不同化学结构盐皮质激素受体拮抗剂在心血管疾病中的应用  

Application of Mineralocorticoid Receptor Antagonists with Different Chemical Structures in Cardiovascular Diseases

作　　者：林中樵 陈佩佩 王蕾[1] LIN Zhongqiao;CHEN Peipei;WANG Lei(General Medical Department,Third Hospital of Shanxi Medical University,Shanxi Bethune Hospital,Shanxi Academy of Medical Sciences,Taiyuan 030032,China;Nanofabrication Laboratory,National Center for Nanoscience and Technology,Chinese Academy Sciences,Beijing 100190,China)

机构地区：[1]山西医科大学第三医院(山西白求恩医院,山西医学科学院)综合医疗科,太原030032 [2]中国科学院国家纳米科学中心纳米加工实验室,北京100190

出　　处：《高等学校化学学报》2022年第6期16-26,共11页Chemical Journal of Chinese Universities

基　　金：山西省重点研发计划项目(批准号:201803D31145);山西省留学人员科技活动择优资助项目(批准号:20200031)资助.

摘　　要：盐皮质激素受体的过表达或过度激活通常参与心血管疾病的发生发展.通过拮抗盐皮质激素受体,抑制其过度激活,阻断盐皮质激素受体介导的生物学效应,能够有效治疗相关疾病.拮抗盐皮质激素受体化合物的化学结构决定了拮抗效应的强弱和临床上的针对性应用.通过对盐皮质激素受体拮抗剂进行化学结构的优化,改善其药理特性,不仅增加了对盐皮质激素受体的选择性,还降低了不良反应的发生率和严重程度,同时在心血管疾病治疗方面也有不同侧重.本文总结了不同化学结构的盐皮质激素受体拮抗剂螺内酯(Spironolac⁃tone)、依普利酮(Eplerenone)和非奈利酮(Finerenone)的作用机制、药理特性和心血管疾病临床应用的各自优势,以期在后续临床应用以及新药研发方面提供新的思路.Over-activation or over-expressions of mineralocorticoid receptors lead to cardiovascular disease and di-sease progression.Antagonizing mineralocorticoid receptor,inhibiting its over activation and blocking the biological effects mediated by mineralocorticoid receptor,which is effective treatment of those diseases.The different chemical structures of mineralocorticoid receptor antagonists determine the strength of antagonistic effect and clinical targeted application.With the development of the times,optimization of the chemical structure of mineralocorticoid receptor antagonists improves the pharmacological properties,increases the selectivity and reduce the side effects.At the same time,there are different emphases in the treatment of cardiovascular diseases.This paper summarizes the action mechanisms,pharmacological characteristics and clinical application advantages of different kinds of mineralocorti⁃coid receptor antagonists:spironolactone,eplerenone and finerenone,in order to provide new ideas in subsequent clinical application and future new drug research and development.

关 键 词：盐皮质激素受体 甾体类化合物 非甾体类化合物 心血管疾病 

分 类 号：O625.45[理学—有机化学]