Knorr A, Garthoff B
Arch Int Pharmacodyn Ther. 1985 Nov;278(1):150-6.
The rank order of diuretic efficacy of furosemide analogs, e.g. bumetanide and piretanide, in humans is reflected better by their ability to inhibit Na+, K+-cotransport in human red blood cells than by their natriuretic activity in rats. High ceiling diuretics which are structurally unrelated to sulfamoyl diuretics, e.g. muzolimine, tizolemide, MK 447, may be similarly effective in rat and man, but by acting via other mechanisms cannot be detected by use of the Na+, K+-cotransport system. On the other hand, a possible conversion of such compounds to metabolites active in the cotransport system cannot be ruled out. In contrast to ethacrynic acid, the weak inhibitory activity of muzolimine on the Na+, K+-cotransport was not potentiated by cysteine. These results suggest that the diuretic activity of muzolimine is not caused by inhibition of Na+, K+-cotransport.
呋塞米类似物（如布美他尼和吡咯他尼）在人体内的利尿效力排序，通过其抑制人红细胞中Na⁺、K⁺协同转运的能力来反映，比通过它们在大鼠中的利钠活性反映得更好。与磺胺酰脲类利尿剂结构无关的高效能利尿剂，如莫唑胺、替唑胺、MK 447，在大鼠和人类中可能同样有效，但通过其他机制起作用，无法通过Na⁺、K⁺协同转运系统检测到。另一方面，不能排除此类化合物转化为在协同转运系统中具有活性的代谢产物的可能性。与依他尼酸不同，莫唑胺对Na⁺、K⁺协同转运的微弱抑制活性不会被半胱氨酸增强。这些结果表明，莫唑胺的利尿活性不是由抑制Na⁺、K⁺协同转运引起的。
