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氨苯蝶啶对上皮细胞中Na⁺与K⁺及H⁺交换的抑制作用(作者译)

[Inhibition of the exchange of Na+ for K+ and and H+ by triamterene (in epithelia)(author's transl)].

作者信息

Knauf H, Wais U, Albiez G, Lübcke R

出版信息

Arzneimittelforschung. 1976 Apr;26(4):484-6.

PMID:133688
Abstract

The salivary duct epithelium, which actively transports Na+, K+ and H+/HCO3/- similarly to renal distal tubules, was used as a model tissue to study the mechanism of action of triamterene (Jatropus, Dyrenium) on electrolyte transport. Triamterene was only effective when administered from the luminal side of the duct, not from the interstitial side. 10-4 M triamterene completely blocked Na+-reabsorption. At the same time K+ secretion dropped to half of control, whereas HCO-/3 accumulated in the duct lumen following reduced H+ secretion. These changes in electrolyte transport are caused by an inhibition of Na+-entry by triamterene as suggested by measurements of ion permeability of the cell membrane. Triamterene has no specific effect on the membrane-bound ATPase. Since Na+-entry is functionally coupled with exit of K+ and H+ from cell to lumen, impairment of Na+-entry by triamterene necessarily causes reduction of K+ and H+ secretion into lumen.

摘要

唾液腺导管上皮细胞与肾远曲小管类似,能主动转运Na+、K+和H+/HCO3-,被用作研究氨苯蝶啶(商品名:Jatropus、Dyrenium)对电解质转运作用机制的模型组织。氨苯蝶啶只有从导管腔侧给药才有效,从间质侧给药则无效。10-4 M氨苯蝶啶能完全阻断Na+重吸收。与此同时,K+分泌降至对照的一半,而随着H+分泌减少,HCO3-在导管腔内蓄积。如细胞膜离子通透性测量结果所示,电解质转运的这些变化是由氨苯蝶啶抑制Na+内流引起的。氨苯蝶啶对膜结合ATP酶无特异性作用。由于Na+内流在功能上与K+和H+从细胞向管腔的外流相偶联,氨苯蝶啶对Na+内流的损害必然导致K+和H+向管腔分泌减少。

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