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BQ-123 is extensively used as an antagonist at endothelin (ET) receptors, having selectivity at the ET A receptor subtype. In this study, the effects of BQ-123 per se on action potentials, l-type calcium currents, and potassium currents, were examined in ventricular cardiomyocytes isolated from adult, male, New Zealand White rabbits, using the patch-clamp technique. BQ-123 (1μM) increased...
IRL1620, a specific endothelin ET B receptor agonist, induced relaxation followed by contraction in the guinea-pig ileum, as did endothelin-1. Both components of the response were concentration-dependent in the range studied. Repeated administration of IRL1620 induced tachyphylaxis only of the contractile component, whereas endothelin-1 desensitized both components. BQ-123 (cyclo[d-Trp-d-Asp-Pro-d-Val-Leu]),...
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