Absorption, Tissue Distribution, Excretion, and Metabolism of Clothianidin in Rats
| Autor: | Tokunori Yokota, Hiromi Nagasaki, Kazuki Mikata, Kazunari Ohta |
|---|---|
| Rok vydání: | 2003 |
| Předmět: |
Male
Insecticides medicine.medical_specialty Absorption (skin) Urine Guanidines Excretion Feces Neonicotinoids chemistry.chemical_compound Oral administration Internal medicine medicine Animals Tissue Distribution Carbon Radioisotopes Rats Wistar Chromatography High Pressure Liquid Kidney Neonicotinoid Clothianidin General Chemistry Metabolism Rats Thiazoles medicine.anatomical_structure Endocrinology Biochemistry chemistry Female Chromatography Thin Layer General Agricultural and Biological Sciences |
| Zdroj: | Journal of Agricultural and Food Chemistry. 51:7066-7072 |
| ISSN: | 1520-5118 0021-8561 |
| DOI: | 10.1021/jf034760f |
| Popis: | Absorption, distribution, excretion, and metabolism of clothianidin [(E)-1-(2-chloro-1,3-thiazol-5-ylmethyl)-3-methyl-2-nitroguanidine] were investigated after a single oral administration of [nitroimino-(14)C]- or [thiazolyl-2-(14)C]clothianidin to male and female rats at a dose of 5 mg/kg of body weight (bw) (low dose) or 250 mg/kg of bw (high dose). The maximum concentration of carbon-14 in blood occurred 2 h after administration of the low oral dose for both labeled clothianidins, and then the concentration of carbon-14 in blood decreased with a half-life of 2.9-4.0 h. The orally administered carbon-14 was rapidly and extensively distributed to all tissues and organs within 2 h after administration, especially to the kidney and liver, but was rapidly and almost completely eliminated from all tissues and organs with no evidence of accumulation. The orally administered carbon-14 was almost completely excreted into urine and feces within 2 days after administration, and approximately 90% of the administered dose was excreted via urine. The major compound in excreta was clothianidin, accounting for60% of the administered dose. The major metabolic reactions of clothianidin in rats were oxidative demethylation to form N-(2-chlorothiazol-5-ylmethyl)-N'-nitroguanidine and the cleavage of the carbon-nitrogen bond between the thiazolylmethyl moiety and the nitroguanidine moiety. The part of the molecule containing the nitroguanidine moiety was transformed mainly to N-methyl-N'-nitroguanidine, whereas the thiazol moiety was further metabolized to 2-(methylthio)thiazole-5-carboxylic acid. With the exception of the transiently delayed excretion of carbon-14 at the high-dose level, the rates of biokinetics, excretion, distribution, and metabolism of clothianidin were not markedly influenced by dose level and sex. |
| Databáze: | OpenAIRE |
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