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Titolo:
ENDOTHELIN ET(B) RECEPTOR ANTAGONIST, RES-701-1 - EFFECTS ON ISOLATEDBLOOD-VESSELS AND SMALL-INTESTINE
Autore:
KARAKI H; SUDJARWO A; HORI M; TANAKA T; MATSUDA Y;
Indirizzi:
UNIV TOKYO,GRAD SCH AGR & LIFE SCI,DEPT VET PHARMACOL,BUNKYO KU TOKYO113 JAPAN KYOWA HAKKO KOGYO CO LTD,TOKYO RES LABS MACHIDA 194 TOKYO JAPAN
Titolo Testata:
European journal of pharmacology
fascicolo: 3, volume: 262, anno: 1994,
pagine: 255 - 259
SICI:
0014-2999(1994)262:3<255:EERAR->2.0.ZU;2-R
Fonte:
ISI
Lingua:
ENG
Soggetto:
RAT AORTA; DEPENDENT RELAXATION; SELECTIVE AGONIST; ETA RECEPTOR; B RECEPTOR; POTENT; IRL-1620; CLONING; SUBTYPE;
Keywords:
SMOOTH MUSCLE; EDRF (ENDOTHELIUM-DERIVED RELAXING FACTOR); ENDOTHELIN; ENDOTHELIN ET(B) RECEPTOR; ENDOTHELIN ET(B) RECEPTOR ANTAGONIST; RES-701-1;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
19
Recensione:
Indirizzi per estratti:
Citazione:
H. Karaki et al., "ENDOTHELIN ET(B) RECEPTOR ANTAGONIST, RES-701-1 - EFFECTS ON ISOLATEDBLOOD-VESSELS AND SMALL-INTESTINE", European journal of pharmacology, 262(3), 1994, pp. 255-259

Abstract

RES-701-1 (cyclic -Gly-Thr-Ala-Pro-Asp-Trp-Phe-Phe-Asn-Tyr-Tyr-Trp)) a peptide isolated from Streptomyces sp., has been reported to inhibitthe endothelin ET(B) receptor. We examined the effects of this peptide on the blood vessels and the small intestine. In isolated rat aorta without endothelium, 10 mu M RES-701-1 did not affect the resting tone, nor did it attenuate the contractions induced by endothelin-1, endothelin-3 or norepinephrine. In the aorta with endothelium, 3 mu M RES-701-1 shifted the concentration-response curves for the contractile effects of endothelin-1 and endothelin-3 to the left. Removal of endothelium showed a similar effect to 3 mu M RES-701-1. In the norepinephrine-stimulated aorta, endothelium-dependent relaxation induced by endothelin-3 was antagonized by 0.3-10 mu M RES-701-1 in a concentration-dependent manner. In the guinea pig ileum stimulated by carbachol, endothelin-3 induced a transient relaxation followed by sustained relaxation. RES-101-1 (3 mu M) selectively inhibited the transient relaxation. Since it has been shown that the contractile effects of endothelins in the aorta are mediated by the endothelin ET(A) receptor whereas the endothelium-dependent relaxation and the ileal relaxation are mediated bythe endothelin ET(B) receptor, it is suggested that RES-701-1 is a selective antagonist against the endothelin ET(B) receptor.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 04/07/20 alle ore 21:28:22