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Titolo:
NOVEL ANTAGONIST OF ENDOTHELIN ET(B1) AND ET(B2) RECEPTORS, BQ-788 - EFFECTS ON BLOOD-VESSEL AND SMALL-INTESTINE
Autore:
KARAKI H; SUDJARWO SA; HORI M;
Indirizzi:
UNIV TOKYO,GRAD SCH AGR & LIFE SCI,DEPT VET PHARMACOL,BUNKYO KU TOKYO113 JAPAN
Titolo Testata:
Biochemical and biophysical research communications
fascicolo: 1, volume: 205, anno: 1994,
pagine: 168 - 173
SICI:
0006-291X(1994)205:1<168:NAOEEA>2.0.ZU;2-O
Fonte:
ISI
Lingua:
ENG
Soggetto:
RAT AORTA; DEPENDENT RELAXATION; SELECTIVE AGONIST; ETA RECEPTOR; B RECEPTOR; POTENT; IRL-1620; CLONING; SUBTYPE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
21
Recensione:
Indirizzi per estratti:
Citazione:
H. Karaki et al., "NOVEL ANTAGONIST OF ENDOTHELIN ET(B1) AND ET(B2) RECEPTORS, BQ-788 - EFFECTS ON BLOOD-VESSEL AND SMALL-INTESTINE", Biochemical and biophysical research communications, 205(1), 1994, pp. 168-173

Abstract

The effects of a peptide, BQ-788 cyl-D-1-methoxycarbonyltryptophanyl-D-norleucine], on isolated blood vessel and small intestine were examined. In the rat aorta, BQ-788 antagonized the endothelium-dependent, ET(B1) receptor-mediated relaxation due to endothelin (ET)-3 with EC(50) of 3 mu M. In the rat aorta without endothelium, 10 mu M BQ-788 weakly antagonized the ET(A1)-mediated contractile effects of ET-1 and ET-3. In the rabbit saphenous vein, it has been shown that ET(A1), ET(A2), ET(B1) and ET(B2) receptors mediate contraction. BQ-788 (10 mu M) almost completely inhibited the contractile effect of sarafotoxin S6c (an ET(B1) and ET(B2) agonist). BQ-788 also antagonized the contractile effect of ET-3 (an ET(A1), ET(B1) and ET(B2) agonist) more strongly than desensitization of ET(B1) and ET(B2) receptors. However, BQ-788 didnot antagonize the effect of ET-1 (agonist of all four receptors). Inthe guinea pig ileum, 10 mu M BQ-788 completely inhibited the relaxation mediated by ET(B1) and ET(B2) receptors. These results suggest that BQ-788 is a novel antagonist of ET(B1) and ET(B2) receptors with weak antagonistic effect on the ET(A1) receptor. (C) 1994 Academic Press,Inc.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 10/07/20 alle ore 19:12:52