The uptake of cardiac glycosides in relation to their actions in isolated cardiac muscle

British Journal of Pharmacology
T Godfraind, M Lesne

Abstract

1. The uptake of (3)H-digitoxin, (3)H-ouabain and (3)H-dihydro-ouabain by isolated guinea-pig atria has been studied and compared with the inhibition of the sodium pump and with the inotropic effect.2. Analysis of the curve relating the uptake of digitoxin and ouabain at equilibrium to the bath concentration enabled a non-saturable and a saturable binding site to be distinguished.3. The uptake of inactive doses of dihydro-ouabain was only by a non-saturable mechanism.4. The uptake of labelled digitoxin and ouabain was reduced in the presence of another glycoside. The amount of bound glycoside was nearly equivalent to the estimated non-saturable uptake.5. The uptake was reduced at 4 degrees C to the clearance of the non-saturable site.6. ED50 of digitoxin and of ouabain for inhibition of the sodium pump were measured and compared to the ED50 for inotropic effect and to the concentrations producing a half-saturation of the saturable binding site.7. It is concluded that binding to the saturable site may be responsible for the cardiac actions of the glycosides.

References

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Citations

Dec 1, 1979·Naunyn-Schmiedeberg's Archives of Pharmacology·H Flasch, N Heniz
Jun 27, 1978·Naunyn-Schmiedeberg's Archives of Pharmacology·N Heinz, H Flasch
May 1, 1977·Naunyn-Schmiedeberg's Archives of Pharmacology·A Marzo, P Ghirardi
Sep 1, 1974·European Journal of Pharmacology·K H Damm, C Woermann
Jan 21, 1977·European Journal of Pharmacology·T Godfraind, N Morel
Dec 20, 1979·European Journal of Pharmacology·T Godfraind, J Ghysel-Burton
Nov 1, 1979·Journal of Molecular and Cellular Cardiology·E NoackB Zettner
May 1, 1990·Journal of the American College of Cardiology·A C PowellW J Louis
May 1, 1980·Proceedings of the National Academy of Sciences of the United States of America·T Godfraind, J Ghysel-Burton
Aug 1, 1979·The Journal of Cell Biology·J H WiddicombeJ Y Yee
Nov 1, 1972·British Journal of Haematology·A Goldberg
Jan 1, 1979·Scandinavian Journal of Immunology·S A Birkeland, K Kristoffersen
Sep 1, 1977·British Journal of Pharmacology·M BentfeldD Proppe
Jan 1, 1976·Drug Metabolism Reviews·W J Jusko, M Gretch
Mar 15, 1979·Experimental Cell Research·L Hammarström, C I Smith
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Jun 10, 1975·Philosophical Transactions of the Royal Society of London. Series B, Biological Sciences·S R Levinson
Sep 8, 1973·Naunyn-Schmiedeberg's Archives of Pharmacology·A RoeschW Schaumann
Mar 1, 1977·British Journal of Pharmacology·K G GreinerJ R Wood
May 1, 1985·The American Journal of Physiology·J H WiddicombeE Highland
Apr 15, 1975·Biochemical Pharmacology·T Godfraind
Oct 15, 1974·Biochemical Pharmacology·A Marzo, P Ghirardi

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