Identification and quantitation of 1-arylpiperazines, metabolites resulting from side-chain cleavage of (4-substituted aryl-1-piperazinyl)alkyl heterocyclic derivatives in rat plasma and brain

S. Caccia, A. Notarnicola, M. H. Fong, E. Benfenati

Research output: Contribution to journalArticle

16 Citations (Scopus)

Abstract

Many drugs contain the arylpiperazine moiety in the side-chain of their molecules. A common metabolic pathway of such drugs is cleavage of the side-chain with the formation of 1-arylpiperazines. This has been verified by combined gas chromatography-mass spectrometry of biological samples from rats given orally a series of heterocyclic derivatives bearing a 4-aryl(phenyl, pyrimidinyl, pyridyl or thiazolyl)-1-piperazinylalkyl moiety (oxypertine, zolertine, millipertine, empiprazole, dapiprazole, antrafenine, piribedil, azaperone). A sensitive and selective electron-capture gas-liquid chromatographic procedure for 1-arylpiperazines in rat plasma and brain is described. The overall recovery from plasma and brain was 70-90%. The limit of detection for substituted (halogenated) phenylpiperazines was 10-25 ng/ml or ng/g and 25-100 ng/ml or ng/g for other derivatives. Preliminary data are reported on the time course of the production and elimination of 1-arylpiperazines after oral administration of representative compounds with the arylpiperazine moiety (oxypertine, azaperone and S-3608).

Original languageEnglish
Pages (from-to)211-221
Number of pages11
JournalJournal of Chromatography A
Volume283
Issue numberC
DOIs
Publication statusPublished - 1984

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Azaperone
1-(coumaran-5-ylmethyl)-4-(2-thiazolyl)piperazine
Metabolites
Rats
Brain
Bearings (structural)
Piribedil
Derivatives
Plasmas
Metabolic Networks and Pathways
Pharmaceutical Preparations
Gas chromatography
Gas Chromatography-Mass Spectrometry
Mass spectrometry
Oral Administration
Limit of Detection
Gases
Electrons
Recovery
Molecules

ASJC Scopus subject areas

  • Analytical Chemistry
  • Clinical Biochemistry
  • Molecular Medicine

Cite this

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title = "Identification and quantitation of 1-arylpiperazines, metabolites resulting from side-chain cleavage of (4-substituted aryl-1-piperazinyl)alkyl heterocyclic derivatives in rat plasma and brain",
abstract = "Many drugs contain the arylpiperazine moiety in the side-chain of their molecules. A common metabolic pathway of such drugs is cleavage of the side-chain with the formation of 1-arylpiperazines. This has been verified by combined gas chromatography-mass spectrometry of biological samples from rats given orally a series of heterocyclic derivatives bearing a 4-aryl(phenyl, pyrimidinyl, pyridyl or thiazolyl)-1-piperazinylalkyl moiety (oxypertine, zolertine, millipertine, empiprazole, dapiprazole, antrafenine, piribedil, azaperone). A sensitive and selective electron-capture gas-liquid chromatographic procedure for 1-arylpiperazines in rat plasma and brain is described. The overall recovery from plasma and brain was 70-90{\%}. The limit of detection for substituted (halogenated) phenylpiperazines was 10-25 ng/ml or ng/g and 25-100 ng/ml or ng/g for other derivatives. Preliminary data are reported on the time course of the production and elimination of 1-arylpiperazines after oral administration of representative compounds with the arylpiperazine moiety (oxypertine, azaperone and S-3608).",
author = "S. Caccia and A. Notarnicola and Fong, {M. H.} and E. Benfenati",
year = "1984",
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T1 - Identification and quantitation of 1-arylpiperazines, metabolites resulting from side-chain cleavage of (4-substituted aryl-1-piperazinyl)alkyl heterocyclic derivatives in rat plasma and brain

AU - Caccia, S.

AU - Notarnicola, A.

AU - Fong, M. H.

AU - Benfenati, E.

PY - 1984

Y1 - 1984

N2 - Many drugs contain the arylpiperazine moiety in the side-chain of their molecules. A common metabolic pathway of such drugs is cleavage of the side-chain with the formation of 1-arylpiperazines. This has been verified by combined gas chromatography-mass spectrometry of biological samples from rats given orally a series of heterocyclic derivatives bearing a 4-aryl(phenyl, pyrimidinyl, pyridyl or thiazolyl)-1-piperazinylalkyl moiety (oxypertine, zolertine, millipertine, empiprazole, dapiprazole, antrafenine, piribedil, azaperone). A sensitive and selective electron-capture gas-liquid chromatographic procedure for 1-arylpiperazines in rat plasma and brain is described. The overall recovery from plasma and brain was 70-90%. The limit of detection for substituted (halogenated) phenylpiperazines was 10-25 ng/ml or ng/g and 25-100 ng/ml or ng/g for other derivatives. Preliminary data are reported on the time course of the production and elimination of 1-arylpiperazines after oral administration of representative compounds with the arylpiperazine moiety (oxypertine, azaperone and S-3608).

AB - Many drugs contain the arylpiperazine moiety in the side-chain of their molecules. A common metabolic pathway of such drugs is cleavage of the side-chain with the formation of 1-arylpiperazines. This has been verified by combined gas chromatography-mass spectrometry of biological samples from rats given orally a series of heterocyclic derivatives bearing a 4-aryl(phenyl, pyrimidinyl, pyridyl or thiazolyl)-1-piperazinylalkyl moiety (oxypertine, zolertine, millipertine, empiprazole, dapiprazole, antrafenine, piribedil, azaperone). A sensitive and selective electron-capture gas-liquid chromatographic procedure for 1-arylpiperazines in rat plasma and brain is described. The overall recovery from plasma and brain was 70-90%. The limit of detection for substituted (halogenated) phenylpiperazines was 10-25 ng/ml or ng/g and 25-100 ng/ml or ng/g for other derivatives. Preliminary data are reported on the time course of the production and elimination of 1-arylpiperazines after oral administration of representative compounds with the arylpiperazine moiety (oxypertine, azaperone and S-3608).

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