Pharmacokinetics, Metabolism and Toxicity of the Plant-Derived Photoxin α-Terthienyl
| Autor: | Robin J. Marles, Mariana Meckes, J. T. Arnason, S. Kacew, C. Rujjanawate, D. Kanjanapothi, C. Soucy-Breau, Xavier Lozoya, M. M. Abou-Zaid, M. Kobaisy, T. Durst |
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| Rok vydání: | 1995 |
| Předmět: |
Male
Insecticides Health Toxicology and Mutagenesis Administration Oral Thiophenes Pharmacology Biology Kidney Toxicology Median lethal dose Lethal Dose 50 Rats Sprague-Dawley Excretion Species Specificity Pharmacokinetics Oral administration Animals Rats Wistar Chromatography High Pressure Liquid Active ingredient Analysis of Variance Kidney metabolism Organ Size Metabolism Rats Liver Toxicity Injections Intraperitoneal |
| Zdroj: | Pharmacology & Toxicology. 77:164-168 |
| ISSN: | 1600-0773 0901-9928 |
| DOI: | 10.1111/j.1600-0773.1995.tb01007.x |
| Popis: | The plant-derived insecticide, alpha-terthienyl was prepared by synthesis as 3',4'-di[14C]-alpha-terthienyl for pharmacokinetic and metabolism studies. When administered orally to rats at a single dose of 50 mg/kg, excretion of the labelled material was maximal one day after administration and declined to no measurable quantities by day 4. Two metabolites [1,4-di(2'-thienyl)1,4-butadione and 2-2'-bithiophene-5-carboxylic acid] and trace quantities of the parent material were isolated from the urine and chemically identified. These represent the first metabolites of alpha-terthienyl identified. In pilot acute and subacute trials, unlabelled alpha-terthienyl was non-toxic when administered orally to rats as the "ready to use" formulation (0.1% active ingredient). The pure compound had an LD50 of 110 mg/kg when administered intraperitoneally to rats. The results suggest that there is considerable separation with respect to mosquito larvae and non-target mammal sensitivity. |
| Databáze: | OpenAIRE |
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