Identification of Metabolites of Azaperone in Horse Urineǁ⊥

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Abstract

Two metabolites of the tranquilizer azaperone were extracted from alkalinized horse urine after treatment with β-glucuronidase/sulfatase from limpets (Patella vulgata). The metabolites were identified by a combination of independent chemical synthesis and GC/MS and 1H NMR analysis. The metabolites were identified as 1-(fluorophenyl)-4-[4-(5-hydroxy-2-pyridinyl)-1-piperazinyl]-1-butanol, designated as 5'-hydroxy-azaperol, and 1 -(fluorophenyl)-4-[4-(5-hydroxy-2-pyridinyl)-1 -piperazinyl]-1-butanone, designated as 5'-hydroxyazaperone. A TLC screening test was developed for detecting both metabolites in basic extracts of horse urine treated with β-glucuronidase/sulfatase. The screening test was used to detect azaperone metabolites in extracts of horse urine collected for 24 h after intravenous administration of azaperone. The administration of azaperone to horses was confirmed by GC/MS identification of 5'-hydroxyazaperone and 5'-hydroxyazaperol from basic extracts of horse urine treated with β-glucuronidase/sulfatase. The extracted metabolites were treated with bis(trimethylsilyl)acetamide to produce trimethylsilyl (TMS) ether derivatives, and mass spectra and retention times were compared to those of the synthesized metabolites treated in the same manner.

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Abstract published in Advance ACS Abstracts, November 15, 1995.

Published as Kentucky Agricultural Experiment Station Article No. 91-4-233 with the approval of the Dean and Director, College of Agriculture and Kentucky Agricultural Experiment Station.

Publication No. 178 from the Kentucky Equine Drug Testing and Research Programs, Department of Veterinary Science and the Graduate Center for Toxicology, University of Kentucky.

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