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Ouabain-receptor interactions in (Na++K+)-ATPase preparations

IV. The molecular structure of different cardioactive steroids and other substances and their affinity to the glycoside receptor

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Summary

  1. 1.

    Dissociation constants (K D ) of the drug receptor complexes of 28 different cardiac glycosides have been determined either with [3H] labelled cardio-active steroids or from displacement of (3H] ouabain with unlabelled cardiac clycosides from the receptor. There is only one single type of cardiac glycoside receptor.

  2. 2.

    Structure-affinity relationship of the different cardiac glycosides indicate that cardiac glycosides are recognized from interactions with

  1. a)

    the unsaturated lactone group

  2. b)

    the steroid nucleus with a cis-configuration of the A∶B ring junction

  3. c)

    the sugar component.

  4. 3.

    Diphenylhydantoin displaces cardiac glycosides from the receptor, and so does prednison-3,20-bisguanylhydrazone.

  5. 4.

    The cardiac glycoside receptor concentration increases proportionally with (Na++K+)-activated ATPase activity. Occupation of the cardiac glycoside receptor results in a proportional inhibition of (Na++K+)-ATPase activity.

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  1. Erland Erdmann

    Present address: Medizinische Universitätsklinik, Georg-August-Universität Göttingen, Humboldtallee 1, D-3400, Göttingen, Germany

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  1. Institut für Biochemie und Endokrinologie, Justus Liebig-Universität, Gießen

    Erland Erdmann & Wilhelm Schoner

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Erdmann, E., Schoner, W. Ouabain-receptor interactions in (Na++K+)-ATPase preparations. Naunyn-Schmiedeberg's Arch. Pharmacol. 283, 335–356 (1974). https://doi.org/10.1007/BF00501108

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