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首页> 外文期刊>Journal of applied toxicology >Low-dose probenecid selectively inhibits urinary excretion of phenolsulfonphthalein in rats without affecting biliary excretion
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Low-dose probenecid selectively inhibits urinary excretion of phenolsulfonphthalein in rats without affecting biliary excretion

机译：小剂量丙磺舒选择性抑制大鼠苯酚磺酞的排泄而不影响胆汁排泄

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摘要

Renal organic anion transport systems play an important role in the excretion of anionic drugs and toxic compounds. Probenecid has been used as a potent inhibitor of urinary and biliary excretion of anionic compounds mediated by transporters such as organic anion transporters and multidrug resistance-associated protein 2 (Mrp2). The purpose of this study was to optimize the dose of probenecid required for selective inhibition of urinary excretion of anionic compounds in rats, without inhibition of biliary excretion. Phenolsulfonphthalein (PSP), a model anionic compound that is excreted in urine and bile, was intravenously administered to rats after intraperitoneal injection of different doses of probenecid (0, 0.2, 2, 10, 100, 200 and 400mgkg-1). Treatment with 100, 200 or 400mgkg-1 probenecid decreased both renal clearance (CLr) and biliary clearance (CLb) of PSP, whereas 0.2mgkg-1 probenecid did not have any effect. Probenecid administered at doses of 2 and 10mgkg-1 decreased only CLr. The median effective doses of probenecid for inhibiting CLr and CLb were 0.925 and 23.9mgkg-1, respectively. These data suggest that a low dose of probenecid selectively inhibits urinary excretion of PSP that may be mediated by organic anion transporters, without affecting biliary excretion that may be mediated by Mrp2.
机译：肾脏有机阴离子转运系统在阴离子药物和有毒化合物的排泄中起着重要作用。丙磺舒已被用作由转运蛋白如有机阴离子转运蛋白和多药耐药相关蛋白2（Mrp2）介导的阴离子化合物的尿和胆汁排泄的有效抑制剂。这项研究的目的是优化选择性抑制大鼠中阴离子化合物的尿排泄而不抑制胆汁排泄所需的丙磺舒的剂量。腹膜内注射不同剂量的丙磺舒（0、0.2、2、10、100、200和400mgkg-1）后，向大鼠静脉内施用苯酚磺酞（PSP），一种在尿液和胆汁中排泄的阴离子模型化合物。用100、200或400mgkg-1丙磺舒治疗可降低PSP的肾脏清除率（CLr）和胆汁清除率（CLb），而0.2mgkg-1丙磺舒则无任何作用。丙磺舒以2和10mgkg-1的剂量给药只能降低CLr。丙磺舒抑制CLr和CLb的中位有效剂量分别为0.925和23.9mgkg-1。这些数据表明，低剂量的丙磺舒可选择性抑制可能由有机阴离子转运蛋白介导的PSP尿排泄，而不影响可能由Mrp2介导的胆汁排泄。

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