MEMBRANE ADENOSINE-TRIPHOSPHATASE - DIGITALIS RECEPTOR
MEMBRANE ADENOSINE-TRIPHOSPHATASE - DIGITALIS RECEPTOR
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DOI：
10.1126/science.144320
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发表时间：
1977-01-01
期刊：
影响因子：
56.9
通讯作者：
AKERA, T
中科院分区：
文献类型：
--
作者：
AKERA, T
Na+，K+-ATPase是受体研究的一个很好的模型，因为它具有已知的功能相关性。洋地黄与体外观察到的酶的结合符合受体结合的标准。对洋地黄结合和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。对其他影响跨膜Na+运动的Na+，K+-ATPase抑制剂和药物的研究提供了进一步的支持性证据，证明Na泵抑制和由此导致的细胞内Na+瞬变的增强导致了洋地黄的变力作用。
The enzyme Na+,K+-ATPase was a good model for receptor studies because of its known functional correlates. Binding of digitalis to the enzyme observed in vitro satisfied the criteria for receptor binding. Studies of the relationship between digitalis binding and drug action revealed an impressive correlation between these events but failed 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) provided further supportive evidence that Na pump inhibition and the resulting enhancement of intracellular Na+ transients caused the inotropic action of digitalis.