AI Article Synopsis
- CERM 3517, an antiemetic, was given to Beagle dogs to identify its major metabolite, which was found to have the same structure as a synthesized compound (CERM 4082).
- The metabolite was produced through the cleavage of the aromatic part of CERM 3517.
- After intravenous administration, 13% and 56% of doses of CERM 3517 and CERM 4082 were eliminated in urine as CERM 4082, indicating at least 25% of CERM 3517 was transformed via N-dephenylation.
Article Abstract
CERM 3517 (mociprazine), a new antiemetic compound, was administered orally at 10 mg/kg twice a day for 4 days to six Beagle dogs in order to identify the major metabolite. Mass spectrometric comparison of this metabolite and a synthesized reference compound (CERM 4082) showed that both had identical structures. The metabolite originated from cleavage of the aromatic moiety. After iv administration of CERM 3517 (0.9 mg/kg) and CERM 4082 (0.6 mg/kg) to five beagle dogs, 13% and 56% of the dose, respectively, were eliminated in the urine as CERM 4082 compound. It can be calculated that at least 25% of CERM 3517 was biotransformed by N-dephenylation.
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N-dephenylated and N-phenyl urinary metabolites of mociprazine (CERM 3517) in beagle dogs after oral administration. A mass spectrometric determination.
Eur J Drug Metab Pharmacokinet
November 1991
Groupe de Recherches en Biodynamique du médicament, Laboratoire de Chimie analytique, Clermont-Ferrand, France.
CERM 3517 (mociprazine), a new anti-emetic compound, was administered orally to six beagle dogs at 10 mg/kg b.i.d.
View Article and Find Full Text PDFArticle Synopsis
- CERM 3517, an antiemetic, was given to Beagle dogs to identify its major metabolite, which was found to have the same structure as a synthesized compound (CERM 4082).
- The metabolite was produced through the cleavage of the aromatic part of CERM 3517.
- After intravenous administration, 13% and 56% of doses of CERM 3517 and CERM 4082 were eliminated in urine as CERM 4082, indicating at least 25% of CERM 3517 was transformed via N-dephenylation.
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