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首页> 外文期刊>Nuclear Medicine and Biology >Drugs interacting with organic anion transporter-1 affect uptake of Tc-99m-mercaptoacetyl-triglycine (MAG3) in the human kidney: Therapeutic drug interaction in Tc-99m-MAG3 diagnosis of renal function and possible application of Tc-99m-MAG3 for drug development
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Drugs interacting with organic anion transporter-1 affect uptake of Tc-99m-mercaptoacetyl-triglycine (MAG3) in the human kidney: Therapeutic drug interaction in Tc-99m-MAG3 diagnosis of renal function and possible application of Tc-99m-MAG3 for drug development

机译：与有机阴离子转运蛋白1相互作用的药物会影响人肾脏中Tc-99m-巯基乙酰基-三甘氨酸（MAG3）的摄取：Tc-99m-MAG3中的治疗药物相互作用对肾功能的诊断以及Tc-99m-MAG3可能在药物中的应用发展

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Introduction: Renal uptake of Tc-99m-MG3 involves organic anion transporter (OAT). Treatment with drugs showing OAT affinity might interfere with renal uptake of Tc-99m-MAG3, leading to misinterpretation in Tc-99m-MAG3. This study was conducted to discuss a possible drug interference with Tc-99m-MAG3 diagnosis on OAT sites. Methods: Renal uptake and plasma clearance of Tc-99m-MAG3 were analyzed in healthy volunteers under control and OAT1 and OAT3 related drug treatment conditions. An in vitro uptake study using OAT1 or OAT3 expressing cells was also conducted. Results: Both PAH and probenecid treatment induced delays in Tc-99m-MAG3 clearance from blood, and reductions in the renal uptake clearance. As a result, the normalized effective renal plasma flow estimated from Tc-99m-MAG3 clearance was significantly underestimated, whereas the glomerular filtration rate estimated from plasma creatinine levels was unchanged. The transport activity of Tc-99m-MAG3 was higher in OAT1-expressing cells than in OAT3-expressing cells. Conclusion: Drugs with OAT1 affinity affect the renal uptake of Tc-99m-MAG3 and blood clearance. This might cause misinterpretation of functional diagnosis of the kidney using Tc-99m-MAG3.
机译：简介：Tc-99m-MG3的肾脏摄取涉及有机阴离子转运蛋白（OAT）。用显示OAT亲和力的药物治疗可能会干扰肾脏对Tc-99m-MAG3的摄取，从而导致Tc-99m-MAG3的误解。进行这项研究的目的是讨论可能的药物干扰OAT部位的Tc-99m-MAG3诊断。方法：在健康志愿者中，在对照以及OAT1，OAT3相关药物治疗条件下，分析Tc-99m-MAG3的肾脏摄取和血浆清除率。还进行了使用OAT1或OAT3表达细胞的体外摄取研究。结果：PAH和丙磺舒治疗均会导致Tc-99m-MAG3从血液清除的延迟，以及肾脏摄取清除的减少。结果，从Tc-99m-MAG3清除率估计的标准化有效肾血浆流量被大大低估了，而从血浆肌酐水平估计的肾小球滤过率却没有改变。 Tc-99m-MAG3在OAT1表达细胞中的转运活性高于OAT3表达细胞。结论：具有OAT1亲和力的药物会影响Tc-99m-MAG3的肾脏摄取和血液清除。这可能会导致使用Tc-99m-MAG3对肾脏功能诊断的误解。

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