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Titolo:
INFLUENCE OF ENDOTHELIN ETA AND ETB RECEPTOR ANTAGONISTS ON ENDOTHELIN-INDUCED CONTRACTIONS OF THE GUINEA-PIG ISOLATED GALL-BLADDER
Autore:
CARDOZO AM; DORLEANSJUSTE P; YANO M; FRANK PA; RAE GA;
Indirizzi:
UNIV FED SANTA CATARINA,DEPT PHARMACOL,CCB,RUA FERREIRA LIMA 82 BR-88015420 FLORIANOPOLIS SC BRAZIL UNIV FED SANTA CATARINA,DEPT PHARMACOL,CCB BR-88015420 FLORIANOPOLIS SC BRAZIL UNIV SHERBROOKE,FAC MED SHERBROOKE PQ J1H 5N4 CANADA BANYU PHARMACEUT CO LTD,TSUKUBA RES INST TSUKUBA IBARAKI 30033 JAPAN
Titolo Testata:
Regulatory peptides
fascicolo: 1, volume: 69, anno: 1997,
pagine: 15 - 23
SICI:
0167-0115(1997)69:1<15:IOEEAE>2.0.ZU;2-Q
Fonte:
ISI
Lingua:
ENG
Soggetto:
SMOOTH-MUSCLE CONTRACTION; NITRIC-OXIDE; A RECEPTOR; POTENT; SELECTIVITY; ET(B); IDENTIFICATION; CLONING; SUBTYPE; AGONIST;
Keywords:
SARAFOTOXIN; BQ-123; BQ-788; IRL 1620; RES-701-1; BOSENTAN; SMOOTH MUSCLE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
42
Recensione:
Indirizzi per estratti:
Citazione:
A.M. Cardozo et al., "INFLUENCE OF ENDOTHELIN ETA AND ETB RECEPTOR ANTAGONISTS ON ENDOTHELIN-INDUCED CONTRACTIONS OF THE GUINEA-PIG ISOLATED GALL-BLADDER", Regulatory peptides, 69(1), 1997, pp. 15-23

Abstract

The receptors mediating guinea pig gall bladder (GPGB) contractions induced by endothelin-l (ET-I) and related peptides were characterized using various ET receptor antagonists. As all ET-receptor agonists used, except sarafotoxin S6c (SRTX), failed to induce a clear-cut maximalresponse at the highest concentration tested (i.e. 100 nM), their potencies are expressed in terms of a CK50 (i.e. the concentration causing 50% of the response to 80 mM KCl). ET-1 (CK50 0.8 mM) was equipotentto ET-2 and SRTX (selective ETB receptor agonist), but more potent than ET-3 (5-fold) or IRL 1620 (selective ETA receptor agonist). BQ-123 (0.3 mu M, peptidic ETB receptor antagonist) did not alter responses to ET-1, ET-3 or SRTX. BQ-788 (1 mu M, peptidic ETB receptor antagonist) reduced the potency of ET-3 (9-fold at the CK50, level) and SRTX ( >20-fold), but not ET-1. SRTX responses were unaffected by RES-701-1 (3 mu M, peptidic ET, receptor antagonist). The combination BQ-123 (0.3mu M) plus BQ-788 (1 mu M) did not modify responses to ET-1, inhibited SRTX responses similarly to BQ-788 alone and abolished ET-3 responses. Bosentan (1 mu M, non-peptidic ETA/ETB receptor antagonist) reducedthe potency of ET-1 (9-fold), ET-3 (9-fold) and SRTX (4-fold). In rataorta, the antagonists blocked ET-1-induced contractions (BQ-123 and bosentan) or SRTX-induced endothelium-dependent relaxations (BQ-788, RES-701-1 and bosentan). Thus, the GPGB expresses both ETA and ETB receptors. As BQ-123 only blocked responses to ET-3 in the presence of BQ-788, there appears to be cross-talk between both receptor types. Also,the binding sites of ET-1 and ET-3 on the ETA receptor may not coincide entirely, as BQ-123, even in presence of BQ-788, did not affect ET-1-induced contractions. Copyright (C) 1997 Elsevier Science B.V.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 15/07/20 alle ore 07:19:11