反向激动剂的特性和研究进展

发布时间：2018-01-28 23:37

本文关键词： 反向激动剂固有活性二态模型 G蛋白耦联受体　出处：《西安交通大学学报(医学版)》2015年03期 　论文类型：期刊论文

【摘要】：反向激动剂是一种新的作用于受体的药物类型,其研究经历了β-卡波啉乙酯的发现、活性研究、概念的提出、二态模型、固有活性几个阶段。多数G蛋白耦联受体具有固有活性,在无激动剂时,部分受体处于活化状态,能主动产生效应。反向激动剂对受体有亲和力,无内在活性,不激动受体,但能拮抗受体的固有活性,产生与激动剂相反的效应。反向激动剂和激动剂均能产生效应,但机制不同,激动剂激动受体,反向激动剂拮抗受体;反向激动剂和拮抗剂均拮抗受体,但反向激动剂拮抗受体的固有活性,而拮抗剂拮抗激动剂的效应。反向激动剂可以治疗受体固有活性增强性疾病,可上调和增敏固有活性受体,内源性反向激动剂可维持特定的生理功能。反向激动剂的研究对于完善受体学说有重要的理论意义,对于固有活性增强性疾病的诊断和治疗具有重要的临床意义。
[Abstract]:Reverse agonist is a new type of drug acting on receptor. Its research has experienced the discovery of 尾 -carboline ethyl ester, the study of its activity, the concept of development, and the two-state model. Most G protein-coupled receptors have intrinsic activity, some of them are active without agonists, and the reverse agonists have affinity to the receptors and have no intrinsic activity. It can antagonize the intrinsic activity of the receptor and produce the opposite effect with the agonist. The reverse agonist and the agonist can produce the effect, but the mechanism is different: the agonist excites the receptor, the reverse agonist antagonizes the receptor; Both the reverse agonist and the antagonist antagonize the receptor, but the reverse agonist antagonizes the intrinsic activity of the receptor, while the antagonist antagonizes the effect of the agonist. Endogenous reverse agonists can maintain specific physiological functions. The study of reverse agonists is of great theoretical significance to improve the receptor theory. It has important clinical significance for the diagnosis and treatment of inherent active enhancement disease.
【作者单位】：西安交通大学医学部;
【分类号】：R96
【正文快照】： 反向激动剂(inverse agonist)又名负性激动剂(negative agonist),是一种新的作用于受体的药物类型。其概念的提出可追溯到20世纪80年代,由于其特别的作用方式和临床价值,已成为近年来的热门研究课题。反向激动剂单独使用时,能产生效应,而拮抗剂单独使用不产生效应,因而不同于

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