Autoradiographic localization of [125I]Endothelin binding sites in human blood vessels and coronary tissue: Functional correlates

M. R. Dashwood, R. M. Sykes, J. R. Muddle, M. J. Collins, S. Prehar, S. Theodoropoulos, M. H. Yacoub

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    The distribution of endothelin-1 (ET-1) receptors on human vascular tissue has been studied. High- and low-resolution autoradiography was used to determine the distribution of [125]ET binding sites in human blood vessels and ventricular myocardium. Dense, displaceable [125I]ET binding was associated with cardiac myocytes and the smooth muscle layer of all vessels were examined. There was also dense binding to vasa vasora. There was increased [125I]ET binding to atheromatous coronary arteries and vein graft, which was associated with the tunica media and vasa vasora or regions of neovascularization. Vasoconstrictor and positive inotropic activity of ET-1 has been established in vitro. The vasoconstrictor effect of ET-1 is likely to be mediated via the binding sites identified on vascular smooth muscle. The striking perivascular [125I]ET-1 binding suggests that ET-1 may also have constrictor activity on vasa vasora. There is experimental evidence that ET-1 has mitogenic activity on vascular smooth muscle cells in culture. The increased binding to both smooth muscle and regions of neovascularization in atheromatous vessels suggests that ET-1 may play a role in atherosclerosis.
    Original languageEnglish
    Pages (from-to)S458-S462
    JournalJournal of Cardiovascular Pharmacology
    Issue number7
    Publication statusPublished - 1991


    • Atheroma
    • Autoradiography
    • Human vascular tissue
    • Neovascularization
    • Vasa vasora
    • Vascular smooth muscle


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