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R-PEP-27是一种强效肾素抑制剂,可降低正常志愿者的血浆血管紧张素II水平和血压。

R-PEP-27, a potent renin inhibitor, decreases plasma angiotensin II and blood pressure in normal volunteers.

作者信息

Zusman R M, Hui K Y, Nussberger J, Christensen D M, Higgins J, Carlson W D, Schoenfeld D, Haber E

机构信息

Division of Hypertension and Vascular Medicine, Massachusetts General Hospital, Boston 02114.

出版信息

Am J Hypertens. 1994 Apr;7(4 Pt 1):295-301. doi: 10.1093/ajh/7.4.295.

DOI:10.1093/ajh/7.4.295
PMID:8031544
Abstract

The hemodynamic and humoral effects of the specific human renin inhibitor R-PEP-27 were studied in six normal human subjects on low and high sodium intake diets. An intravenous infusion of R-PEP-27 (0.5 to 16 micrograms/min/kg body wt) reduced blood pressure in a dose-dependent fashion; the mean arterial blood pressure at the end of the infusion fell from 128 +/- 4/83 +/- 4 to 119 +/- 3/71 +/- 3 mm Hg (mean +/- SEM) (P < .01) during the low sodium intake diet. R-PEP-27 had no effect on blood pressure during the high sodium intake diet. R-PEP-27 significantly reduced plasma angiotensin II and aldosterone concentrations. The temporal response to R-PEP-27 suggests that it is a short-lived although highly potent competitive inhibitor of renin; this peptide is a valuable and specific physiologic probe of the renin-angiotensin system.

摘要

在六名正常人类受试者身上,研究了特定的人肾素抑制剂R-PEP-27在低钠和高钠摄入饮食情况下的血流动力学和体液效应。静脉输注R-PEP-27(0.5至16微克/分钟/千克体重)以剂量依赖方式降低血压;在低钠摄入饮食期间,输注结束时平均动脉血压从128±4/83±4降至119±3/71±3毫米汞柱(平均值±标准误)(P<.01)。在高钠摄入饮食期间,R-PEP-27对血压无影响。R-PEP-27显著降低血浆血管紧张素II和醛固酮浓度。对R-PEP-27的时间反应表明,它是一种短效但高效的肾素竞争性抑制剂;这种肽是肾素-血管紧张素系统的一种有价值且特异性的生理探针。

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Am J Hypertens. 1994 Apr;7(4 Pt 1):295-301. doi: 10.1093/ajh/7.4.295.
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引用本文的文献

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Renin inhibitors: optimal strategy for renal protection.肾素抑制剂:肾脏保护的最佳策略。
Curr Hypertens Rep. 2007 Nov;9(5):415-21. doi: 10.1007/s11906-007-0076-5.
2
Clinical pharmacokinetics and efficacy of renin inhibitors.肾素抑制剂的临床药代动力学与疗效
Clin Pharmacokinet. 1995 Jul;29(1):6-14. doi: 10.2165/00003088-199529010-00002.