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[糖皮质激素受体对血管紧张素转换酶活性的调节机制及心血管疾病治疗的新前景]

[Glucocorticoid receptor mechanism of regulation of the activity of angiotensin-converting enzyme and new prospects in the treatment of cardiovascular diseases].

作者信息

Golikov P P

出版信息

Vestn Ross Akad Med Nauk. 1992(3):8-12.

PMID:1382764
Abstract

Based on the concept of glucocorticoid-receptor induction of angiotensin-converting enzyme (ACE), approaches to inhibiting enzyme induction with drugs that suppress the function of type II cytoplasmic glucocorticoid receptors, (genuine glucocorticoid receptors), are suggested. Three types of inhibiting the function of type II glucocorticoid receptors by drugs were distinguished. Type I is characterized by competition of the drugs with natural and synthetic glucocorticoids for interaction with glucocorticoid receptors (cortexolone, progesterone); type II is determined by irreversible inactivation of type II glucocorticoid receptors (aminazine, tisercin); type III is related to an increase of interaction of transcorticoid receptors with natural glucocorticoids which is accompanied by a reduction of the interaction of natural glucocorticoids with genuine glucocorticoid receptors (analgin, amidopyrine). It has been established that the drugs that provoke irreversible inactivation of the function of type II glucocorticoid receptors decrease ACE activity in blood plasma and in the lungs, that may serve the main reason for their high hypotensive effect in arterial hypertension. A concept is advanced, providing evidence for the use of the classical ACE inhibitors and of type II glucocorticoid receptor inhibitors.

摘要

基于糖皮质激素受体诱导血管紧张素转换酶(ACE)的概念,有人提出用抑制Ⅱ型细胞质糖皮质激素受体(真正的糖皮质激素受体)功能的药物来抑制酶诱导的方法。区分了三种药物抑制Ⅱ型糖皮质激素受体功能的类型。Ⅰ型的特征是药物与天然和合成糖皮质激素竞争与糖皮质激素受体的相互作用(皮质酮、孕酮);Ⅱ型由Ⅱ型糖皮质激素受体的不可逆失活决定(氯丙嗪、替色林);Ⅲ型与转糖皮质激素受体与天然糖皮质激素相互作用的增加有关,同时伴随着天然糖皮质激素与真正的糖皮质激素受体相互作用的减少(安乃近、氨基比林)。已经确定,引起Ⅱ型糖皮质激素受体功能不可逆失活的药物会降低血浆和肺中的ACE活性,这可能是它们在动脉高血压中具有高效降压作用的主要原因。提出了一个概念,为使用经典的ACE抑制剂和Ⅱ型糖皮质激素受体抑制剂提供了证据。

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