METABOLIC STUDIES WITH DI(AZIRIDIN‐I‐YL) SULPHOXIDE (DIETHYLENEIMINOSULPHOXIDE)

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Abstract
The work described was undertaken after the observation that the diuresis induced by several derivatives of ethyleneimine could be correlated with their content of ethyleneimine. The preparation of 35S-labelled di(aziridin-1-yl) sulphoxide (diethyl-eneiminosulphoxide) is described together with its metabolism in rat, mouse, rabbit and dog. The drug was completely metabolized in all species and, with the exception of the dog, most of the activity was excreted in the urine within 3 days. The main radioactive metabolite in all species was sulphate. In vitro studies demonstrated that the compound was slowly broken down to sulphite and free ethyleneimine; this hydrolysis was greatly accelerated in the presence of phosphate.

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