Summary
Cardiac glycosides bind specifically with high affinity to the external surface of (Na++ K+)-ATPase thus inhibiting the sodium pump. In cardiac cell membranes, in ventricular heart tissue, and in cultured beating myocardial cells of the rat, two different types of receptors with high and low affinity for ouabain are present. These receptors mediate positive inotropic effects at low and high concentrations of ouabain. Arrhythmogenic effects never were seen when the high affinity receptor only was occupied by a drug molecule.
Evidence is presented suggesting that digitalis sensitive species also have different types of cardiac glycoside receptors in the heart.
After treatment with T3 or after chronic hypokalaemia cultured myocardial cells increase the number of high and low affinity receptors concomitantly without any change in their affinity.
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© 1987 Martinus Nijhoff Publishing, Boston
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Erdmann, E., Brown, L., Werdan, K., Berger, H.J. (1987). Multiple Forms of the Cardiac Glycoside Receptor with Different Affinities for Cardiac Glycosides. In: Beamish, R.E., Panagia, V., Dhalla, N.S. (eds) Pharmacological Aspects of Heart Disease. Developments in Cardiovascular Medicine, vol 68. Springer, Boston, MA. https://doi.org/10.1007/978-1-4613-2057-9_21
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DOI: https://doi.org/10.1007/978-1-4613-2057-9_21
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