Hypolocomotor effects in rats of capsaicin and two long chain capsaicin homologues (Articolo in rivista)

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Label
  • Hypolocomotor effects in rats of capsaicin and two long chain capsaicin homologues (Articolo in rivista) (literal)
Anno
  • 2001-01-01T00:00:00+01:00 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi
  • 10.1016/S0014-2999(01)01012-3 (literal)
Alternative label
  • Di Marzo V., Lastres-Becker I., Bisogno T., De Petrocellis L., Milone A., Davis J.B. and Fernandez-Ruiz J.J. (2001)
    Hypolocomotor effects in rats of capsaicin and two long chain capsaicin homologues
    in European journal of pharmacology; ELSEVIER SCIENCE BV, PO BOX 211, 1000 AE AMSTERDAM, NETHERLANDS, AMSTERDAM (Paesi Bassi)
    (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
  • Di Marzo V., Lastres-Becker I., Bisogno T., De Petrocellis L., Milone A., Davis J.B. and Fernandez-Ruiz J.J. (literal)
Pagina inizio
  • 123 (literal)
Pagina fine
  • 131 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroVolume
  • 420 (literal)
Rivista
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroFascicolo
  • 2-3 (literal)
Note
  • ISI Web of Science (WOS) (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni
  • 1. CNR, Ist Chim Mol Interesse Biol, Endocannabinoid Res Grp, I-80072 Arco, Naples, Italy 2. CNR, Ist Cibernetica, Endocannabinoid Res Grp, I-80072 Arco, Naples, Italy 3. Univ Complutense, Fac Med, Dept Biochem & Mol Biol, E-28040 Madrid, Spain 4. GlaxoSmithKline, Neurobiol, Harlow CM19 5AW, Essex, England (literal)
Titolo
  • Hypolocomotor effects in rats of capsaicin and two long chain capsaicin homologues (literal)
Abstract
  • Capsaicin and its analogue N-arachidonoyl-vanillyl-amine (arvanil) are agonists of vanilloid VR, receptors. and suppress spontaneous activity in mice through an unknown mechanism. Here, we tested in rats the effect on motor behavior of: (1) capsaicin; (2) N-linoleoyl-vanillyl-amine (livanil) and N-alpha -linolenoyl-vanillyl-amine (linvanil), which, unlike arvanil, have very little affinity for cannabinoid CB1 receptors; and (3) the endocannabinoid anandamide ( N-arachidonoyl-ethanolamine), which is a full agonist at both cannabinoid CB1 and vanilloid VR, receptors. All compounds, administered i.p., dose-dependently (0.1-10 mg/kg) inhibited ambulation and stereotypic behavior and increased inactivity in the open field test. The rank of potency observed in vivo (livanil > capsaicin > linvanil > anandamide) bore little resemblance with the relative potencies in a functional assay for rat vanilloid VR1 receptors (livanil = linvanil > capsaicin > anandamide) and even less with the relative affinities in rat CB, receptor binding assays (anandamide > livanil > linvanil > capsaicin). The vanilloid VR1 receptor antagonist capsazepine (10 mg/kg, i.p.) blocked the effect of capsaicin but not of livanil or anandamide, whereas the CB1 receptor antagonist (N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1 H-pyrazole-3-carboxamide. HCl (SR141716A, 3 mg/kg, i.p.) antagonized the actions of the CB1 receptor agonist Delta (9)-tetrahydrocannabinol, but not of livanil, anandamide or capsaicin. Anandamide occluded the effects of livanil on locomotion, possibly suggestive of a common mechanism of action for the two compounds. Finally, stimulation with capsaicin of cells expressing rat vanilloid VR1 receptors led to anandamide formation. These data suggest that motor behavior can be suppressed by the activation of: (1) vanilloid receptors, possibly via the intermediacy of anandamide; or (2) capsazepine- and SR141716A-insensitive sites of action for anandamide, livanil and linvanil, possibly the same that were previously suggested to mediate arvanil hypokinetic effects in mice. (literal)
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