卡维地洛药理作用与临床应用研究进展  

Research progress in pharmacological action and clinical application of carvedilol

作　　者：周子豪 杨帆[1] 汤雅东 李茹艳 罗思琦 于航[1] 杨瑞楠 刘亚婧[1] ZHOU Zi-hao;YANG Fan;TANG Ya-dong;LI Ru-yan;LUO Si-qi;YU Hang;YANG Rui-nan;LIU Ya-jing(Key Laboratory of Structure-Based Drug Design&Discovery of Ministry of Education,Shenyang Pharmaceutical University,Shenyang LIAONING 110016,China)

机构地区：[1]沈阳药科大学基于靶点的药物设计与研究教育部重点实验室,辽宁沈阳110016

出　　处：《中国新药与临床杂志》2024年第3期170-176,共7页Chinese Journal of New Drugs and Clinical Remedies

基　　金：2021年辽宁省教育厅面上项目(LJKZ0958);2022年辽宁省应用基础研究计划项目(2022JH2/101)。

摘　　要：卡维地洛作为肾上腺素β受体阻滞药,对α1和β受体均有阻断作用,在临床上已广泛应用于高血压、心力衰竭、心律失常等心血管疾病。近年来,在预防动脉粥样硬化、保护不同并发症患者的心脏功能、改善糖尿病患者血糖调节能力、防治乳腺癌和抗阿尔茨海默病等方面进行了多项卡维地洛的临床研究。此外,随着对G蛋白偶联受体(GPCR)的深入研究,发现卡维地洛存在独特的偏向β-抑制蛋白的GPCR信号传导,高选择性作用于靶细胞,可减少药物不良反应的发生。Carvedilol,aβ-blocker with the function of blockingαs andβadrenoceptors,has been widely used in existing clinical practice for cardio vascular diseases,such as hypertension,chronic heart failure and arrhythmia.In recent years,some clinical researches showed that carvedilol might have some potentially novelty prospect on prevention of atherosclerosis,protection of cardiac function of patients with different complications,improvement of diabetic patients"ability to regulate blood sugar,and treatment of breast cancer and Alzheimer's disease.Moreover,with the further study of G protein coupled receptor(GPCR),the special mechanism ofβ-arrestin-biased GPCR signal transduction had been found in carvedilol,Which could contribute to its highly selective action on target cells and could reduce the incidence of adverse drug reactions.

关 键 词：卡维地洛 药理作用 受体 G蛋白偶联 临床应用 

分 类 号：R914[医药卫生—药物化学]