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阻断组织肾素-血管紧张素系统:未来治疗的基石

Blocking the tissue renin-angiotensin system: the future cornerstone of therapy.

作者信息

Unger T, Azizi M, Belz G G

机构信息

Institute of Pharmacology, Christian Albrechts University, Kiel, Germany.

出版信息

J Hum Hypertens. 2000 Oct;14 Suppl 2:S23-31. doi: 10.1038/sj.jhh.1001070.

DOI:10.1038/sj.jhh.1001070
PMID:11086633
Abstract

The development of angiotensin-converting enzyme inhibitors and selective angiotensin type 1 (AT1)-receptor antagonists has provided new insights into understanding the mechanism of the renin-angiotensin system (RAS) in the pathophysiology of cardiovascular disease. There is good evidence from meta-analyses that shows that inhibition of the RAS achieves organ protection features that go beyond blood pressure control. Candesartan cilexetil, a new angiotensin II receptor antagonist, is characterised by its tight binding to and slow dissociation from the AT1 receptor, and high antagonistic potency, resulting in long-lasting antagonistic effects. It is anticipated that these pharmacological characteristics may bring additional benefits to patients, not only for the management of essential hypertension but also for the management of end-organ damage.

摘要

血管紧张素转换酶抑制剂和选择性血管紧张素1型(AT1)受体拮抗剂的研发,为理解肾素-血管紧张素系统(RAS)在心血管疾病病理生理学中的机制提供了新的见解。荟萃分析有充分证据表明,抑制RAS可实现超出血压控制的器官保护作用。新型血管紧张素II受体拮抗剂坎地沙坦酯,其特点是与AT1受体紧密结合且解离缓慢,拮抗效力高,从而产生持久的拮抗作用。预计这些药理学特性可能给患者带来更多益处,不仅用于原发性高血压的治疗,还可用于终末器官损伤的治疗。

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Blocking the tissue renin-angiotensin system: the future cornerstone of therapy.阻断组织肾素-血管紧张素系统:未来治疗的基石
J Hum Hypertens. 2000 Oct;14 Suppl 2:S23-31. doi: 10.1038/sj.jhh.1001070.
2
Persistent cardiovascular effects of chronic renin-angiotensin system inhibition following withdrawal in adult spontaneously hypertensive rats.成年自发性高血压大鼠撤药后慢性肾素-血管紧张素系统抑制的持续性心血管效应
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Renal responses to angiotensin receptor antagonist and angiotensin-converting enzyme inhibitor in partially nephrectomized spontaneously hypertensive rats.部分肾切除的自发性高血压大鼠对血管紧张素受体拮抗剂和血管紧张素转换酶抑制剂的肾脏反应。
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Comparison of type 1 angiotensin II receptor blockers and angiotensin converting enzyme inhibitors in the treatment of hypertension.1型血管紧张素II受体阻滞剂与血管紧张素转换酶抑制剂治疗高血压的比较。
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Acute effects of candesartan cilexetil (the new angiotensin II antagonist) on systemic and renal haemodynamics in hypertensive patients.坎地沙坦酯(新型血管紧张素II拮抗剂)对高血压患者全身及肾脏血流动力学的急性影响
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Regional hemodynamic effects of candesartan cilexetil (TCV-116), an angiotensin II AT1-receptor antagonist, in conscious spontaneously hypertensive rats.血管紧张素II AT1受体拮抗剂坎地沙坦酯(TCV-116)对清醒自发性高血压大鼠的局部血流动力学影响。
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Key features of candesartan cilexetil and a comparison with other angiotensin II receptor antagonists.
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引用本文的文献

1
Candesartan cilexetil: an update of its use in essential hypertension.坎地沙坦酯:其在原发性高血压治疗中应用的最新进展
Drugs. 2002;62(8):1253-87. doi: 10.2165/00003495-200262080-00016.