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血管肽酶抑制剂对利钠肽神经激素系统的调节——高血压治疗的新方法。

The natriuretic peptide neurohormonal system modulation by vasopeptidase inhibitors--the novel therapeutical approach of hypertension treatment.

作者信息

Machowska Anna, Juszczak Kajetan, Novak Paweł, Thor Piotr

机构信息

Department of Pathophysiology, Jagiellonian University, Medical College, Cracow, Poland.

出版信息

Folia Med Cracov. 2009;50(3-4):35-42.

PMID:21853869
Abstract

Vasopeptidase inhibitors (VPI) are a new promising class of drugs, that simultaneously inhibit Angiotensin - Converting Enzyme (ACE) and an enzyme Neutral Endopeptidase (NEP), that cleaves the natriuretic peptides. These drugs, such as omapatrilat, sampatrilat, fasidotrilat, by combined inhibition of ACE and degradation of natriuretic peptides and in turn by inhibiting the Renin - Angiotensin - Aldosterone system and potentiating the Natriuretic Peptide system and Kinin system should decrease the mortality rate in the group of patients with hypertension being not adequately controlled with ACE inhibitors. Thus, finding the new therapeutic strategy using drugs that act on the hormonal systems other than Renin - Angiotensin - Aldosterone system seems to be crucial. The aim of the study was to compare the molecular aspects of the conventional schemes that are being used in the antihypertension therapy to the new drugs from the vasopeptidase inhibitors group--with focusing on the natriuretic peptide system (NPS)--and, taking these considerations, making clues about therapeutical implications to reveal promising results in antihypertension treatment.

摘要

血管肽酶抑制剂(VPI)是一类前景广阔的新型药物,它能同时抑制血管紧张素转换酶(ACE)和一种可裂解利钠肽的中性内肽酶(NEP)。这些药物,如奥帕曲拉、桑帕曲拉、法西多曲拉,通过联合抑制ACE和利钠肽的降解,进而抑制肾素-血管紧张素-醛固酮系统并增强利钠肽系统和激肽系统,应该能够降低那些使用ACE抑制剂控制不佳的高血压患者群体的死亡率。因此,寻找使用作用于肾素-血管紧张素-醛固酮系统以外激素系统的药物的新治疗策略似乎至关重要。本研究的目的是比较抗高血压治疗中使用的传统方案与血管肽酶抑制剂组新药的分子层面——重点关注利钠肽系统(NPS)——并基于这些考虑,得出有关治疗意义的线索,以揭示抗高血压治疗中的有前景结果。

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The natriuretic peptide neurohormonal system modulation by vasopeptidase inhibitors--the novel therapeutical approach of hypertension treatment.血管肽酶抑制剂对利钠肽神经激素系统的调节——高血压治疗的新方法。
Folia Med Cracov. 2009;50(3-4):35-42.
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Vasopeptidase inhibition: a new concept in blood pressure management.血管肽酶抑制作用:血压管理的新概念。
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Vasopeptidase inhibition: a new direction in cardiovascular treatment.
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Combined inhibition of neutral endopeptidase and angiotensin-converting enzyme by sampatrilat in essential hypertension.在原发性高血压中,sampatrilat对中性内肽酶和血管紧张素转换酶的联合抑制作用
Clin Pharmacol Ther. 1998 Oct;64(4):439-49. doi: 10.1016/S0009-9236(98)90075-3.
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[Vasopeptidase inhibition: a new mechanism of action--a new antihypertensive drug].血管肽酶抑制作用:一种新的作用机制——一种新型抗高血压药物
Praxis (Bern 1994). 2000 Apr 13;89(16):649-53.
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Effects of omapatrilat on pharmacodynamic biomarkers of neutral endopeptidase and Angiotensin-converting enzyme activity in humans.奥帕曲拉对人体中性内肽酶和血管紧张素转换酶活性的药效学生物标志物的影响。
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A review of vasopeptidase inhibitors: a new modality in the treatment of hypertension and chronic heart failure.
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Vasopeptidase inhibition: a novel approach to cardiovascular therapy.血管肽酶抑制作用:心血管治疗的新方法。
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Combined neutral endopeptidase inhibitors.联合型中性内肽酶抑制剂。
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