阿米洛利对膜ATP酶的非特异性抑制作用：与哇巴因的体内外比较研究

Non-specific inhibition of membrane-ATPase by amiloride: a comparative in vivo and in vitro study with ouabain.

作者信息

Knauf H, Simon B, Wais U

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1976;292(2):189-92. doi: 10.1007/BF00498591.

Abstract

The submaxillary duct epithelium, which actively transports Na+ (rabbit) and, in addition, K+ and H+/HCO-/3 (rat), was used as a model epithelium to compare the effects of ouabain and amiloride on transport parameters. 1. Ouabain was only effective from the interstitial side, amiloride, however, only from the luminal side. Amiloride induced effects on transport of the ions were seen within less than 1 s, ouabain effects, however, only after minutes. 2. Ouabain inhibited in a parallel fashion the Na+ transport potential and the Na+-K+-ATPase activity. It had no effect on the Mg2+-ATPase and the HCO-/3-ATPase. 3. Amiloride also inhibited the Na+ transport potential and the Na+-K+-ATPase; however, the Na+ transport potential was significantly more sensitive to amiloride than the Na+-K+-ATPase. 4. Amiloride inhibited in a similar fashion the Na+-K+-ATPase, the Mg2+-ATPase and the HCO-/3-ATPase, but did not influence active HCO-/3 secretion. 5. It is concluded that the amiloride induced effects on the membrane ATPases are non-specific.

摘要

颌下腺导管上皮细胞可主动转运Na⁺（兔），此外还可转运K⁺和H⁺/HCO₃⁻（大鼠），以此作为模型上皮细胞来比较哇巴因和氨氯吡咪对转运参数的影响。1. 哇巴因仅从间质侧起作用，而氨氯吡咪仅从管腔侧起作用。氨氯吡咪对离子转运的影响在不到1秒内即可显现，而哇巴因的作用则需数分钟后才出现。2. 哇巴因以平行方式抑制Na⁺转运电位和Na⁺-K⁺-ATP酶活性。它对Mg²⁺-ATP酶和HCO₃⁻-ATP酶无影响。3. 氨氯吡咪也抑制Na⁺转运电位和Na⁺-K⁺-ATP酶；然而，Na⁺转运电位对氨氯吡咪的敏感性明显高于Na⁺-K⁺-ATP酶。4. 氨氯吡咪以类似方式抑制Na⁺-K⁺-ATP酶、Mg²⁺-ATP酶和HCO₃⁻-ATP酶，但不影响HCO₃⁻的主动分泌。5. 得出结论：氨氯吡咪对膜ATP酶的诱导作用是非特异性的。