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首页> 外文期刊>Clinical and experimental pharmacology & physiology >Effect of organic cations on the renal tubular secretion of pseudoephedrine in the rat.
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Effect of organic cations on the renal tubular secretion of pseudoephedrine in the rat.

机译：有机阳离子对大鼠伪麻黄碱肾小管分泌的影响。

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1. Pseudoephedrine is a weak organic base that undergoes renal tubular secretion. The aim of the present study was to assess whether two other commonly used weak organic bases (cimetidine and morphine) inhibit the renal tubular secretion of pseudoephedrine in the rat isolated perfused kidney. 2. A total of 12 perfusions were performed with four perfusions in each of three treatment groups. In the control group, pseudoephedrine was administered as a bolus dose of [14C]-pseudoephedrine and unlabelled pseudoephedrine to achieve an initial perfusate concentration of 0.4 microg/mL. For the treatment groups, pseudoephedrine was administered as above and cimetidine or morphine was added to the perfusion medium in increasing concentrations of 0.5-12.5 and 0.2-5.0 microg/mL, respectively. 3. The mean (+/-SD) fraction unbound of pseudoephedrine alone in perfusate was 0.866+/-0.014 and was not different (P> 0.05) in the presence of cimetidine or morphine. 4. In control experiments, the renal excretory clearance (CLR) of pseudoephedrine was three-fold greater than glomerular filtration rate (GFR), yielding a ratio consistently greater than unity, which indicates extensive net tubular secretion of pseudoephedrine. The CLR and total clearance of pseudoephedrine were similar, suggesting an absence of renal metabolism of pseudoephedrine. 5. The CLR/GFR ratio for pseudoephedrine was not affected by morphine, but was significantly reduced (P < 0.05) in the presence of cimetidine. 6. The results indicate that cimetidine inhibits the renal tubular secretion of pseudoephedrine.
机译：伪麻黄碱是一种弱有机碱，会经历肾小管分泌。本研究的目的是评估另外两种常用的弱有机碱（西咪替丁和吗啡）是否能抑制大鼠离体灌注肾脏中伪麻黄碱的肾小管分泌。 2.在三个治疗组中的每一个中进行总共12次灌注，其中4次灌注。在对照组中，伪麻黄碱以推注剂量的[14C]-伪麻黄碱和未标记伪麻黄碱的剂量给药，初始灌注液浓度为0.4微克/毫升。对于治疗组，按上述方式施用伪麻黄碱并将西咪替丁或吗啡分别以增加的浓度0.5-12.5和0.2-5.0 microg / mL添加到灌注培养基中。 3.单独的伪麻黄碱在灌流液中未结合的平均（+/- SD）分数为0.866 +/- 0.014，在存在西咪替丁或吗啡的情况下没有差异（P> 0.05）。 4.在对照实验中，伪麻黄碱的肾排泄清除率（CLR）是肾小球滤过率（GFR）的三倍，产生的比率始终大于一，表明伪麻黄碱有大量的净肾小管分泌。伪麻黄碱的CLR和总清除率相似，表明缺乏伪麻黄碱的肾脏代谢。 5.伪麻黄碱的CLR / GFR比值不受吗啡的影响，但是在存在西咪替丁的情况下，其明显降低（P <0.05）。 6.结果表明西咪替丁抑制伪麻黄碱的肾小管分泌。

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