Akera T
Science. 1977 Nov 11;198(4317):569-74. doi: 10.1126/science.144320.
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.
由于已知其功能关联，钠钾ATP酶是受体研究的一个良好模型。在体外观察到的洋地黄与该酶的结合符合受体结合的标准。对洋地黄结合与药物作用之间关系的研究揭示了这些事件之间令人印象深刻的相关性，但未能提供因果关系的证据。对其他钠钾ATP酶抑制剂以及影响跨膜钠转运（钠钾ATP酶抑制之后的步骤）的药物的研究提供了进一步的支持性证据，即钠泵抑制以及由此导致的细胞内钠瞬变增强会引起洋地黄的正性肌力作用。
