《生命科学》 2018, 30(7): 790-797
摘 要:摘 要:有机阳离子转运体2 (organic cation transporter 2, OCT2) 是溶质转运体(solute carriers, SLC) 超家族中SLC22A 家族的重要成员之一。肾小管上皮细胞基底膜侧表达的OCT2 在维持机体内环境平衡方面起着重要作用,是肾脏主动分泌众多内、外源性有机阳离子型化合物( 包括环境毒素、药物以及内源性代谢产物等) 的主要转运体。在急性肾损伤(acute kidney injury, AKI) 期间,OCT2 功能与表达的改变对其底物的清除具有巨大的影响,可导致药物的药代动力学过程发生改变,从而影响药物的安全性和有效性。现就OCT2 的结构与分布、生理作用与调控机制以及在各种因素诱导的AKI 中的功能与表达变化和病理生理调控等方面进行综述,旨在为临床合理用药提供参考。
Abstract: Abstract: Orangic cation transporter 2 (OCT2) is an important member of superfamily of solute carriers 22A (SLC22A). As a major transporter involved in both endogenous and exogenous active secretion in the basolateral of renal tubular epithelial, OCT2 can transport drugs, toxins and endogenous by-products in kidney, and therefore,plays an important role in maintaining the homeostasis of internal environment. Under the circumstance of acute kidney injury (AKI), the functional and expressional variations of renal OCT2 have a huge impact on systemicclearance of substrate drugs, thereby affecting the safety and efficacy of the drug. This review highlights the structure and distribution of OCT2, its physiological effects and regulation mechanism, as well as its function and expression changes and pathophysiological regulation in a variety of factors inducing AKI, aiming to provide theoretical basis for the rational use of drugs.