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激肽拮抗剂:设计与活性

Kinin antagonists: design and activities.

作者信息

Stewart J M, Vavrek R J

机构信息

Department of Biochemistry, University of Colorado School of Medicine, Denver 80262.

出版信息

J Cardiovasc Pharmacol. 1990;15 Suppl 6:S69-74.

PMID:1697364
Abstract

Bradykinin antagonists effective in a great variety of kinin-responsive tissues have been developed and used to study the roles of kinins in various physiological and pathological phenomena. Structural changes required to yield antagonists and to confer high potency, tissue selectivity, and resistance to enzymatic degradation have been explored in several hundred analogs. Certain of these offer promise for the development of drugs effective against pain, inflammation, and asthma.

摘要

已开发出对多种激肽反应性组织有效的缓激肽拮抗剂,并用于研究激肽在各种生理和病理现象中的作用。在数百种类似物中探索了产生拮抗剂并赋予高效力、组织选择性和抗酶降解能力所需的结构变化。其中某些化合物有望开发出有效对抗疼痛、炎症和哮喘的药物。

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