N-Dephenylated and N-phenyl urinary metabolites of mociprazine (CERM 3517) in beagle dogs after oral administration. A mass spectrometric determination

@article{Enreille2010NDephenylatedAN,
  title={N-Dephenylated and N-phenyl urinary metabolites of mociprazine (CERM 3517) in beagle dogs after oral administration. A mass spectrometric determination},
  author={A Enreille and J. F. Pognat and M. J. Galmter and C. Larttgue-Mattei and Jean Louis Chabard and Norbert Busch and J. A. Berger},
  journal={European Journal of Drug Metabolism and Pharmacokinetics},
  year={2010},
  volume={16},
  pages={161-172}
}
SummaryCERM 3S17 (mociprazine), a new anti-emetic compound, was administered orally to six beagle dogs at 10 mg/kg b.i.d. for four days. Unconjugated urinary metabolites were identified by GC-MS analysis against synthesized reference compounds, after solvent extraction, purification by TLC and concentration. Twenty one metabolites were identified indicating the following biotransformations: N-dephenylation followed by reactions on the exposed secondary amine such as methylation and acetylation… 

References

SHOWING 1-10 OF 15 REFERENCES
Dephenylation of N-phenyl-2-naphthylamine in dogs and its possible oncogenic implications.
TLDR
Calculations based on Druckery and Küpfmüller's equation and present data indicate that, for dogs to form BNA tumours through exposure to a relatively high dose-level of PBNA, the period of daily dosing would occupy, or even exceed, the normal life-span.
N-dephenylation of CERM 3517 (mociprazine) in beagle dogs. A mass spectrometric determination.
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
Hepatic microsomal metabolism and macromolecular binding of the antioxidant, N-phenyl-2-naphthylamine.
TLDR
There was a time-dependent linear increase in covalent binding of P2NA to microsomal protein and the extent of binding approximately paralleled the rate of metabolism, and macromolecular binding of this aromatic amine appears to occur without an obligatory N-dephenylation and may be due to the metabolic formation of epoxides.
Metabolism of methylscopolammonium methylsulfate (DD-234) in rats.
The metabolism of methylscopolammonium methylsulfate (I) in rats was investigated. Eight metabolites were detected in urine and faeces after oral and subcutaneous administrations. The feature of
Mass spectrometric studies of the metabolites of niaprazine
Conversion of the N-Q-glucuronide and N-O-sulfate conjugates of N-hydroxyphenacetin to reactive intermediates.
Excretion, isolation and identification of the metabolites of Bisolvon.
Species differences in metabolism and excretion of bromhexine in mice, rats, rabbits, dogs and man.
Experimental study of relationship between hypertension and tumor growth and metastases.
TLDR
The results of several clinical studies have disclosed a dissociation between hypertensive and neoplastic diseases, particularly in males, and the lack of experimental information concerning the possible relationship between hypertension and tumor growth and metastases has prompted us to investigate the effect of 2 forms of experimental hypertension on the subcutaneous and hepatic growth and Metastases of the Walker tumor in the rat.
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