PMID: 8587422Jan 1, 1995Paper

Agonist-dependent inhibition by peptide and nonpeptide endothelin receptor antagonists in the rabbit isolated pulmonary artery

Journal of Cardiovascular Pharmacology
G BeckE H Ohlstein

Abstract

This study examined the effect of peptide and nonpeptide endothelin (ET) receptor antagonists on the contractile actions of ET-1 and sarafotoxin S6c (STXc) in the rabbit isolated pulmonary artery (RbPA). The peptide antagonists BQ-123, BQ-788, and RES-701 (10 microM) did not inhibit ET-1-induced RbPA contractions. The nonpeptide antagonists PD 156123, Ro 47-0203, and SB 217242 (10 microM) also had no effect on ET-1--induced contractions. In contrast, the nonpeptide antagonists SB 209670 and L-749,239 (10 microM) both caused a shift to the right of the ET-1 concentration-response curve (Kbs of 231 nM and 1.42 microM, respectively) and a two- to three-fold increase in nH (Hill slope), without altering the Rmax (maximal agonist-induced contraction). Contractile responses to STXc were unaffected by BQ-123, RES-701, and PD 156123 (10 microM). SB 209670, SB 217242, L-749,239, Ro 47-0203, and BQ-788 (10 microM) caused a shift to the right of the STXc response curve (Kbs of 16, 353, 202, 1,303 and 1,499 nM, respectively) and an increase in nH and Rmax. SB 209670 and L-749,239 were both approximately 10-fold more potent in antagonizing STXc than ET-1. Assuming, at best, Kbs of 10 microM for SB 217242, Ro 47-0203, and BQ-788 against ET-1...Continue Reading

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