Receptor occupancy with digoxin vs receptor occupancy with a putative endogenous digitalislike factor.
The possibility that an endogenous ligand for the digitalis receptor might exist has been a source of speculation resulting in efforts over the past decades to identify such a hormone. In the current context it is of interest that prolonged wash of myocardial and skeletal muscular samples from subjects who were not in digoxin treatment generally resulted in small tendencies to increase 3H-ouabain binding ranging from 2 to 9% and from -2 to 7%, respectively. It may be appreciated that neither wet weight nor water content of left ventricular or skeletal muscular samples have been found to change as a result of the prolonged wash. Although these tendencies most likely are a mere play of chance, it may be argued that the studies did not entirely rule out the possibility of the existence of a quantitatively small amount of endogenous digitalislike factor. However, based on the evaluations of receptor occupancy with digoxin during treatment of 24-34% in the left ventricle and 9-13% in skeletal muscle, it would seem reasonable to expect that a comparatively larger fraction of digitalis receptors should be occupied by a putative endogenous digitalislike factor, if such a factor were to be of any physiological significance.
Schmidt
T A
TA
Department of Medicine B, The Heart Centre, Rigshospitalet, Denmark.
Bundgaard
H
H
Kjeldsen
K
K
D001667:Binding, Competitive; D002298:Cardenolides; D002316:Cardiotonic Agents / Q000378:metabolism / Q000494:pharmacology*; D004077:Digoxin / Q000378:metabolism / Q000494:pharmacology*; D006801:Humans; D066298:In Vitro Techniques; D018482:Muscle, Skeletal / Q000737:chemistry / Q000201:enzymology; D009206:Myocardium / Q000737:chemistry / Q000201:enzymology; D010042:Ouabain / Q000378:metabolism / Q000494:pharmacology; D011869:Radioligand Assay; D012503:Saponins / Q000378:metabolism*; D000254:Sodium-Potassium-Exchanging ATPase / Q000032:analysis / Q000037:antagonists & inhibitors / Q000378:metabolism*; D014316:Tritium
D002298:Cardenolides; D002316:Cardiotonic Agents; D012503:Saponins; C027082:digitalis receptor; C034504:digoxin-like factors; D014316:Tritium; D010042:Ouabain; D004077:Digoxin; D000254:Sodium-Potassium-Exchanging ATPase