http://www.cnr.it/ontology/cnr/individuo/prodotto/ID169966

Cannabinoid actions at TRPV channels: effects on TRPV3 and TRPV4 and their potential relevance to gastrointestinal inflammation. (Articolo in rivista)

Type

Articolo in rivista (Classe)
Prodotto della ricerca (Classe)

Label

Cannabinoid actions at TRPV channels: effects on TRPV3 and TRPV4 and their potential relevance to gastrointestinal inflammation. (Articolo in rivista) (literal)

Anno

2012-01-01T00:00:00+01:00 (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi

10.1111/j.1748-1716.2011.02338.x (literal)

Alternative label

De Petrocellis L., Orlando P., Schiano Moriello A., Aviello G., Stott C., Izzo A., and Di Marzo V. (2012)
Cannabinoid actions at TRPV channels: effects on TRPV3 and TRPV4 and their potential relevance to gastrointestinal inflammation.
in Acta physiologica (Print); WILEY-BLACKWELL PUBLISHING, INC, MALDEN (Stati Uniti d'America)
(literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori

De Petrocellis L., Orlando P., Schiano Moriello A., Aviello G., Stott C., Izzo A., and Di Marzo V. (literal)

Pagina inizio

255 (literal)

Pagina fine

266 (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroVolume

204 (literal)

Rivista

Acta physiologica (Rivista)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#note

doi: 10.1111/j.1748-1716.2011.02338.x. Acta Physiol. (2011) (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroFascicolo

2 (literal)

Note

ubMe (literal)
Scopus (literal)
ISI Web of Science (WOS) (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni

CNR, Inst Biomol Chem, Endocannabinoid Res Grp, I-80078 Pozzuoli, NA, Italy Univ Naples Federico 2, Endocannabinoid Res Grp, Inst Prot Biochem, Naples, Italy Univ Naples Federico 2, Dept Expt Pharmacol, Endocannabinoid Res Grp, Naples, Italy CNR, Inst Cybernet, Endocannabinoid Res Grp, I-80078 Pozzuoli, NA, Ita GW Pharmaceut Ltd, Salisbury, Wilts, England (literal)

Titolo

Cannabinoid actions at TRPV channels: effects on TRPV3 and TRPV4 and their potential relevance to gastrointestinal inflammation. (literal)

Abstract

AIM: Plant cannabinoids, like ?(9)-tetrahydrocannabinol (THC) and cannabidiol (CBD), activate/desensitize thermosensitive transient receptor potential (TRP) channels of vanilloid type-1 or -2 (TRPV1 or TRPV2). We investigated whether cannabinoids also activate/desensitize two other 'thermo-TRP's', the TRP channels of vanilloid type-3 or -4 (TRPV3 or TRPV4), and if the TRPV-inactive cannabichromene (CBC) modifies the expression of TRPV1-4 channels in the gastrointestinal tract. METHODS: TRP activity was assessed by evaluating elevation of [Ca(2+)](i) in rat recombinant TRPV3- and TRPV4-expressing HEK-293 cells. TRP channel mRNA expression was measured by quantitative RT-PCR in the jejunum and ileum of mice treated with vehicle or the pro-inflammatory agent croton oil. RESULTS: (i) CBD and tetrahydrocannabivarin (THCV) stimulated TRPV3-mediated [Ca(2+)](i) with high efficacy (50-70% of the effect of ionomycin) and potency (EC(50~) 3.7 ?m), whereas cannabigerovarin (CBGV) and cannabigerolic acid (CBGA) were significantly more efficacious at desensitizing this channel to the action of carvacrol than at activating it; (ii) cannabidivarin and THCV stimulated TRPV4-mediated [Ca(2+)](i) with moderate-high efficacy (30-60% of the effect of ionomycin) and potency (EC(50) 0.9-6.4 ?m), whereas CBGA, CBGV, cannabinol and cannabigerol were significantly more efficacious at desensitizing this channel to the action of 4-?-phorbol 12,13-didecanoate (4?-PDD) than at activating it; (iii) CBC reduced TRPV1?, TRPV3 and TRPV4 mRNA in the jejunum, and TRPV3 and TRPV4 mRNA in the ileum of croton oil-treated mice. CONCLUSIONS: Cannabinoids can affect both the activity and the expression of TRPV1-4 channels, with various potential therapeutic applications, including in the gastrointestinal tract. (literal)

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