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C Zell

Publications and source records attributed to C Zell.

4 recordsLinked to original sources
PubMed1994

Pharmacokinetics of the organic nitrates trans-N-(4-nitroxycyclohexyl)-urea in dogs and trans-N-(4-nitroxycyclohexyl)-acetamide in dogs and in man.

The pharmacokinetic behavior of the organic nitrates BM 12.1247 (trans-N-(4-nitroxycyclohexyl)-urea) and BM 12.1307 (trans-N-(4-nitroxycyclohexyl)-acetamide, CAS 137291-91-3) were examined in beagle dogs after oral and intravenous administration. To this end, a reliable and specific assay using capillary gaschromatography with electron capture detection (GC-ECD) was developed. BM 12.1247 showed its maximum plasma level after 2.2 h by oral application; the bioavailability was nearly 100%. The elimination half-life of 8.8 h p.o. Corresponded to the half-life after i.v. administration, concerning BM 12.1307, the elimination half-lives were still longer, they reached 11-13 h and bioavailability reached 68-70%; these results were confirmed by crossover tests. In a first application of healthy volunteers it was possible to show that the organic nitrate BM 12.1307 is eliminated much more slowly in man than in dog, the half-life of the compound in man being longer than the half-life in dog by a factor of 2.3.

Acetamides↗
PubMed1994

Biotransformation of the organic nitrate trans-N-(4-nitroxycyclohexyl)acetamide in dogs.

The biotransformation of BM 12.1307 (trans-N-(4-nitroxycyclohexyl)acetamide, CAS 137291-91-3) in the dog was examined after oral and intravenous administration. For that purpose, the organic nitrate was synthesized as radioactive [14C]- and as [13C]-labeled compounds. The defined isotopic mixture was administered to the dogs. Within the examined period of 168 h, the elimination of BM 12.1307 and its metabolites via urine and feces amounted to 76.5% after oral application, and to 80.7% of the applied dose after intravenous application. The major amount of radioactivity was eliminated via urine (69.4% and 73.6% of the dose, respectively), whereas the fecal elimination was found to be negligible. Investigations of the urinary samples showed that the drug is metabolized to a high percentage trans-N-(4-Hydroxycyclohexyl) acetamide is the main metabolite; 73% of the radioactive compounds (after p.o.-administration and 69% after intravenous application could be identified as the alcohol of BM 12.1307; the amounts of the drug totalled 9% and 13%, respectively. The quantitative determination of BM 12.1307 in urine and plasma was performed by gas chromatography; the amount of the main metabolite excreted in urine was determined by high-pressure liquid chromatography. Trans-N-(4-hydroxycyclohexyl)-acetamide, N-(4-oxocyclohexyl)acetamide, and 3-acetamido-7-oxa-bicyclo [4.1.0]heptane were formed as metabolites. For the identification and characterization of the possible metabolic structures, these compounds were synthesized and used in comparison with the detected drugs.

Acetamides↗