Fate of etiproston, a synthetic analogue of PGF2α, in cows |
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| Authors: | H BENECH P BRUNE A PRUVOST P ARCHIMBAULT P GUILLOT‡ R C MURPHY J MACLOUF JM GROGNET |
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| Institution: | *Service de Pharmacologie et ?Immunologie, Commissariat à?Energie Atomique, CE-Saclay 91191 Gif-sur-Yvette Cedex.;?Laboratoire VIRBAC, BP 27, 06511 Carros.;?Laboratoire des Médicaments Vétérinaires, Centre National ?Etudes Vétérinaires et Alimentaires, Javene, 35133 Fougères, France.;§National Jewish Center for Immunology and Respiratory Medicine, 1400 Jackson Street, Denver, CO 80206.;¶U 150 INSERM, Hôpital Lariboisèdre, 75010 Paris, France |
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| Abstract: | The pharmacokinetics and metabolic fate of labelled compounds were investigated after intramuscular administration of 3H-radiolabelled etiproston to nine cows. Elimination was rapid ( t 1/2β= 2.8 h). Forty-eight h after administration 92.6% of the radioactivity had been eliminated, mainly via the urinary (66% at 48 h) and faecal routes (26% at 48 h). In comparison, little elimination in milk occurred (less than 0.034% dose/l by 24 h). Radioactivity at the injection site 48 h after administration was seen in one cow (< 4.68 × 10-5% dose/g). No radioactivity was detected in the tissues. Urinary metabolites were purified and isolated using XAD-2 extraction and preparative HPLC in reverse and normal phases. The main urinary metabolite, identified by mass spectrometry, was the tetranor acid derivative in equilibrium with its lactone form. |
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