Sodium-potassium adenosine triphosphatase-a receptor for digitalis?

Schwartz, A.

Biochemical Pharmacology 25(3): 237-239


ISSN/ISBN: 0006-2952
PMID: 131555
DOI: 10.1016/0006-2952(76)90206-9
Accession: 068521469

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Recent research relevant to whether Na+, K+-ATPase may represent a component of a digitalis receptor was studied. Na+, K+-ATPase is a conformationally sensitive enzyme with multiple sites. Digitalis apparently interacts with a site on an intact system located on the external surface and this somehow affects activity. The isolated enzyme system of canine kidney was characterized. Using a highly purified Na+, K+-ATPase from sheep kidney medulla, binding sites associated with the phospholipid component for Ca were demonstrated. Ouabain produced a significant decrease in affinity for Ca in the absence of Na and increased affinity in the presence of Na. Cardiac glycosides perhaps increase an extracellular-bound pool of Ca by an action on the Na+, K+-ATPase which is responsible for the increase of contractility produced by digitalis. The evidence seems to be consistent with the definition of a pharmacological receptor of a drug. Na+, K+-ATPase apparently is the pharmacological receptor for digitalis.