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Research ArticleCARDIOVASCULAR

Cantharidin Enhances Norepinephrine-Induced Vasoconstriction in an Endothelium-Dependent Fashion

Jörg Knapp, Peter Bokník, Bettina Linck, Hartmut Lüss, Frank U. Müller, Lars Petertönjes, Wilhelm Schmitz and Joachim Neumann
Journal of Pharmacology and Experimental Therapeutics August 2000, 294 (2) 620-626;
Jörg Knapp
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Peter Bokník
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Bettina Linck
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Hartmut Lüss
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Frank U. Müller
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Lars Petertönjes
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Wilhelm Schmitz
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Joachim Neumann
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Abstract

In this study we characterized the effects of the protein phosphatase (PP) type 1 and type 2A inhibitor cantharidin (Cant) and its structural analogs cantharidic acid and endothall on PP activity, force of contraction, and myosin light chain phosphorylation in rat aorta. All compounds inhibited PP activity in homogenates of rat aorta with a rank order of potency of Cant = cantharidic acid > endothall. However, only Cant increased force of contraction and myosin light chain phosphorylation in intact isolated rat aortic rings. Based on these findings, we investigated the effects of Cant on α-adrenoceptor-mediated vasoconstriction. Cant (1 and 3 μM) enhanced norepinephrine-induced contraction in endothelium-intact rat aorta. In contrast, Cant did not affect norepinephrine-induced contraction in endothelium-denuded rat aorta. We suggest that inhibition of PP1 and/or PP2A activities by Cant enhances vascular contractility in endothelium-intact rat aorta by increasing the phosphorylation state of endothelial regulatory proteins.

Footnotes

  • Send reprint requests to: Dr. med. Jörg Knapp, Institut für Pharmakologie und Toxikologie, Westfälische Wilhelms-Universität Münster, Domagkstraße 12, D-48129 Münster, FRG. E-mail: jknapp{at}uni-muenster.de

  • ↵1 This study was supported by the Deutsche Forschungsgemeinschaft and the Interdisziplinäres Zentrum für Klinische Forschung, Münster.

  • Abbreviations:
    MLC20
    regulatory light chains of myosin (20 kDa)
    PP
    serine/threonine protein phosphatase
    OA
    okadaic acid
    Cant
    cantharidin
    CA
    cantharidic acid
    ETA
    endothall
    NE
    norepinephrine
    KHS
    Krebs-Henseleit solution
    CB
    carbachol
    2D-PAGE
    two-dimensional polyacrylamide gel electrophoresis
    DMSO
    dimethyl sulfoxide
    NOS
    nitric-oxide synthase
    NO
    nitric oxide
    eNOS
    endothelial NOS
    PLB
    phospholamban
    pD2
    −log EC50
    • Received December 21, 1999.
    • Accepted May 1, 2000.
  • The American Society for Pharmacology and Experimental Therapeutics
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Journal of Pharmacology and Experimental Therapeutics: 294 (2)
Journal of Pharmacology and Experimental Therapeutics
Vol. 294, Issue 2
1 Aug 2000
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Research ArticleCARDIOVASCULAR

Cantharidin Enhances Norepinephrine-Induced Vasoconstriction in an Endothelium-Dependent Fashion

Jörg Knapp, Peter Bokník, Bettina Linck, Hartmut Lüss, Frank U. Müller, Lars Petertönjes, Wilhelm Schmitz and Joachim Neumann
Journal of Pharmacology and Experimental Therapeutics August 1, 2000, 294 (2) 620-626;

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Research ArticleCARDIOVASCULAR

Cantharidin Enhances Norepinephrine-Induced Vasoconstriction in an Endothelium-Dependent Fashion

Jörg Knapp, Peter Bokník, Bettina Linck, Hartmut Lüss, Frank U. Müller, Lars Petertönjes, Wilhelm Schmitz and Joachim Neumann
Journal of Pharmacology and Experimental Therapeutics August 1, 2000, 294 (2) 620-626;
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