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Titolo:
Evidence that ET-1, but not ET-3 and S6b, ETA-receptor mediated contractions in isolated rat mesenteric arteries are modulated by co-activation of ETB receptors
Autore:
Adner, M; Shankley, N; Edvinsson, L;
Indirizzi:
Univ Hosp, UMAS, Dept Otorhinolaryngol, Allergy Lab, SE-20502 Malmo, Sweden Univ Hosp Malmo Sweden SE-20502 gol, Allergy Lab, SE-20502 Malmo, Sweden James Black Fdn Ltd, London SE25 9JE, England James Black Fdn Ltd LondonEngland SE25 9JE td, London SE25 9JE, England Univ Hosp, Dept Internal Med, SE-22185 Lund, Sweden Univ Hosp Lund Sweden SE-22185 Dept Internal Med, SE-22185 Lund, Sweden
Titolo Testata:
BRITISH JOURNAL OF PHARMACOLOGY
fascicolo: 6, volume: 133, anno: 2001,
pagine: 927 - 935
SICI:
0007-1188(200107)133:6<927:ETEBNE>2.0.ZU;2-F
Fonte:
ISI
Lingua:
ENG
Soggetto:
ENDOTHELIN-B RECEPTORS; ET(B) RECEPTORS; SMOOTH-MUSCLE; ORGAN-CULTURE; IN-VITRO; ET(A); SUBTYPES; BINDING; VASCULATURE; HETEROGENEITY;
Keywords:
rat mesenteric artery; myograph; endothelin receptors; FR139317; IRL2500; sarafotoxin 6b; sarafotoxin 6c; cross-talk; adenylate cyclase;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
35
Recensione:
Indirizzi per estratti:
Indirizzo: Adner, M Univ Hosp, UMAS, Dept Otorhinolaryngol, Allergy Lab, SE-20502 Malmo, Sweden Univ Hosp Malmo Sweden SE-20502 rgy Lab, SE-20502 Malmo, Sweden
Citazione:
M. Adner et al., "Evidence that ET-1, but not ET-3 and S6b, ETA-receptor mediated contractions in isolated rat mesenteric arteries are modulated by co-activation of ETB receptors", BR J PHARM, 133(6), 2001, pp. 927-935

Abstract

1 The effects of agonists with endothelin (ET) ETA-receptor activity have been analysed in relation to their interaction with ETB receptors in rat mesenteric arteries.2 ET-1, sarafotoxin 6b (S6b) and ET-3 induced large, slow-onset and sustained contractions whereas S6c induced weak transient contractions. However, following pre-contraction with U46619 and subsequent relaxation with forskolin, the effect of S6c was amplified, indicating a potential for powerful ETB-receptor mediated contraction.3 The selective ETA-receptor antagonist, FR139317, produced parallel rightward shifts of ET-1, S6b and ET-3 concentration-effect curves indicating that the contractions were mediated by ETA receptors. However, the corresponding FR139317 pK(B) values were significantly different between the agonists. As expected FR139317 had no effect on S6c responses.4 Pre-treatment with S6c to desensitize ETB receptors, increased ET-1 potency and the pK(B) value for FR139317. In contrast, neither the potency of S6b and ET-3 nor the pK(B) values for FR139317 estimated using these agonists were affected by ETB-receptor desensitization.5 Segments pre-contracted with submaximal concentrations of S6b and ET-3, but not ET-1, rapidly relaxed following wash-out or FR139317 administration.6 The results indicate that the small contractile response to selective ETB receptor activation, barely detectable under standard bioassay conditions, is greatly amplified when adenylate cyclase activity is elevated. Moreover, the response to ETA receptor activation by ET-1, but not ET-3 and S6b, is significantly modified by co-activation of ETB receptors. This interaction has a significant effect on the apparent affinity of ETA-receptor selective antagonists when ET-1 is used as agonist and decreases the potency of ET-I.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 16/07/20 alle ore 18:40:17