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Titolo:
EFFECTS OF ET ANTAGONISTS (PD143296 AND PD145065) ON CONTRACTIONS IN GUINEA-PIG HILAR BRONCHUS INDUCED BY ENDOTHELIN-1 AND ITS RELATED PEPTIDE
Autore:
NAKAJIMA Y; KIZAWA Y; NAKANO J; KOTAKE H; INAMI T; KUSAMA T; MURAKAMI H;
Indirizzi:
NIHON UNIV,COLL PHARM,DEPT PHYSIOL & ANAT FUNABASHI CHIBA 274 JAPAN NIHON UNIV,COLL PHARM,DEPT PHYSIOL & ANAT FUNABASHI CHIBA 274 JAPAN
Titolo Testata:
Receptor
fascicolo: 3, volume: 5, anno: 1995,
pagine: 177 - 183
SICI:
1052-8040(1995)5:3<177:EOEA(A>2.0.ZU;2-H
Fonte:
ISI
Lingua:
ENG
Soggetto:
RECEPTOR ANTAGONIST; ET(B) RECEPTOR; HIGHLY POTENT; ETA RECEPTOR; IRL-1620; CLONING; AGONIST;
Keywords:
ENDOTHELIN; SARAFOTOXIN S6C; IRL1620; PD145065; PD143296; BRONCHUS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
29
Recensione:
Indirizzi per estratti:
Citazione:
Y. Nakajima et al., "EFFECTS OF ET ANTAGONISTS (PD143296 AND PD145065) ON CONTRACTIONS IN GUINEA-PIG HILAR BRONCHUS INDUCED BY ENDOTHELIN-1 AND ITS RELATED PEPTIDE", Receptor, 5(3), 1995, pp. 177-183

Abstract

ETs-induced contractions were resistant to ET(A)-selective antagonists and believed to be mediated by activation of ET, receptors in guineapig bronchus. In the present study, the effects of the ET antagonists, PD143296 (Ac-D-Phe-L-Leu-L-Phe-L-Ile-L-Ile-L-Trp . 2Na) and PD145065(Ac-[{R}-2-10, 11-dihydro-5H-dibenzo{a, yclohepten-5-yl]Gly)-L-Leu-L-Asp-L-Ile-L-Ile-L-Trp . 2Na), on contractions induced by ET-1, ET-3, sarafotoxin S6c (STXc), and IRL1620 in the isolated hilar bronchus of the guinea pig were investigated. An ET(A/B) nonselective antagonist, PD145065 antagonized contractions induced by ET-1, ET-3, STXc, and IRL1620. Its antagonistic activity against ET-1, with pK(B) of 5.77 +/- 0.02 (n = 16, 3-10 mu M), was significantly lower than that against ET-3, with pK(B) of 6.18 +/- 0.02 (n = 12, 3-10 mu M), STXc, with pK, of 5.97 +/- 0.01 (n = 14, 3-10 mu M), and IRL1620, with pK, of 6.80 +/- 0.04 (n = 14, 0.3-1 mu-M) Conversely, although a putative ET(B)-selective antagonist, PD143296 (10 mu M) slightly but significantly antagonized the concentration-response curve of IRL1620 (pK(B) 5.28 +/- 0.14, n = 6), it had no effect on ET-1-, ET-3-, or STXc-induced contractions. These results suggest that ETs possibly activate ET(B2) or an atypicalET(B) receptor subtype in guinea pig hilar bronchus.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 08/08/20 alle ore 14:44:32