@prefix prodottidellaricerca: . @prefix istituto: . @prefix prodotto: . istituto:CDS024 prodottidellaricerca:prodotto prodotto:ID19337 . @prefix pubblicazioni: . @prefix unitaDiPersonaleInterno: . unitaDiPersonaleInterno:MATRICOLA4773 pubblicazioni:autoreCNRDi prodotto:ID19337 . @prefix modulo: . modulo:ID7701 prodottidellaricerca:prodotto prodotto:ID19337 . @prefix rdf: . @prefix retescientifica: . prodotto:ID19337 rdf:type retescientifica:ProdottoDellaRicerca , prodotto:TIPO1101 . @prefix rdfs: . prodotto:ID19337 rdfs:label "N-palmitoyl-vanillamide (palvanil) is a non-pungent analogue of capsaicin with stronger desensitizing capability against the TRPV1 receptor and potential anti-hyperalgesic activity (Articolo in rivista)"@en . @prefix xsd: . prodotto:ID19337 pubblicazioni:anno "2011-01-01T00:00:00+01:00"^^xsd:gYear ; pubblicazioni:doi "10.1016/j.phrs.2010.12.019"^^xsd:string . @prefix skos: . prodotto:ID19337 skos:altLabel "
De Petrocellis L., Guida F., Schiano Moriello A., De Chiaro M., Piscitelli F., de Novellis V., Maione S., and Di Marzo V. (2011)
N-palmitoyl-vanillamide (palvanil) is a non-pungent analogue of capsaicin with stronger desensitizing capability against the TRPV1 receptor and potential anti-hyperalgesic activity
in Pharmacological research (Print)
"^^rdf:HTML ; pubblicazioni:autori "De Petrocellis L., Guida F., Schiano Moriello A., De Chiaro M., Piscitelli F., de Novellis V., Maione S., and Di Marzo V."^^xsd:string ; pubblicazioni:paginaInizio "294"^^xsd:string ; pubblicazioni:paginaFine "299"^^xsd:string ; pubblicazioni:numeroVolume "63"^^xsd:string . @prefix ns11: . prodotto:ID19337 pubblicazioni:rivista ns11:ID510772 ; pubblicazioni:note "Pharmacological Research 63 (2011) 294-299."^^xsd:string ; pubblicazioni:numeroFascicolo "4"^^xsd:string ; skos:note "ISI Web of Science (WOS)"^^xsd:string ; pubblicazioni:affiliazioni "ICIB-CNR"^^xsd:string ; pubblicazioni:titolo "N-palmitoyl-vanillamide (palvanil) is a non-pungent analogue of capsaicin with stronger desensitizing capability against the TRPV1 receptor and potential anti-hyperalgesic activity"^^xsd:string ; prodottidellaricerca:abstract "N-acyl-vanillamide (NAVAM) analogues of the natural pungent principle of \ncapsicum, capsaicin, were developed several years ago as potential non-pungent analgesic \ncompounds. N-oleoyl-vanillamide (olvanil) and N-arachidonoy-vanillamide (arvanil), in \nparticular, were described in several publications and patents to behave as potent \nanti-hyperalgesic compounds in experimental models of chronic and inflammatory pain, and \nto activate both \\\"capsaicin receptors\\\", i.e. the transient receptor potential of \nvanilloid type-1 (TRPV1) channel, and, either directly or indirectly, cannabinoid \nreceptors of type-1. Here we report the biochemical and pharmacological characterization \nof a so far neglected NAVAM, N-palmitoyl-vanillamide (palvanil), and propose its possible \nuse instead of capsaicin, as a possible topical analgesic. Palvanil exhibited a kinetics \nof activation of human recombinant TRPV1-mediated intracellular calcium elevation \nsignificantly slower than that of capsaicin (t(1/2) = 21 s and 8 s, respectively at 1 mu \nM). Slow kinetics of TRPV1 agonists were previously found to be associated with stronger \npotencies as TRPV1 desensitizing agents, which in turn are usually associated with lower \npungency and stronger anti-hyperalgesic activity. Accordingly, palvanil desensitized the \nhuman recombinant TRPV1 to the effect of capsaicin (10 nM) with significantly higher \npotency than capsaicin (IC(50) = 0.8 nM and 3.8 nM, respectively), this effect reaching \nits maximum more rapidly (50 and 250 min, respectively). Palvanil was also more potent \nthan capsaicin at desensitizing the stimulatory effect of TRPV1 by low pH together with \nanandamide, which mimics conditions occurring during inflammation. In the eye-wiping \nassay carried out in mice, palvanil was not pungent and instead caused a strong and \nlong-lasting inhibition of capsaicin-induced eye-wiping. Finally, intraplantar palvanil \ninhibited the second phase of the nociceptive response to formalin in mice. In \nconclusion, palvanil appears to be a non-pungent analogue of capsaicin with stronger \ndesensitizing effects on TRPV1 and hence potentially higher anti-hyperalgesic activity." ; prodottidellaricerca:prodottoDi istituto:CDS024 , modulo:ID7701 ; pubblicazioni:autoreCNR unitaDiPersonaleInterno:MATRICOLA4773 . ns11:ID510772 pubblicazioni:rivistaDi prodotto:ID19337 .