Membrane adenosinetriphosphatase: a digitalis receptor?
The enzyme Na+,K+-ATPase is a good model for receptor studies because of its known functional correlates. The binding of digitalis to the enzyme observed in vitro satisfied the criteria for receptor binding. Studies of the relationship between the digitalis binding and the drug action reveal an impressive correlation between these events but fail to provide proof of a causal relationship. Studies with other Na+,K+-ATPase inhibitors and agents that affect transmembrane Na+ movements (steps that would follow Na+,K+-ATPase inhibition) provide further supportive evidence that sodium pump inhibition and the resulting enhancement of intracellular Na+ transients cause the inotropic action of digitalis.
D000251:Adenosine Triphosphatases / Q000037:antagonists & inhibitors / Q000378:metabolism*; D000494:Allosteric Regulation; D000818:Animals; D001692:Biological Transport / Q000187:drug effects; D002118:Calcium / Q000378:metabolism; D004071:Digitalis Glycosides / Q000378:metabolism* / Q000494:pharmacology; D009200:Myocardial Contraction / Q000187:drug effects*; D009206:Myocardium / Q000201:enzymology* / Q000378:metabolism; D011188:Potassium / Q000378:metabolism; D011955:Receptors, Drug / Q000378:metabolism*; D012964:Sodium / Q000378:metabolism; D013045:Species Specificity
D004071:Digitalis Glycosides; D011955:Receptors, Drug; D012964:Sodium; D000251:Adenosine Triphosphatases; D011188:Potassium; D002118:Calcium