Plasma kinetics of dihydroergotoxin in rat by using a radioreceptor assay |
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| Authors: | M Palmi G Segre |
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| Affiliation: | 1. Department of Occupational Health and Occupational Medicine, Guangdong Provincial Key Laboratory of Tropical Disease Research, School of Public Health, Southern Medical University, Guangzhou, Guangdong, China;2. Department of Occupational & Environmental Health and the Ministry of Education Key Lab of Hazard Assessment and Control in Special Operational Environment, School of Public Health, Fourth Military Medical University, Xi''an 710032, China;1. Division of Genetic and Molecular Toxicology, National Center for Toxicological Research, Jefferson, AR 72079, USA;2. Division of Biochemical Toxicology, National Center for Toxicological Research, Jefferson, AR 72079, USA;3. Division of Pharmacology Toxicology Review, Office of Safety and Clinical Evaluation, Center for Drug Evaluation and Research, Silver Spring, MD 20993, USA;1. ToxMinds BVBA, Brussels, Belgium;2. TotalEnergies Refining & Chemicals, Seneffe, Belgium;3. Shell International BV, Den Haag, the Netherlands;4. LyondellBasell Industries, Rotterdam, the Netherlands;5. ExxonMobil Petroleum & Chemical BVBA, Machelen, Belgium |
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| Abstract: | A radioreceptor assay (RRA) (with brain dopamine receptors) has been developed to determine the levels of dihydroergotoxin-equivalent (DHT-equivalent) material in rat plasma and its kinetics after oral and i.v. administration (5 mg/kg). After i.v. administration the plasma kinetics follows a two-exponential equation, with an apparent distribution volume of 7-9 1/kg and a long half-life (about 36 hours). The kinetics of DHT after oral administration shows two peaks; this could indicate a biliary recycling of the drug and/or of its metabolites. The low bioavailability (19%) and the biliary recycling of DHT-equivalent material suggest a first pass effect. |
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