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 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.