Novel TRPV1 Channel Agonists With Faster and More Potent Analgesic Properties Than Capsaicin

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dc.contributor.authorDuarte, Y.
dc.contributor.authorCáceres, J.
dc.contributor.authorSepúlveda, R.V.
dc.contributor.authorArriagada, D.
dc.contributor.authorOlivares, P.
dc.contributor.authorDíaz-Franulic, I.
dc.contributor.authorStehberg, J.
dc.contributor.authorGonzález-Nilo, F.
dc.date.accessioned2021-10-19T14:32:21Z
dc.date.available2021-10-19T14:32:21Z
dc.date.issued2020-07
dc.descriptionIndexación: Scopus.es
dc.description.abstractThe transient receptor potential vanilloid 1 (TRPV1) ion channel is a member of the family of Transient Receptor Potential (TRP) channels that acts as a molecular detector of noxious signals in primary sensory neurons. Activated by capsaicin, heat, voltage and protons, it is also well known for its desensitization, which led to the medical use of topically applied TRPV1 agonist capsaicin for its long-lasting analgesic effects. Here we report three novel small molecules, which were identified using a Structure-Based Virtual Screening for TRPV1 from the ZINC database. The three compounds were tested using electrophysiological assays, which confirmed their capsaicin-like agonist activity. von Frey filaments were used to measure the analgesic effects of the compounds applied topically on tactile allodynia induced by intra-plantar carrageenan. All compounds had anti-nociceptive activity, but two of them showed faster and longer lasting analgesic effects than capsaicin. The present results suggest that TRPV1 agonists different from capsaicin could be used to develop topical analgesics with faster onset and more potent effects. © Copyright © 2020 Duarte, Cáceres, Sepúlveda, Arriagada, Olivares, Díaz-Franulic, Stehberg and González-Nilo.es
dc.description.urihttps://www.frontiersin.org/articles/10.3389/fphar.2020.01040/full
dc.identifier.citationFrontiers in Pharmacology Open Access Volume 1114 July 2020 Article number 1040es
dc.identifier.doi10.3389/fphar.2020.01040
dc.identifier.issn1663-9812
dc.identifier.urihttp://repositorio.unab.cl/xmlui/handle/ria/20519
dc.language.isoenes
dc.publisherFrontiers Media S.Aes
dc.rights.licenseAttribution 4.0 International (CC BY 4.0)
dc.rights.urihttps://creativecommons.org/licenses/by/4.0/
dc.subjectallodyniaes
dc.subjectanalgesices
dc.subjectcapsaicines
dc.subjectcarrageenanes
dc.subjectdrug discoveryes
dc.subjecttransient receptor potential vanilloid 1 channelses
dc.titleNovel TRPV1 Channel Agonists With Faster and More Potent Analgesic Properties Than Capsaicines
dc.typeArtículoes
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