Biotransformation study of para-substituted phenylpiperazines in beagle dogs by gas chromatography-mass spectrometry.
1. Beagle dogs were treated orally (10 mg/kg) with para-chloro-, para-fluoro- and para-methyl-phenylpiperazine derivatives, and urine was collected for 72 h after treatment. 2. Metabolites were extracted, converted into trimethylsilyl (TMS) derivatives and examined by g.l.c.-mass spectrometry. 3. The metabolites fall into two main groups, N-desphenylated metabolites, which result from N-desphenylation, and N-phenyl metabolites. 4. Two kinds of hydroxylated metabolites were found. Some lost the original para substituent (Cl, F or CH3); others retained it. 5. These results are consistent with the NIH shift reaction.
Galmier
M J
MJ
Groupe de recherches en biodynamique du médicament, Faculté de pharmacie de Clermont-Ferrand, France.
Pognat
J F
JF
Lartigue-Mattei
C
C
Chabard
J L
JL
Bastide
M
M
Busch
N
N
Berger
J A
JA
D000818:Animals; D001711:Biotransformation; D004285:Dogs; D008401:Gas Chromatography-Mass Spectrometry; D008297:Male; D015394:Molecular Structure; D010879:Piperazines / Q000737:chemistry / Q000493:pharmacokinetics* / Q000652:urine
D010879:Piperazines