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

Type
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 AA., 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)
    (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
  • De Petrocellis L., Orlando P., Schiano Moriello A., Aviello G., Stott C., Izzo AA., Di Marzo V. (literal)
Pagina inizio
  • 255 (literal)
Pagina fine
  • 266 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#altreInformazioni
  • ACTA PHYSIOLOGICA, vol. 204, p. 255-266, ISSN: 1748-1708, doi: 10.1111/j.1748-1716.2011.02338.x. (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#volumeInCollana
  • 204 (literal)
Rivista
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni
  • ICIB-CNR (literal)
Titolo
  • Cannabinoid actions at TRPV channels: effects on TRPV3 and TRPV4 and their potential relevance to gastrointestinal inflammation (literal)
Abstract
  • 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+) 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+) 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+) 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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