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Titolo:
DELINEATION OF ENDOTHELIN RECEPTOR SUBTYPES IN RAT AND RABBIT AORTAS
Autore:
SHETTY SS; DELGRANDE D; SAVAGE P; KSANDER GM; JENG AY;
Indirizzi:
CIBA GEIGY PHARMACEUT CORP,DIV PHARMACEUT,RES DEPT,556 MORRIS AVE,LSB2215 SUMMIT NJ 07901
Titolo Testata:
Journal of cardiovascular pharmacology
, volume: 26, anno: 1995, supplemento:, 3
pagine: 310 - 313
SICI:
0160-2446(1995)26:<310:DOERSI>2.0.ZU;2-B
Fonte:
ISI
Lingua:
ENG
Soggetto:
SMOOTH-MUSCLE; ETA-RECEPTOR; ANTAGONIST; CLONING;
Keywords:
ENDOTHELIN RECEPTOR ANTAGONIST; ENDOTHELIN RECEPTOR SUBTYPES; IRL 2500; SB 209670; PD 156707; BQ 788; SARAFOTOXIN S6C;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
18
Recensione:
Indirizzi per estratti:
Citazione:
S.S. Shetty et al., "DELINEATION OF ENDOTHELIN RECEPTOR SUBTYPES IN RAT AND RABBIT AORTAS", Journal of cardiovascular pharmacology, 26, 1995, pp. 310-313

Abstract

The receptor subtypes mediating tension responses to endothelin-1 (ET-1) in isolated rat and rabbit aortic preparations were examined with various ET receptor antagonists. In the presence of 3 mu M IRL 2500 (an ET(B)-selective antagonist), SB 209670 (an ET(A)/ET(B) antagonist) induced monophasic inhibitions of the ET-1 dose-response curves of bothrat (pK(B) 9.1) and rabbit aortas (pK(B) 8.9). In the presence of IRL2500, PD 156707 (an ET(A) antagonist) also caused a similar monophasic inhibition of the agonist-induced dose-response curve of the rat aorta (pK(B) 7.7) but produced a biphasic inhibition of the curve obtained with the rabbit aorta. PD 156707, however, produced monophasic inhibitions of the ET-1-induced dose-response curve of rabbit aortas pretreated either with BQ 788 (an ET(B)-selective antagonist) or desensitized with sarafotoxin S6c (an ET(B)-selective agonist). The receptor subtypes mediating the contractile responses to ET-1 were further characterized by examining the effects of the antagonists on the binding of [(125)]ET-1 to these two tissues. In the presence of 1 nM IRL 2500, SB 209670 displaced [I-125]ET-1 binding in both rat and rabbit aortic membrane preparations in a monophasic manner, with similar potencies (IC501.2-1.6 nM). Similar results were also obtained with PD 156707 in rataortic membrane (IC50 0.27 nM). In contrast, the data obtained with PD 156707 using rabbit aortic membrane were best-fitted with a two-sitemodel (site 1, IC50 0.21 nM, 67% of B-max; site 2, 100 nM and 33%, respectively). Therefore, the-constrictor response to ET-1 in the rat aorta is mediated exclusively by the ET(A) receptor, whereas that in therabbit aorta is additionally mediated by an ET(B) receptor subtype that is sensitive to SB 209670 and BQ 788 but insensitive to IRL 2500.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 21/09/20 alle ore 12:47:46