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Titolo:
DISTRIBUTION OF ENDOTHELIN-1-RECEPTOR SUBTYPES IN RAT PORTAL-VEIN
Autore:
FILIPPELLI A; FALCIANI M; PALLA A; DAMICO M; VACCA C; ROSSI F;
Indirizzi:
VIA BROGGIA 3 I-80138 NAPLES ITALY UNIV NAPLES FEDERICO II,FAC MED & SURG,INST PHARMACOL & TOXICOL NAPLES ITALY
Titolo Testata:
Journal of cardiovascular pharmacology
fascicolo: 1, volume: 27, anno: 1996,
pagine: 113 - 118
SICI:
0160-2446(1996)27:1<113:DOESIR>2.0.ZU;2-3
Fonte:
ISI
Lingua:
ENG
Soggetto:
ENDOTHELIN RECEPTOR; VASOCONSTRICTOR PEPTIDE; HIGHLY POTENT; ANTAGONIST; CLONING; MUSCLE; ETA; RESPONSES; ARTERIES; CELLS;
Keywords:
ENDOTHELIN-1; SARAFOTOXIN-S6C; RAT; PORTAL VEIN STRIP; PORTAL VEIN RING; ETA RECEPTOR ANTAGONIST; BQ-123; ET(A)-ET(B) RECEPTOR ANTAGONIST PD-145065; ET(B) RECEPTOR ANTAGONIST IRL-1038; PHARMACOLOGY IN VITRO;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
29
Recensione:
Indirizzi per estratti:
Citazione:
A. Filippelli et al., "DISTRIBUTION OF ENDOTHELIN-1-RECEPTOR SUBTYPES IN RAT PORTAL-VEIN", Journal of cardiovascular pharmacology, 27(1), 1996, pp. 113-118

Abstract

Endothelin-1 (ET-1), a potent vasoactive peptide, was first isolated from cultured porcine endothelial cells. Subsequent studies revealed the existence of two additional related peptides, ET-2 and ET-3, and atleast two distinct ET-receptor subtypes, ET(A) (selective for ET-1) and ET(B) (nonselective for ET isopeptides). These isopeptides and receptors are widely distributed in many tissues and are involved in numerous biological responses. The aim of this study was to identify the eventual distribution of the two distinct endothelin-receptor subtypes in isolated endothelium-denuded rat portal vein rings (PVRs) and strips(PVSs). BQ-123 (0.6, 1, and 6 mu M) and PD-145065 (0.06, 0.1, 0.6, and 6 mu M) were used to differentiate the subtypes because they are selective antagonists for ET(A) and nonselective antagonists for ET(A)-ET(B) receptors, respectively. To characterize the ET receptors further,sarafotoxin-S6c (a selective ET(B)-receptor agonist) and IRL-1038 (a selective ET(B)-receptor antagonist) were used. In PVRs, cumulative additions of ET-1 (0.1-100 nM) caused graded and slow contractions and potentiated spontaneous rhythmic contractions. The EC(50) values and maximal response to 100 nM of ET-1 were 2.72 nM and 0.75 g, respectively(n = 7). PVSs showed ET-1 EC(50) values very similar to those of PVRs, but E(max) values to 100 nM of ET-1 were significantly lower (E(max)= 0.33 g; n = 7). Moreover, ET-1 clearly increased the amplitude and frequency of spontaneous contractions in both types of specimens, although these were greater in the PVSs. Thirty-minute incubation with theselective ET(A)-receptor antagonist BQ-123 blunted ET-1-induced effects in PVS specimens but only weakly antagonized ET-1-induced contractions in PVRs. In contrast, the nonselective ET(A)-ET(B)-receptor antagonist PD-145065 significantly shifted the ET-1 concentration-response curve to the right in PVRs and partially inhibited ET-1 effects in PVSs. Moreover, sarafotoxin-S6c (0.1-100 nM) contracted PVRs and PVSs in asimilar manner to ET-1; its effects were antagonized by IRL-1038 onlyat the PVR level. The differences observed in PVR and PVS specimens in response to agonists and antagonists of ET confirmed the great heterogeneity of endothelin-sarafotoxin receptors. In our experimental models, functionally ET(B)-like (or non-ET(A)) receptors seem mostly to mediate vasoconstriction.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 22/09/20 alle ore 19:59:45