The mode of action of bumetanide: inhibition of chloride transport across the amphibian cornea.
The mode of action of bumetanide: inhibition of chloride transport across the amphibian cornea.
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布美他尼的作用方式：抑制氯离子穿过两栖动物角膜的转运。
DOI：
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发表时间：
1977
影响因子：
3.5
通讯作者：
P. Bentley
中科院分区：
文献类型：
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作者：
M. Mcgahan;T. Yorio;P. Bentley
利尿剂布美他尼(10(-7M))在体外可降低两栖动物角膜的跨壁电位差和短路电流。这一效应反映了CI的外流(内皮到上皮，或撕裂侧)的减少，这是其主动运输的方向。在涌入的过程中没有任何变化。这种作用在10(-4)M时是缓慢可逆的，当药物作用于内皮细胞时，其作用约为上皮侧的两倍。速尿对CI转运的影响相似，但两种药物的量效曲线并不平行。速尿的效力大约是布美他尼的60到200倍。当药物作用于内皮细胞时，速尿的效果大约是放置在上皮侧时的五倍。硫氰酸盐(2×10(-2)M)也能抑制活性CI的跨角膜转运，但对膜两侧的作用相同。布美他尼对体外培养的蟾蜍晶状体和蛙皮的被动CI运动无影响。皮肤的反应与速尿和硫氰酸盐不同。布美他尼对CI转运的影响可能与其在肾小管的利尿作用机制有关。
The diuretic drug bumetanide (10(-7 M) reduced the transmural potential difference and short-circuit current across the amphibian cornea in vitro. This effect reflected a decline in the outflux (endothelial to epithelial, or tear, side) of CI, which is the direction of its active transport. There was no change in the influx. The effect was slowly reversible at 10(-4) M and was about two times as great when the drug was on the endothelial as compared to the epithelial side. Furosemide had a similar effect on CI transport, but the dose-response curves of the two drugs were not parallel. Furosemide was about 60 to 200 times less potent than bumetanide. The effect of furosemide was about five times as great when the drug was on the endothelial rather than when it was placed on the epithelial side. Thiocyanate (2 x 10(-2) M) also inhibited the active CI transport across the cornea, but it was equally effective on either side of the membrane. Bumetanide had no effect on the passive CI movements across the toad lens or frog skin in vitro. The response of the skin differs from that of furosemide and thiocyanate. These observations of the effects of bumetanide on CI transport may be relevant to the mechanism of its diuretic actions in the kidney tubule.