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Titolo:
CHARACTERIZATION OF A POTENT AND SELECTIVE ENDOTHELIN-B RECEPTOR ANTAGONIST, IRL-2500
Autore:
BALWIERCZAK JL; BRUSEO CW; DELGRANDE D; JENG AY; SAVAGE P; SHETTY SS;
Indirizzi:
CIBA GEIGY PHARMACEUT CORP,556 MORRIS AVE SUMMIT NJ 07940 CIBA GEIGY CORP,DEPT RES,DIV PHARMACEUT SUMMIT NJ 07901
Titolo Testata:
Journal of cardiovascular pharmacology
, volume: 26, anno: 1995, supplemento:, 3
pagine: 393 - 396
SICI:
0160-2446(1995)26:<393:COAPAS>2.0.ZU;2-K
Fonte:
ISI
Lingua:
ENG
Soggetto:
VASCULAR ENDOTHELIUM; ETA RECEPTOR;
Keywords:
CHO CELLS; IN VITRO STUDIES; DOG; RABBIT;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
13
Recensione:
Indirizzi per estratti:
Citazione:
J.L. Balwierczak et al., "CHARACTERIZATION OF A POTENT AND SELECTIVE ENDOTHELIN-B RECEPTOR ANTAGONIST, IRL-2500", Journal of cardiovascular pharmacology, 26, 1995, pp. 393-396

Abstract

IRL 2500 N-methyl-(D)-(4-phenylphenyl)-alanyl-L-tryptophan] inhibitedthe binding of [I-125]-endothelin-1 (ET-1) to human ET(B) (IC50 1.3 +/- 0.2 nM) and ET(A) (IC50 94 +/- 3 nM) receptors expressed in transfected Chinese hamster ovary (CHO) cells. In in vitro studies, IRL 2500 inhibited the sarafotoxin S6c (STX6c)-mediated contraction of the dog saphenous vein (pK(b) 7.77) and the STX6c-induced relaxation of the preconstricted rabbit mesenteric artery (pK(b) 6.92). In the anesthetized rat, IRL 2500 (10 mg/kg, i.v.) inhibited the initial transient decrease in mean arterial pressure (MAP) induced by the ET(B)-selective agonist IRL 1620 (0.5 nmol/kg, i.v.). IRL 2500 also attenuated the IRL 1620-mediated increase in renal vascular resistance (RVR) in the anesthetized rat. Therefore, IRL 2500 is a potent and selective ET(B) receptor antagonist that can be used to delineate ET responses mediated by the ET(B) receptor.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 21/09/20 alle ore 12:41:07