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.
Pognat
J F
JF
Enreille
A
A
Chabard
J L
JL
Busch
N
N
Berger
J A
JA
D000818:Animals; D000932:Antiemetics / Q000008:administration & dosage / Q000378:metabolism*; D001711:Biotransformation; D004285:Dogs; D008401:Gas Chromatography-Mass Spectrometry; D010879:Piperazines / Q000378:metabolism* / Q000652:urine
D000932:Antiemetics; D010879:Piperazines; C048372:4082CERM; C048371:mociprazine