酯酶的药物代谢与种属差异研究进展  

Research Progress of Esterases in Drug Metabolism and Species Difference

作　　者：李鑫 王文艳[1] LI Xin;WANG Wenyan(School of Pharmacy,Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong,Key Laboratory of Molecular Pharmacology and Drug Evaluation of Ministry of Education,Yantai University,Yantai 264005,China)

机构地区：[1]烟台大学新型制剂与生物技术药物研究山东省高校协同创新中心分子药理和药物评价教育部重点实验室,山东烟台264005

出　　处：《药学进展》2021年第10期784-792,共9页Progress in Pharmaceutical Sciences

摘　　要：羧酸酯酶(CES)、芳基乙酰胺脱乙酰酶(AADAC)、丁酰胆碱酯酶(BCHE)和对氧磷酶(PON)是人体内重要的酯酶,参与药物在体内的代谢、活化解毒,在前药的设计中也起到非常重要的作用。围绕人体内广泛参与药物代谢的酯酶,对其在体内的组织分布、底物和抑制剂的特异性及种属差异研究进展进行综述,为临床前动物模型选择、新药的设计和开发提供参考。Carboxylesterase,arylacetamide deacetylase,butyrylcholinesterase,paraoxonase are important esterases in the human body,participating in the metabolism,activation and detoxification of drugs in the body,thus with a very important role in the design of prodrugs.This paper focuses on the esterases that are widely involved in drug metabolism in human body,and summarizes their tissue distribution in vivo,substrate and inhibitor and species differences,aiming to provide reference for preclinical selection of animal models,drugs design and development of new drugs.

关 键 词：羧酸酯酶 芳基乙酰胺脱乙酰酶 丁酰胆碱酯酶 对氧磷酶 组织分布 种属差异 

分 类 号：R969.1[医药卫生—药理学]