## Abstract Three healthy male subjects received single 100mg oral doses of carprofen containing 20 ΞΌCi of ^14^Cβcarprofen. Venous blood samples were drawn during the first 48 h after the dose and urine and feces were collected for 120h. Concentrations of carprofen and its metabolites in body fluid
Metabolism of DL-[14C]prenylamine in man
β Scribed by G. Remberg; M. Eichelbaum; G. Spiteller; H. J. Dengler
- Publisher
- John Wiley and Sons
- Year
- 1977
- Tongue
- English
- Weight
- 801 KB
- Volume
- 4
- Category
- Article
- ISSN
- 1076-5174
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β¦ Synopsis
Following oral administration of DL-[14C]prenylamine, about 40% of the dose administered was excreted in urine within 10 days. Less than 0.1% of the dose was excreted as unchanged prenylamine. The drug was extensively metabolized to at least 20 to 25 metabolites. The structure of 12 metabolites could be elucidated by means of g.c.m.s. Ring hydroxylation and further methylation of the phenolic metabolites are the main metabolic pathways involved. A substantial part of the drug and/or its metabolites is metabolized via cleavage of the C--N--C bond, giving rise to amphetamine and diphenylpropylamine which are further metabolized by aromatic and sidechain hydroxylation.
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A new method of synthesis of DL-[ 7-14C]indospicine and DL-2-amino-[ 7-1 4C]pimelic acid and their nonradioactive equivalents is reported. The combined radiochemical yield of both compounds, starting from potassium 1 14C]cyanide was 15.3%. Indospicine was isolated as the flavianate.
The disposition of the enantiomers of oxaprotiline has been investigated after single 100 mg oral doses of racemic 14C-labelled oxaprotiline.HC1 in two healthy subjects. Absorption was complete. Peak blood concentrations of total I4C were 804 and 1010ngequiv.g-' after 4-6 h in the two subjects. Afte
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