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Synthese, Verteilung und Ausscheidung von 14C markiertem 2-Phenyl-3-methyl-tetrahydro-1,4-oxazin (Preludin)

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A radioactive preludin preparation, C14 labelled on the 2-carbon of the tetrahydrooxazine ring, was injected into mice in doses of 100 mg/kg s.c. and rats in doses of 10 mg/kg i.v. The radioactivity of the tissues and excreta was followed for 48 hours. An activity concentration surpassing the average body concentration was obtained for a short time in the lungs and for a longer time in kidneys, liver and in the wall of stomach and small intestine. 95–99% of the total activity is found in the urine. The kidney excretion is virtually finished at the end of 8 hours; 1–5% appear after the 8th hour in faeces. No radioactivity was obtained from the expired CO2. The main excretion organs are kidneys and liver; 3–6% of the injected dose is found in the contents of the stomach. The liver excretes more than 40% of the given dose via the bile into the small intestine, where the major portion is reabsorbed and after passing the enterohepatic circulation is eliminated by the kidneys. With larger doses the increase in the amount excreted by the liver is relatively greater than the increase in the amount excreted by the kidneys.

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Über einen Teil der Ergebnisse hat einer von uns (A. E.) auf der 23. Tagung der Deutschen Pharmakologischen Gesellschaft in Freiburg berichtet.

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Engelhardt, A., Jerchel, D., Weidmann, H. et al. Synthese, Verteilung und Ausscheidung von 14C markiertem 2-Phenyl-3-methyl-tetrahydro-1,4-oxazin (Preludin). Naunyn - Schmiedebergs Arch 235, 10–18 (1958). https://doi.org/10.1007/BF00246709

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