Priewer H, Kraft H, Mutschler E
Arzneimittelforschung. 1986 Feb;36(2):213-5.
The diuretic, natriuretic and antikaliuretic properties of several straight-chain and branched-chain acidic triamterene derivatives were investigated in male Wistar rats. Among the straight-chain compounds the ether of hydroxytriamterene with five C atoms in the side chain (S3) revealed the maximum effects. The iso-compounds (derivatives of 4-carboxymethoxy triamterene S1) showed much better water solubility than the n-acids, but they increased the natriuresis only slightly and had no effect on kaliuresis when they were injected intravenously alone; whereas the isocompound Si4 showed potassium retaining properties when it was administered together with furosemide. From these results it can be suggested that the negative charge in the side chain has to be in a distinct distance from the pteridine ring to produce antikaliuretic effects.
在雄性Wistar大鼠中研究了几种直链和支链酸性氨苯蝶啶衍生物的利尿、利钠和抗利尿钾特性。在直链化合物中，侧链含有5个碳原子的羟基氨苯蝶啶醚（S3）显示出最大效果。异化合物（4-羧基甲氧基氨苯蝶啶S1的衍生物）的水溶性比正酸好得多，但单独静脉注射时，它们仅轻微增加利钠作用，对尿钾排泄没有影响；而异化合物Si4与呋塞米一起给药时显示出保钾特性。从这些结果可以推测，侧链中的负电荷必须与蝶啶环保持一定距离才能产生抗利尿钾作用。
