Characterization of digoxin binding and daunorubicin uptake by isolated mature rat cardiac myocytes.

Myocytes isolated from ventricular muscle of mature rat heart have been used for characterization of digoxin binding and to establish whether a relationship exists between digoxin binding and uptake of daunorubicin. High- and low-affinity digoxin binding sites have been identified; respectively, 0.9 +/- 0.1 X 10(7) sites/myocyte, Kd 70-77 nM and 7 +/- 2 X 10(7) sites/myocyte, Kd 1.4-1.7 microM. Myocytes accumulate daunorubicin to an intracellular concentration 30-40 times that in the medium. We find no evidence that saturation of digoxin binding sites alters daunorubicin uptake or that daunorubicin influences binding of digoxin. Alteration of sarcolemmal membrane properties is demonstrated by inhibition of amino acid transport reflected in protein synthesis rates. Calmodulin activation of phosphodiesterase appears insensitive to daunorubicin.