PMID: 9163578Mar 12, 1997Paper

Influence of endothelin ET(A) and ET(B) receptor antagonists on endothelin-induced contractions of the guinea pig isolated gall bladder

Regulatory Peptides
A M CardozoG A Rae

Abstract

The receptors mediating guinea pig gall bladder (GPGB) contractions induced by endothelin-1 (ET-1) and related peptides were characterized using various ET receptor antagonists. As all ET-receptor agonists used, except sarafotoxin S6c (SRTX), failed to induce a clear-cut maximal response at the highest concentration tested (i.e. 100 nM), their potencies are expressed in terms of a CK50 (i.e. the concentration causing 50% of the response to 80 mM KCl). ET-1 (CK50 0.8 nM) was equipotent to ET-2 and SRTX (selective ET(B) receptor agonist), but more potent than ET-3 (5-fold) or IRL 1620 (selective ET(B) receptor agonist). BQ-123 (0.3 microM, peptidic ET(A) receptor antagonist) did not alter responses to ET-1, ET-3 or SRTX. BQ-788 (1 microM, peptidic ET(B) receptor antagonist) reduced the potency of ET-3 (9-fold at the CK50 level) and SRTX ( > 20-fold), but not ET-1. SRTX responses were unaffected by RES-701-1 (3 microM, peptidic ET(B) receptor antagonist). The combination BQ-123 (0.3 microM) plus BQ-788 (1 microM) did not modify responses to ET-1, inhibited SRTX responses similarly to BQ-788 alone and abolished ET-3 responses. Bosentan (1 microM, non-peptidic ET(A)/ET(B) receptor antagonist) reduced the potency of ET-1 (15-fold). E...Continue Reading

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Citations

Mar 7, 2001·Regulatory Peptides·S C HuangS M Huang
Oct 16, 2001·Regulatory Peptides·B O Al-JiffryG T Saccone
May 2, 2002·Journal of Gastroenterology and Hepatology·Bilal O Al-JiffryGino T P Saccone
Jan 22, 2005·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·S Remzi Erdem, Meral Tuncer
Jun 19, 2002·Cardiovascular Drug Reviews·Megumu Okada, Masaru Nishikibe

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