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[特定血管紧张素抑制剂在激素-受体相互作用研究中的应用]

[Use of specific angiotensin inhibitors in the study of hormone-receptor interaction].

作者信息

Myshlyakova N V, Klusha V E, Chipens G I

出版信息

Biokhimiia. 1976 Jul;41(6):1008-13.

PMID:194624
Abstract

The specificity of receptors participating in the interaction with angiotensin II (AT 1--8) fragments, e. g. N-terminal tri-(AT 1--3), C-terminal penta-(AT 4--8), and middle tetrapeptide (at 3--6), was studied in experiments on rat ascending colon which were performed to investigate the influence of a specific angiotensin antagonist, /1-hydantoic acid, 5-valine, 8-alanine/-angiotensin (HAAT 1--8), on myotropic effects of these fragments as well as the influence of the fragments on the myotropic activity of the whole hormone molecule. Competitive antagonism was found between HAAT 1--8 and AT 4--8 and AT 3--6 and between these fragments and AT 1--8. No antagonisma was revealed between AT 1--3 and HAAT 1--8, and between AT 1--3 and AT 1--8. It is assumed that the fragments AT 4--8 and AT 3--6 interact at the level of angiotensin receptors, and that of AT 1--3 at the level of non-specific receptors. A new model for the structural and functional organization of angiotensin is proposed.

摘要

在大鼠升结肠实验中研究了参与与血管紧张素II(AT 1-8)片段相互作用的受体特异性,例如N端三肽(AT 1-3)、C端五肽(AT 4-8)和中间四肽(at 3-6),这些实验旨在研究特异性血管紧张素拮抗剂/1-乙内酰脲酸,5-缬氨酸,8-丙氨酸/-血管紧张素(HAAT 1-8)对这些片段的肌动效应的影响以及这些片段对整个激素分子肌动活性的影响。发现HAAT 1-8与AT 4-8和AT 3-6之间以及这些片段与AT 1-8之间存在竞争性拮抗作用。在AT 1-3与HAAT 1-8之间以及AT 1-3与AT 1-8之间未发现拮抗作用。推测片段AT 4-8和AT 3-6在血管紧张素受体水平相互作用,而AT 1-3在非特异性受体水平相互作用。提出了一种血管紧张素结构和功能组织的新模型。

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