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Titolo:
Anandamide transport inhibition by the varmilloid agonist olvanil
Autore:
Beltramo, M; Piomelli, D;
Indirizzi:
Inst Neurosci, San Diego, CA 92121 USA Inst Neurosci San Diego CA USA 92121 st Neurosci, San Diego, CA 92121 USA
Titolo Testata:
EUROPEAN JOURNAL OF PHARMACOLOGY
fascicolo: 1, volume: 364, anno: 1999,
pagine: 75 - 78
SICI:
0014-2999(19990101)364:1<75:ATIBTV>2.0.ZU;2-8
Fonte:
ISI
Lingua:
ENG
Soggetto:
CANNABINOID RECEPTOR; RAT-BRAIN; CAPSAICIN; NE-19550; NEURONS; ENZYME;
Keywords:
cannabinoid; anandamide; transport; olvanil; capsaicin; analgesia;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
21
Recensione:
Indirizzi per estratti:
Indirizzo: Piomelli, D Univ Calif Irvine, Dept Pharmacol, 360 Med Surge 2, Irvine, CA92697 USA Univ Calif Irvine 360 Med Surge 2 Irvine CA USA 92697 2697 USA
Citazione:
M. Beltramo e D. Piomelli, "Anandamide transport inhibition by the varmilloid agonist olvanil", EUR J PHARM, 364(1), 1999, pp. 75-78

Abstract

The structural similarities between the anandamide transport inhibitor N-(4-hydroxyphenyl)-arachidonylamide (AM404) and the synthetic vanilloid agonist olvanil [(N-vanillyl)-9-oleamide], prompted us to investigate the possibility that olvanil may interfere with anandamide transport. The intracellular accumulation of [H-3]anandamide by human astrocytoma cells was preventedby olvanil with a K-i value of 14.1 +/- 7.1 mu M. By contrast, capsaicin [(8-methyl-N-vanillyl)-6-noneamide], a plant-derived vanilloid agonist, and capsazepine (N-[2-(4-chlorophenyl)ethyl]-1,3,4,5-tetrahydro-7,8-dihydroxy-2H-2-benzazepine-2-carbothioamide), a vanilloid antagonist, had no such effect (K-i > 100 mu M). These results indicate that, although less potent thanAM404 (K-i 2.1 +/- 0.2 mu M), olvanil may reduce anandamide clearance at concentrations similar to those needed for vanilloid receptor activation. (C) 1999 Elsevier Science B.V. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 05/12/20 alle ore 14:09:55