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来自高血压肾衰竭患者腹膜透析液的一种不稳定钠泵抑制剂:效能评估

A labile sodium pump inhibitor from the peritoneal dialysate of hypertensive renal failure patients: estimates of potency.

作者信息

Graves S W, Tao Q F, Markides K E, Williams G H, Hollenberg N K

机构信息

Department of Medicine, Harvard Medical School and Brigham and Women's Hospital, Boston, Massachusetts 02115, USA.

出版信息

Clin Exp Hypertens. 1998 Jul-Aug;20(5-6):611-6. doi: 10.3109/10641969809053239.

DOI:10.3109/10641969809053239
PMID:9682917
Abstract

Estimations of concentration of the labile sodium pump inhibitor isolated from human peritoneal dialysate were made using supercritical fluid chromatography coupled to flame ionization detection to determine the quantity of this factor in half of a purified preparation of the factor compared to the bioactivity of the other half in different assays. Ouabain was used for comparison. The labile factor appeared to be 30 times more effective than ouabain against canine renal [Na,K]ATPase. Moreover, this same factor appeared to be approximately 1,000 times more potent than ouabain in causing vascular smooth muscle contraction. The differences between this labile sodium pump inhibitor and ouabain most likely reflect their respective binding affinities. The assay differences in half maximal response to the labile sodium pump inhibitor may be due to differences in sodium pump alpha isoform sensitivity.

摘要

使用超临界流体色谱-火焰离子化检测法对从人腹膜透析液中分离出的不稳定钠泵抑制剂的浓度进行了测定,以确定该因子纯化制剂一半中的该因子量,并与另一半在不同测定中的生物活性进行比较。使用哇巴因作为对照。该不稳定因子对犬肾[钠,钾]ATP酶的作用似乎比哇巴因强30倍。此外,在引起血管平滑肌收缩方面,该因子的效力似乎比哇巴因强约1000倍。这种不稳定钠泵抑制剂与哇巴因之间的差异很可能反映了它们各自的结合亲和力。对不稳定钠泵抑制剂半数最大反应的测定差异可能是由于钠泵α同工型敏感性的差异。

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