强心甾体类药物：体外钠钾三磷酸腺苷抑制及离子转运与犬类正性肌力活性和毒性的相关性
Cardiotonic steroids: correlation of sodium-potassium adenosine triphosphate inhibition and ion transport in vitro with inotropic activity and toxicity in dogs.
作者信息
Beard N A, Rouse W, Somerville A R
出版信息
Br J Pharmacol. 1975 May;54(1):65-74. doi: 10.1111/j.1476-5381.1975.tb07411.x.
Abstract
- A new series of cardiotonics based on five steroid nuclei has been evaluated for inhibition of Na-+/K-+-ATPase and Rb uptake by red blood cells, and for inotropic activity and toxicity in dogs. Structure-activity relationships are discussed. 2. The in vitro tests can be used satisfactorily to predict inotropic activity, but not toxicity or therapeutic ratio. 3. Although compounds with greatly improved therapeutic ratios relative to ouabain and tolusin have been obtained, they proved to be strongly emetic in the conscious dog.
摘要
- 已对基于五个甾体核的一系列新型强心药进行了评估，以检测其对红细胞钠钾ATP酶的抑制作用、对铷摄取的影响，以及在犬类中的变力活性和毒性。讨论了构效关系。2. 体外试验可令人满意地用于预测变力活性，但不能预测毒性或治疗指数。3. 尽管已获得了相对于哇巴因和托鲁辛治疗指数有显著提高的化合物，但它们在清醒犬中表现出强烈的催吐作用。
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Cardiotonic steroids: correlation of sodium-potassium adenosine triphosphate inhibition and ion transport in vitro with inotropic activity and toxicity in dogs.强心甾体类药物：体外钠钾三磷酸腺苷抑制及离子转运与犬类正性肌力活性和毒性的相关性
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