Harders H, Armah B, Cohnen E, Führ J, Heinz N, Schröder H F
Arzneimittelforschung. 1980;30(2):254-8.
The cupriuretic effectivity of tetradentate chelating agents was measured in rats and compared with that of D-penicillamine. The applied chelators are aliphatic and alicyclic tetramines and tetramine-analogous substances with two nitrogen-atoms substituted by oxygen. Urine copper excretion was measured during 24 h (and 6 and the following 18 h, respectively) after single and repeated doses over a period of 5 days. The aliphatic tetramines, triethylenetetramine (TETA, TRIEN) and BE 6184, were the most active substances. Simultaneous application of TETA and D-penicillamine does not induce a summation or potentiation of the copper elimination. After s.c. application TETA seems to be three times more effective than orally. The potency of aliphatic and alicyclic tetramines is discussed on the basis of in vitro data.
在大鼠中测定了四齿螯合剂的促排铜效果,并与D-青霉胺进行了比较。所应用的螯合剂是脂肪族和脂环族四胺以及两个氮原子被氧取代的四胺类似物。在单次和重复给药5天后的24小时内(分别为6小时及随后的18小时)测量尿铜排泄量。脂肪族四胺,三亚乙基四胺(TETA,TRIEN)和BE 6184是最具活性的物质。同时应用TETA和D-青霉胺不会引起铜排泄的累加或增强作用。皮下注射后,TETA的效果似乎比口服高三倍。基于体外数据讨论了脂肪族和脂环族四胺的效力。