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首页> 外文期刊>Research communications in molecular pathology and pharmacology >The inhibitory effect of diuretics on carbonic anhydrases.
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The inhibitory effect of diuretics on carbonic anhydrases.

机译：利尿剂对碳酸酐酶的抑制作用。

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摘要

A classification of diuretics mainly comprises mercurials; carbonic anhydrase inhibitors, thiazide diuretics, loop diuretics, inhibitors of renal epithelial Na+ channels and antagonists of mineralocorticoid receptors. We studied in this paper the relationship between diuretics and carbonic anhydrase (CA). Our in vitro and in vivo results show that all diuretics inhibit carbonic anhydrase II and renal CA IV. Further, our data show that they also inhibit epithelial cell CA in the renal tubules. The changes in intracellular pH (pHi) induced by these diuretics through CA inhibition would influence: a) the coupling to their receptors affecting information transmission to the epithelial cells of renal tubules as well as diuretic response; b) the decrease of Na+ exchanger (thiazide), of Na+ - K+ - 2Cl- relation (loop diuretics), Na+ channel blocking in distal and collecting tubules (amiloride, triamterene), as well as the antagonism between spironolactone and aldosterone at the mineralocorticoid receptor level, suggest that this competition might also be produced on CA II and on renal CA IV, which, in turn, could be influenced by pH-induced changes, the binding of the diuretic to its membrane receptor as well as the activity of the brush membrane or cytosolic pump. Furosemide and indapamide, diuretics known to have vasodilating effects, induce the fall of blood pressure that parallels the decrease of CA I activity. These results show the involvement of CA in the mechanism of action of the diuretics and in their actions associated with vasodilating effects. pH changes resulting from the action of CA contribute to the action of diuretics. All diuretics inhibit CA isozymes.
机译：利尿剂的分类主要包括汞。碳酸酐酶抑制剂，噻嗪类利尿剂，loop利尿剂，肾上皮Na +通道抑制剂和盐皮质激素受体拮抗剂。我们在本文中研究了利尿剂和碳酸酐酶（CA）之间的关系。我们的体外和体内结果表明，所有利尿剂均抑制碳酸酐酶II和肾CA IV。此外，我们的数据表明它们还抑制肾小管中的上皮细胞CA。这些利尿剂通过CA抑制作用诱导的细胞内pH（pHi）的变化将影响：a）与它们的受体的偶联，影响信息向肾小管上皮细胞的传递以及利尿反应。 b）Na +交换剂（噻嗪类），Na +-K + -2Cl-关系（利尿剂）减少，远端和收集小管（阿米洛利，氨苯蝶啶）的Na +通道阻滞以及螺内酯和醛固酮在盐皮质激素上的拮抗作用减少受体水平，表明这种竞争也可能在CA II和肾脏CA IV上产生，而这些竞争又可能受到pH诱导的变化，利尿剂与其膜受体的结合以及HIF活性的影响。刷膜或胞浆泵。速尿和吲达帕胺是已知具有血管舒张作用的利尿剂，可导致血压下降，与CA I活性下降同时发生。这些结果表明CA参与了利尿剂的作用机理及其与血管舒张作用有关的作用。由CA作用引起的pH值变化有助于利尿剂的作用。所有利尿剂均抑制CA同工酶。

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