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Tissue selectivity of endothelin.

R Borges1, H Von Grafenstein, D E Knight

  • 1Division of Biomedical Sciences, King's College, University of London, U.K.

European Journal of Pharmacology
|June 20, 1989
PubMed
Summary
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Endothelin, a vasoconstrictor peptide, contracted various non-vascular tissues like the uterus and trachea. Its effects suggest a distinct receptor, separate from calcium channels, impacting smooth muscle modulation.

Area of Science:

  • Pharmacology
  • Physiology
  • Endocrinology

Background:

  • Endothelin is a potent endogenous vasoconstrictor peptide.
  • Its effects on diverse tissues require comprehensive investigation.

Purpose of the Study:

  • To investigate the effects of endothelin on various vascular and non-vascular tissues.
  • To determine the receptor interaction of endothelin and its relation to calcium channels.

Main Methods:

  • Administration of endothelin to isolated rat and guinea pig tissues (portal vein, aorta, uterus, trachea, vas deferens, ileum).
  • Assessment of cardiac function (inotropic and chronotropic effects) in isolated rat heart.
  • Evaluation of endothelin's impact on secretion and aggregation in various cell types (neuromuscular junction, adrenal medullary cells, neutrophils, platelets).

Related Experiment Videos

  • Testing the inhibitory effects of nifedipine, a calcium channel antagonist.

    • Main Results:

    • Endothelin caused significant contraction in rat uterus, trachea, and vas deferens, but not guinea pig ileum, at concentrations effective in aorta and portal vein.
    • Nifedipine partially inhibited endothelin-induced contractions.
    • Endothelin exhibited no inotropic or chronotropic effects on the isolated rat heart and did not affect secretion or aggregation in platelets, neutrophils, or adrenal medullary cells.
    • Tissue responsiveness to endothelin did not correlate with dihydropyridine receptor distribution, suggesting a distinct receptor.

    Conclusions:

    • Endothelin interacts with a specific receptor, distinct from dihydropyridine-sensitive calcium channels.
    • The contractile effects of endothelin on non-vascular smooth muscle indicate a potential role in epithelium-dependent modulation of non-vascular tissues, extending the concept of endothelium-dependent vascular smooth muscle tone regulation.