TRPV1 in human pain, there is pressing need for improved TRPV1 antagonists, the development of which will require identification of new pharmacophore scaffolds. Uncompetitive antagonists acting as open-channel blockers might serve as activity-dependent blockers that preferentially modulate the activity of overactive channels, thus displaying fewer side effects than their competitive counterparts. Herein we report the design, synthesis, biological evaluation, and SAR analysis of a family of triazine-based compounds acting as TRPV1 uncompetitive antagonists. We identified the triazine 8aA as a potent, pure antagonist that inhibits TRPV1 channel activity with nanomolar efficacy and strong voltage dependency. It represents a new class of activity-dependent TRPV1 antagonists and may serve as the basis for lead optimization in the development of new analgesics.es_ES
dc.description.sponsorshipThis work was supported by grants from Spanish Ministry of Science and Innovation (Grant SAF2008-00048 to A.M., Grant BFU2009-08346 to A.F.-M., CONSOLIDER-INGENIO 2010 (Grant CSD2008-00005) to A.F.-M., J.M.G.-R., and A.M.), from Fundació La Marató de TV3 (to A.F.-M. and A.M.), and from PROMETEO/2010/046 from the GVA to A.F.-M.-
dc.language.isoenges_ES
dc.publisherAmerican Chemical Societyes_ES
dc.rightsclosedAccesses_ES
dc.titleTriazine-Based Vanilloid 1 Receptor Open Channel Blockers: Design, Synthesis, Evaluation, and SAR Analysises_ES
dc.typeartículoes_ES
dc.identifier.doi10.1021/jm200981s-
dc.description.peerreviewedPeer reviewedes_ES
dc.relation.publisherversionhttp://dx.doi.org/10.1021/jm200981ses_ES
dc.identifier.e-issn1520-4804-
dc.type.coarhttp://purl.org/coar/resource_type/c_6501es_ES
item.openairetypeartículo-
item.cerifentitytypePublications-
item.languageiso639-1en-
item.grantfulltextnone-
item.openairecristypehttp://purl.org/coar/resource_type/c_18cf-
item.fulltextNo Fulltext-
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