Johnston P A, Kau S T
Department of Pharmacology, A Business Unit of ICI Americas Inc., Wilmington, DE.
Methods Find Exp Clin Pharmacol. 1992 Sep;14(7):523-9.
Increases in the delivery of solute to the loop of Henle result in increased reabsorption, vasoconstriction of the afferent arteriole, and a reduction in the glomerular filtration. Although the details of this tubuloglomerular feedback (TGF) mechanism are not completely worked out, it appears certain that alterations in reabsorption by the loop of Henle are critical to its operation. In the following study, we assessed the effect of several different loop of Henle diuretics on the response of the TGF mechanism. The function of TGF was monitored by measuring the stop-flow pressure (SFP) in the early proximal tubule in response to alterations in perfusion rate through the loop of Henle. All drugs were given directly into the loop of Henle in a concentration of 10(-4) M. With control solutions, SFP fell in a sigmoidal fashion over a perfusion range of 5 to 45 nl/min. When furosemide was added to the perfusate at a dose of 10(-4) M, SFP did not change. Bumetanide had an effect similar to furosemide, but muzolimine failed to inhibit the reduction in SFP over the perfusion range. Three experimental compounds were tested. All three cause diuresis when administered orally to animals. MK447 had no effect on SFP, but its metabolite, MK447-SO4, had an effect similar to furosemide. Another compound with modest diuretic effects, ICI 207,828, actually increased the response in SFP. Two distal diuretics, hydrochlorothiazide and amiloride, had no effect on SFP. The response of SFP to all these compounds correlated with its measured effect on loop reabsorption of sodium. Furosemide, bumetanide and MK447-SO4 significantly reduced sodium reabsorption.(ABSTRACT TRUNCATED AT 250 WORDS)
溶质输送至髓袢增加会导致重吸收增加、入球小动脉血管收缩以及肾小球滤过率降低。尽管这种管球反馈(TGF)机制的细节尚未完全阐明,但髓袢重吸收的改变对其运作至关重要这一点似乎是确定的。在以下研究中,我们评估了几种不同的髓袢利尿剂对TGF机制反应的影响。通过测量近端小管起始段的停流压力(SFP)来监测TGF的功能,以应对髓袢灌注速率的改变。所有药物均以10⁻⁴ M的浓度直接注入髓袢。使用对照溶液时,在5至45 nl/min的灌注范围内,SFP呈S形下降。当以10⁻⁴ M的剂量将呋塞米添加到灌注液中时,SFP没有变化。布美他尼的作用与呋塞米相似,但莫唑胺未能抑制灌注范围内SFP的降低。测试了三种实验性化合物。这三种化合物口服给动物时均会引起利尿。MK447对SFP没有影响,但其代谢产物MK447-SO4的作用与呋塞米相似。另一种具有适度利尿作用的化合物ICI 207,828实际上增加了SFP的反应。两种远端利尿剂氢氯噻嗪和阿米洛利对SFP没有影响。SFP对所有这些化合物的反应与其对髓袢钠重吸收的测量效应相关。呋塞米、布美他尼和MK447-SO4显著降低了钠重吸收。(摘要截取自250字)