http://www.cnr.it/ontology/cnr/individuo/prodotto/ID169572
Capsaicin-like effects of N-arachidonoyl-dopamine in the isolated guinea pig bronchi and urinary bladder. (Articolo in rivista)
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- Capsaicin-like effects of N-arachidonoyl-dopamine in the isolated guinea pig bronchi and urinary bladder. (Articolo in rivista) (literal)
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- 2003-01-01T00:00:00+01:00 (literal)
- Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi
- 10.1016/S0014-2999(03)02114-9 (literal)
- Alternative label
Harrison S., De Petrocellis L., Trevisani M., Benvenuti F., Bifulco M., Geppetti P., Di Marzo V. (2003)
Capsaicin-like effects of N-arachidonoyl-dopamine in the isolated guinea pig bronchi and urinary bladder.
in European journal of pharmacology; ELSEVIER SCIENCE BV, PO BOX 211, 1000 AE AMSTERDAM, NETHERLANDS, AMSTERDAM (Paesi Bassi)
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- Harrison S., De Petrocellis L., Trevisani M., Benvenuti F., Bifulco M., Geppetti P., Di Marzo V. (literal)
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- IF 2002: 2,34. Settore disciplinare Farmacologia (categorie ISI-CRUI). IF ricalcolato in base al rango: 0,729. ImmediacyIndex 0,23, Cit Half-Life 6,9. (literal)
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- 1. Univ Ferrara, Dipartimento Med Sperimentale & Clin, Ferrara, Italy
2. CNR, Ist Cibernetica, Endocannoabinoid Res Grp, I-80078 Pozzuoli, NA, Italy
3. Univ Salerno, Dipartimento Sci Farmaceut, Endocannabinoid Res Grp, Fisciano, SA, Italy
4. Dipartimento Area Critica Medico Chirurg, Florence, Italy
5. CNR, Ist Chim Biomol, Endocannabinoid Res Grp, I-80078 Pozzuoli, NA, Italy (literal)
- Titolo
- Capsaicin-like effects of N-arachidonoyl-dopamine in the isolated guinea pig bronchi and urinary bladder. (literal)
- Abstract
- A capsaicin-like endogenous ligand of vanilloid (VR1) receptors, N-arachidonoyl-dopamine, was recently identified in bovine and rat nervous tissue, and found to be almost as potent as capsaicin, and 5-10-fold more potent than anandamide, on these receptors, both in isolated cells and in vivo. Here we have investigated if N-arachidonoyl-dopamine also exerts other capsaicin-like effects at VR1 receptors in some isolated organ preparations. N-arachidonoyl-dopamine exerted a potent contractile response of guinea pig isolated bronchi (EC50=12.6 +/- 1.7 microM, Emax=69.2 +/- 2.4% of carbachol Emax), which was blocked by pre-treatment with capsaicin or with the VR1 antagonist capsazepine, as well as by a combination of tachykinin NK1 and NK2 receptor antagonists. In this assay, N-arachidonoyl-dopamine was less and more potent and/or efficacious than capsaicin (EC50=40.0 nM; Emax=93.5%) and anandamide (EC50=15.2 microM, Emax=38.0%), respectively. Unlike capsaicin and anandamide, forskolin or ethanol did not enhance N-arachidonoyl-dopamine effect in this preparation, whereas epithelial denudation resulted in a 2.5-fold increase in potency without affecting the efficacy. N-arachidonoyl-dopamine also contracted the isolated guinea pig urinary bladder, although in this preparation, as well as in the isolated rat urinary bladder, the potency (EC50=3.7 +/- 0.3 and 19.9 +/- 0.1 microM) and/or efficacy (Emax=12.0 +/- 0.1% and 20.7 +/- 0.7% of carbachol Emax) of the compound were significantly lower than those of both capsaicin and anandamide. These data suggest that the extent to which exogenous N-arachidonoyl-dopamine activates VR1 receptor in isolated organs is largely dependent on pharmacodynamics and bioavailability. (literal)
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