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为了排泄外源性物质和体内代谢产物,人体的肝脏、肾脏和肠道上广泛分布有各种转运体。其中有机阳离子转运体(organic cation transporters,OCTs)介导了一些药物、毒物和内源性化合物等一系列有机阳离子的转运。OCTs家族的第一成员OCT1在许多外源性药物的吸收、分布和排泄中发挥着重要的作用。OCT1存在许多基因多态性,有些多态性与其转运活性密切相关。此外,OCT1的转运活性可以被蛋白激酶C(protein kinase C,PKC)和蛋白激酶A(protein kinase A,PKA)所增强,这样介导了许多底物药物之间以及底物药物和PKC,PKA激活剂或抑制剂之间的相互作用。本文就OCT1的生理和遗传药理作用进行了综述。
In order to excrete exogenous substances and metabolites in the body, the body’s liver, kidney and intestinal distribution of a wide range of transporters. Among them, organic cation transporters (OCTs) mediate the transport of a series of organic cations such as drugs, poisons and endogenous compounds. OCT1, the first member of the OCTs family, plays an important role in the absorption, distribution and excretion of many exogenous drugs. There are many gene polymorphisms in OCT1, some of which are closely related to its transport activity. In addition, the transporter activity of OCT1 can be enhanced by protein kinase C (PKC) and protein kinase A (PKA), which mediates the interaction between many substrate drugs and substrate drugs and PKC, PKA Activator or Inhibitor Interactions. This article reviews the physiological and genetic pharmacological effects of OCT1.