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      Pathophysiological role of endothelin revealed by the first orally active endothelin receptor antagonist.

      Nature
      Administration, Oral, Animals, Endothelin Receptor Antagonists, Endothelins, physiology, Humans, In Vitro Techniques, Male, Molecular Structure, Muscle Contraction, drug effects, Pyrimidines, blood, pharmacology, Rats, Rats, Wistar, Sulfonamides, Vasoconstriction

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          Abstract

          Since its discovery, endothelin-1 has attracted considerable scientific interest because of its extremely potent and long-lasting vasoconstrictor effect and its binding to G-protein-coupled receptors. Plasma concentrations of endothelin-1 are low and its release by endothelial cells is polarized towards the basolateral side, suggesting that it is a paracrine factor and not a hormone. Consequently, the effect of injected endothelin-1 may not reflect the effect of endogenous endothelin-1. In contrast, blockade of the action of endogenous endothelin-1 using receptor antagonists should be a valuable means of investigating its physiological and pathological effects. We report here evidence for the pathophysiological role of endothelin-1 as brought by the first synthetic orally active nonpeptide antagonist of endothelin receptors, Ro 46-2005.

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