药物转运体的研究方法.pdf

药学学报 Acta Pharmaceutica Sinica 2014, 49 (7): 963−970 ·963 · 药物转运体的研究方法 * 李 聃, 盛 莉, 李 燕 ( 中国医学科学院、北京协和医学院药物研究所药物代谢室, 天然药物活性物质与功能国家重点实验室, 活性物质发现与适药化研究北京市重点实验室, 北京 100050) 摘要: 位于细胞膜上的转运体是体内重要的功能性膜蛋白, 在药物吸收、分布、代谢及排泄的动力学过程中 发挥重要作用。转运体的功能缺失或抑制是引起药物相互作用及某些疾病的重要原因。了解转运体的功能对阐 明药物的体内药代动力学特征、药效及毒性具有重要意义。本文对目前常用的主要药物转运体的研究方法进行 综述。 关键词: 转运体; 药物吸收; 药物相互作用 中图分类号: R969.1 文献标识码: A 文章编号: 0513-4870 (2014) 07-0963-08 Methods for the study of drug transporters * LI Dan, SHENG Li, LI Yan (Department of Drug Metabolism, Beijing Key Laboratory of Active Substances Discovery and Drug Ability Evaluation, State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences Peking Union Medical College, Beijing 100050, China) Abstract : As a functional membrane protein, drug transporters play an important role in the absorption, distribution, metabolism and excretion of drugs. The functional omission or inhibition of drug transporters is believed to be involved in the drug-drug interaction and pathogenesis of certain diseases. Understanding the function of drug transporters is highly significant in terms of pharmacokinetics, pharmacodynamics and toxicity of drugs. This article summarized the methods for the study of drug transporters in vitro and in vivo. Key words: drug t