Abstract
Forty-eight hours after a single dose of 14C-imipramine to rats, 14C-radioactivity could be measured in the following organs: liver > kidney > serum > fat > spleen > duodenum > lung > muscle and brain. Liver microsomes contained the main part of radioactivity derived from 14C-imipramine.
After exhaustive extraction, only the proteins of liver, kidney, spleen, lung and serum contained measurable amounts of radioactive labeling. The greatest amount of 14C-imipramine irreversibly bound to proteins was detected in liver microsomes.
The question, as to whether the irreversible protein binding of imipramine, if it occurs during therapy, results in toxic side-effects, is discussed.
Zusammenfassung
Achtundvierzig Stunden nach einer einzelnen Gabe von 14C-Imipramin an Ratten konnte 14C-Radioaktivität in folgenden Organen gemessen werden: Leber > Niere > Serum > Fett > Milz > Dünndarm > Lunge > Muskel und Gehirn. Die Lebermikrosomen enthielten den größten Anteil an Imipramin-Radioaktivität.
Nach erschöpfender Extraktion enthielten nur die Proteine von Leber, Niere, Milz, Lunge und Serum meßbare Mengen radioaktiver Markierung. Die größte Menge 14C-Imipramin, welches irreversibel an Proteine gebunden war, wurde in Lebermikrosomen gefunden.
Die Frage, ob die irreversible Bindung von Imipramin an Proteine zu toxischen Nebenwirkungen führt, wenn sie während der Therapie auftritt, wird diskutiert.
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Kappus, H. Irreversible protein binding of 14C-imipramine in rats in vivo. Arch. Toxicol. 37, 75–80 (1976). https://doi.org/10.1007/BF00353357
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DOI: https://doi.org/10.1007/BF00353357