Transporter systems involved in the permeation of drugs and solutes across biological membranes are recognized as key determinants of pharmacokinetics. Typically, the action of membrane transporters on drug exposure to tissues in living organisms is inferred from invasive procedures, which cannot be applied in humans. In recent years, imaging methods have greatly progressed in terms of instruments, synthesis of novel imaging probes as well as tools for data analysis. Imaging allows pharmacokinetic parameters in different tissues and organs to be obtained in a non-invasive or minimally invasive way. The aim of this overview is to summarize the current status in the field of molecular imaging of drug transporters. The overview is focused on human studies, both for the characterization of transport systems for imaging agents as well as for the determination of drug pharmacokinetics, and makes reference to animal studies where necessary. We conclude that despite certain methodological limitations, imaging has a great potential to study transporters at work in humans and that imaging will become an important tool, not only in drug development but also in medicine. Imaging allows the mechanistic aspects of transport proteins to be studied, as well as elucidating the influence of genetic background, pathophysiological states and drug-drug interactions on the function of transporters involved in the disposition of drugs.

涉及药物和溶质跨生物膜渗透的转运蛋白系统被认为是药代动力学的关键决定因素。通常，膜转运蛋白对药物暴露于活生物体组织的作用是从侵入性过程中推断出来的，而侵入性过程无法应用于人类。近年来，成像方法在仪器，新型成像探针的合成以及数据分析工具方面取得了长足的进步。成像允许以无创或微创方式获得不同组织和器官中的药代动力学参数。本概述的目的是总结药物转运蛋白分子成像领域的当前状况。概述着重于人类研究，既可用于表征显像剂的运输系统，也可用于确定药物药代动力学，并在必要时参考动物研究。我们得出的结论是，尽管存在某些方法上的局限性，但成像技术仍具有研究人类工作转运蛋白的巨大潜力，并且成像技术将不仅在药物开发中而且在医学中都将成为重要的工具。影像学可以研究转运蛋白的力学方面，并阐明遗传背景，病理生理状态和药物相互作用对参与药物处置的转运蛋白功能的影响。影像学具有研究人类工作转运蛋白的巨大潜力，影像学将成为重要的工具，不仅在药物开发中，而且在医学中。影像学可以研究转运蛋白的力学方面，并阐明遗传背景，病理生理状态和药物相互作用对参与药物处置的转运蛋白功能的影响。影像学具有研究人类工作转运蛋白的巨大潜力，影像学将成为重要的工具，不仅在药物开发中，而且在医学中。影像学可以研究转运蛋白的力学方面，并阐明遗传背景，病理生理状态和药物相互作用对参与药物处置的转运蛋白功能的影响。