美吡拉敏敏感的、逆质子有机阳离子转运体的研究进展

Research progress of pyrilamine-sensitive H^+/OC antiporter

近年来,一种新型的有机阳离子转运体被发现存在于脑毛细血管内皮细胞和Caco-2(人克隆结肠腺癌细胞)等细胞上,介导美吡拉敏、苯海拉明和氧可酮等有机阳离子药物的吸收和外排。其所介导的转运过程不能被典型的有机阳离子转运体底物或抑制剂所抑制,转运特性不同于已报道的有机阳离子转运体(OCTs)、有机阳离子/肉毒碱转运体(OCTNs)、多药及毒性化合物外排转运体(MATE)及细胞膜单胺转运体(PMAT)等,是一种新型的逆质子有机阳离子转运体,被称为美吡拉敏敏感的、逆质子有机阳离子转运体(pyrilamine-sensitive H^+/OC antiporter)。本文将对其转运特性、底物结构特点、表达组织以及与其他有机阳离子转运体的区别等进行全面的归纳和阐述。

In recent years, a new type of organic cation transporter has been found to transport organic cation drugs like pyrilamine, diphenhydramine and oxycodone in brain capillary endothelial cells, Caco-2 cells and other cells. Its transport activity can not be inhibited by typical organic cation transporter substrates or inhibitors, and its transport characteristics are different from those reported for the organic cation transporters, such as organic cation transporters（OCTs）, organic cation/carnitine transporters（OCTNs）, multidrug and toxin extrusion transporters（MATE） and the plasma membrane monoamine transporter（PMAT）. It is a novel organic cation transporter, called pyrilamine-sensitive H~＋/OC antiporter. This review will present a comprehensive summary to elaborate the transport characteristics, structure of the substrates, tissue expression and the differences with other organic cation transporters.