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对乙酰氨基酚及其共轭物在犬肾小管中的转运

Renal tubular transport of paracetamol and its conjugates in the dog.

作者信息

Duggin G G, Mudge G H

出版信息

Br J Pharmacol. 1975 Jul;54(3):359-66. doi: 10.1111/j.1476-5381.1975.tb07576.x.

Abstract

1 The renal tubular transport of paracetamol and its conjugates was investigated with renal clearance and stop flow studies in the dog. Paracetamol is sparingly bound to plasma proteins and therefore undergoes glomerular filtration. It is reabosrbed in the renal tubules by simple diffusion. 2 The conjugates of paracetamol, the sulphate and the glucuronide, both undergo glomerular filtration being weakly protein bound. At low concentrations in plasma both compounds are secreted by an active transport process. At higher concentrations both compounds are reabsorbed. Clearances are not dependent on urinary pH or flow rate. It is concluded that reabsorption is not a passive process but that there is an active bidirectional transport of the conjugates. 3 Net tubular secretion of the sulphate, but not the glucuronide, conjugate was inhibited by the administration of probenecid.

摘要
  1. 采用肾脏清除率和停流实验,在犬身上研究了对乙酰氨基酚及其结合物的肾小管转运情况。对乙酰氨基酚与血浆蛋白结合较少,因此可经肾小球滤过。它通过简单扩散在肾小管中被重吸收。2. 对乙酰氨基酚的结合物,即硫酸盐和葡萄糖醛酸结合物,均经肾小球滤过,与蛋白结合较弱。在血浆中低浓度时,这两种化合物均通过主动转运过程分泌。在较高浓度时,这两种化合物均被重吸收。清除率不依赖于尿液pH值或流速。得出的结论是,重吸收不是一个被动过程,而是结合物存在主动双向转运。3. 丙磺舒的给药抑制了硫酸盐结合物(而非葡萄糖醛酸结合物)的肾小管净分泌。

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本文引用的文献

1
Necrosis of the renal papillae and prolonged abuse of phenacetin.肾乳头坏死与长期滥用非那西丁。
Acta Med Scand. 1959 Dec 5;165:321-8. doi: 10.1111/j.0954-6820.1959.tb14507.x.
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[Studies on the oxidative metabolism of phenacetin in rats].
Biochem Pharmacol. 1967 Dec;16(12):2247-56. doi: 10.1016/0006-2952(67)90212-2.
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Renal excretion of uric acid in the dog.狗体内尿酸的肾脏排泄。
Am J Physiol. 1968 Aug;215(2):404-10. doi: 10.1152/ajplegacy.1968.215.2.404.

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