Untersuchungen zum Stoffwechsel von Tropan-Alkaloiden, VIII. Chemische Analyse des Stoffwechsels von (—)-Scopolamin bei einigen Säugetieren

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Abstract
Using three differently labelled samples of (-)-scopolamine (9-14C; 9-C3H3; U-3H), the metabolism of this alkaloid was studied in the mouse, rat, guinea pig and common marmoset. The following metabolites were identified chemically in the urine of the mouse, following the administration of ([long dash])-scopolamine: ([long dash])-scopolamine-9[image]-glucuronide, (-)-norscopolamine-9[image]-glucuronide, aposcopolamine, 6-hydroxy-([long dash])-hyoscyamine, scopine, ([long dash])-norscopolamine, and unchanged ([long dash])-scopolamine. After the injection of [9-14C]scopolamine, 23% of the radioactivity of the N-methyl group was expired as 14CO2 by the mouse, 5.9% by the rat, 12.5% by the guinea pig, and 4.5% by the monkey. Also after the injection of ([long dash])-scopolamine-9[image]-glucuronide into the mouse, this derivative was metabolised to the nor-compound, and 14CO2 was found in the expired air. During passage through the body, there was no racemisation of scopolamine or any of its optically active metabolites. The concentrations of scopolamine metabolites were determined in body fluids and organs and their distribution was characteristic. To determine the metabolic pathway, the metabolites of scopolamine were isolated from the urine and their metabolism studied after reinjection. Variations in the dose of ([long dash])-scopolamine (10[long dash]1000 [mu]g/mouse) caused hardly any differences in the relationship of metabolites.

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