Phoneutria toxin PnTx3-5 inhibits TRPV1 channel with antinociceptive action in an orofacial pain model.

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MetadadosDescriçãoIdioma
Autor(es): dc.creatorPereira, Elizete Maria Rita-
Autor(es): dc.creatorSouza, Jéssica Mabelle-
Autor(es): dc.creatorCarobin, Natália Virtude-
Autor(es): dc.creatorSilva, Juliana Figueira da-
Autor(es): dc.creatorAstoni, Duana Carvalho dos Santos-
Autor(es): dc.creatorSilva Júnior, Cláudio Antônio da-
Autor(es): dc.creatorBinda, Nancy Scardua-
Autor(es): dc.creatorBorges, Marcia Helena-
Autor(es): dc.creatorNagem, Ronaldo Alves Pinto-
Autor(es): dc.creatorKushmerick, Christopher-
Autor(es): dc.creatorFerreira, Juliano-
Autor(es): dc.creatorCastro Junior, Célio José de-
Autor(es): dc.creatorRibeiro, Fabiola Mara-
Autor(es): dc.creatorGomez, Marcus Vinicius-
Data de aceite: dc.date.accessioned2025-08-21T15:12:13Z-
Data de disponibilização: dc.date.available2025-08-21T15:12:13Z-
Data de envio: dc.date.issued2020-05-22-
Data de envio: dc.date.issued2020-05-22-
Data de envio: dc.date.issued2019-
Fonte completa do material: dc.identifierhttp://www.repositorio.ufop.br/handle/123456789/12245-
Fonte completa do material: dc.identifierhttps://www.sciencedirect.com/science/article/pii/S0028390819303922?via%3Dihub-
Fonte completa do material: dc.identifierhttps://doi.org/10.1016/j.neuropharm.2019.107826-
Fonte: dc.identifier.urihttp://educapes.capes.gov.br/handle/capes/1005655-
Descrição: dc.descriptionCapsaicin, an agonist of TRPV1, evokes intracellular [Ca2+] transients and glutamate release from perfused trigeminal ganglion. The spider toxin PnTx3-5, native or recombinant is more potent than the selective TRPV1 blocker SB-366791 with IC50 of 47 ± 0.18 nM, 45 ± 1.18 nM and 390 ± 5.1 nM in the same experimental conditions. PnTx3-5 is thus more potent than the selective TRPV1 blocker SB-366791. PnTx3-5 (40 nM) and SB-366791 (3 μM) also inhibited the capsaicin-induced increase in intracellular Ca2+ in HEK293 cells transfected with TRPV1 by 75 ± 16% and 84 ± 3.2%, respectively. In HEK293 cells transfected with TRPA1, cinnamaldehyde (30 μM) generated an increase in intracellular Ca2+ that was blocked by the TRPA1 antagonist HC-030031 (10 μM, 89% inhibition), but not by PnTx3-5 (40 nM), indicating selectivity of the toxin for TRPV1. In whole-cell patch-clamp experiments on HEK293 cells transfected with TRPV1, capsaicin (10 μM) generated inward currents that were blocked by SB-366791 and by both native and recombinant PnTx3-5 by 47 ± 1.4%; 54 ± 7.8% and 56 ± 9.0%, respectively. Intradermal injection of capsaicin into the rat left vibrissa induced nociceptive behavior that was blocked by pre-injection with either SB-366791 (3 nmol/site i.d., 83.3 ± 7.2% inhibition) or PnTx3-5 (100 fmol/site, 89 ± 8.4% inhibition). We conclude that both native and recombinant PnTx3-5 are potent TRPV1 receptor antagonists with antinociceptive action on pain behavior evoked by capsaicin.-
Formato: dc.formatapplication/pdf-
Idioma: dc.languageen-
Direitos: dc.rightsrestrito-
Palavras-chave: dc.subjectCapsaicin-
Palavras-chave: dc.subjectInhibition-
Título: dc.titlePhoneutria toxin PnTx3-5 inhibits TRPV1 channel with antinociceptive action in an orofacial pain model.-
Aparece nas coleções:Repositório Institucional - UFOP

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