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Titolo:
INDUCTION OF ENDOTHELIUM-DEPENDENT RELAXATION IN THE RAT AORTA BY IRL-1620, A NOVEL AND SELECTIVE AGONIST AT THE ENDOTHELIN ET(B)-RECEPTOR
Autore:
KARAKI H; SUDJARWO A; HORI M; TAKAI M; URADE Y; OKADA T;
Indirizzi:
UNIV TOKYO,FAC AGR,DEPT VET PHARMACOL,BUNKYO KU TOKYO 113 JAPAN CIBA GEIGY JAPAN LTD,INT RES LABS TAKARAZUKA 665 JAPAN
Titolo Testata:
British Journal of Pharmacology
fascicolo: 2, volume: 109, anno: 1993,
pagine: 486 - 490
SICI:
0007-1188(1993)109:2<486:IOERIT>2.0.ZU;2-G
Fonte:
ISI
Lingua:
ENG
Soggetto:
VASCULAR SMOOTH-MUSCLE; CYTOSOLIC CALCIUM LEVELS; RELAXING FACTOR; CELLS; RECEPTOR; CLONING; ANALOGS;
Keywords:
IRL-1620; ET(B)-RECEPTOR AGONIST; IRL-1038; ET(B)-RECEPTOR ANTAGONIST; ENDOTHELIN-3; ENDOTHELIUM-DEPENDENT RELAXATION; CYTOSOLIC CA2+ LEVEL; RAT AORTA;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
27
Recensione:
Indirizzi per estratti:
Citazione:
H. Karaki et al., "INDUCTION OF ENDOTHELIUM-DEPENDENT RELAXATION IN THE RAT AORTA BY IRL-1620, A NOVEL AND SELECTIVE AGONIST AT THE ENDOTHELIN ET(B)-RECEPTOR", British Journal of Pharmacology, 109(2), 1993, pp. 486-490

Abstract

1 The effects of a novel and selective agonist at the endothelin ET(B) receptor, IRL 1620 (Suc-[Glu9, Ala11,15] endothelin-1 (8-21)), were examined in the isolated aorta of the rat. 2 IRL 1620 (1-300 nM) changed neither the resting tone nor the cytosolic Ca2+ level ([Ca2+]i) of the aorta without endothelium. In the presence of endothelium, however, IRL 1620 increased endothelial [Ca2+]i with little effect on the muscle tone. In the absence of external Ca2+, IRL 1620 still induced a transient increase in endothelial [Ca2+]i. 3 Noradrenaline (100 nM) increased both muscle [Ca2+]i and tension. IRL 1620 (1-300 nM) relaxed themuscle with an increase in endothelial [Ca2+]i only in the presence of endothelium. An inhibitor of nitric oxide synthase, 100 muM N(G)-monomethyl-L-arginine, inhibited the relaxant effect of IRL 1620 but not the increase in endothelial [Ca2+]i. 4 In resting and noradrenaline-stimulated aorta, the effects of IRL 1620 were inhibited by a selective antagonist of the ET(B) receptor, IRL 1038 (0.3-3 muM), although a selective antagonist of the ET(A) receptor, BQ-123 (3 muM), was ineffective. Verapamil (10 muM) did not alter the effects of IRL 1620. 5 A muscarinic receptor agonist, carbachol (1 muM), also induced endothelium-dependent relaxation with an increase in endothelial [Ca2+]i. However, the effects of carbachol were not inhibited by the ET(B) antagonist, IRL 1038 (3 muM).6 These results suggest that IRL 1620 is a selective agonist at the ET(B) receptor which increases endothelial (Ca2+]i by releasing Ca2+ from storage sites and by opening non-L type Ca2+ channels, activates nitric oxide synthase, releases nitric oxide, and relaxesvascular smooth muscle.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 07/07/20 alle ore 18:46:03