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Titolo:
Cannabinoid activation of recombinant and endogenous vanilloid receptors
Autore:
Ralevic, V; Kendall, DA; Jerman, JC; Middlemiss, DN; Smart, D;
Indirizzi:
Univ Nottingham, Sch Med, Queens Med Ctr, Sch Biomed Sci, Nottingham NG7 2UH, England Univ Nottingham Nottingham England NG7 2UH , Nottingham NG7 2UH, England GlaxoSmithKline, Neurosci Res, Harlow CM19 5AW, Essex, England GlaxoSmithKline Harlow Essex England CM19 5AW ow CM19 5AW, Essex, England
Titolo Testata:
EUROPEAN JOURNAL OF PHARMACOLOGY
fascicolo: 3, volume: 424, anno: 2001,
pagine: 211 - 219
SICI:
0014-2999(20010727)424:3<211:CAORAE>2.0.ZU;2-5
Fonte:
ISI
Lingua:
ENG
Soggetto:
MESENTERIC ARTERIAL BED; SENSORY NERVES MEDIATE; ANANDAMIDE TRANSPORT; EFFERENT FUNCTION; SPINAL-CORD; CAPSAICIN; ANTAGONIST; OLVANIL; VASODILATION; INHIBITION;
Keywords:
anandamide; cannabinoid; capsaicin; mesenteric arterial bed; sensory nerve; vanilloid receptor;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
29
Recensione:
Indirizzi per estratti:
Indirizzo: Ralevic, V Univ Nottingham, Sch Med, Queens Med Ctr, Sch Biomed Sci, Nottingham NG7 2UH, England Univ Nottingham Nottingham England NG7 2UH m NG7 2UH, England
Citazione:
V. Ralevic et al., "Cannabinoid activation of recombinant and endogenous vanilloid receptors", EUR J PHARM, 424(3), 2001, pp. 211-219

Abstract

The effects of three structurally related cannabinoids on human and rat recombinant vanilloid VR1 receptors expressed in human embryonic kidney (HEK293) cells and at endogenous vanilloid receptors in the rat isolated mesenteric arterial bed were studied. In the recombinant cells, all three were full agonists, causing concentration-dependent increases in [Ca2+](i) (FLIPR(TM)), with a rank order of potency relative to the vanilloids capsaicin and olvanii, of olvanil greater than or equal to capsaicin > AM404 ((allZ)-N-(4-hydroxyphenyl)-5,8,11,14-eicosatetraenamide) > anandamide > methanandamide. These responses were inhibited by the vanilloid VR1 receptor antagonist, capsazepine. In the mesenteric arterial bed, vasorelaxation was evoked by these ligands with a similar order of potency. The AM404-induced vasorelaxation was virtually abolished by capsaicin pretreatment. AM404 inhibition of capsaicin-sensitive sensory neurotransmission was blocked by ruthenium red,but not by cannabinoid CB1 and CB2 receptor antagonists. AM404 had no effect on relaxations to calcitonin gene-related peptide. These data demonstrate that the vasorelaxant and sensory neuromodulator properties of AM404 in the rat isolated mesenteric arterial bed are mediated by vanilloid VR1 receptors. (C) 2001 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 20/09/20 alle ore 04:21:02