- Synthesis, in vivo effects, metabolism, and excretion of 5 (p hydroxyanilino) 1,2,3,4 thiatriazole in the beagle dog
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Trained normal and hypertensive beagle dogs were given tritiated 5 (p hydroxyanilino) 1,2,3,4 thiatriazole orally (30 mg/kg) and intravenously (20 mg/kg). Pasma levels of radioactivity as well as blood pressure and heart rate were measured concomitantly at various times following drug administration. The maximum hypotensive effect occurred 2 hr after intravenous administration and 4 to 8 hr after oral administration. This maximum effect did not correlate with maximum plasma levels of parent drug or metabolic, suggesting that a single agent may not be responsible for the hypotensive effect; a secondary mechanism may be involved. Excretion of radioactivity was followed for 5 to 6 days after administration. Biliary secretion of parent drug or its metabolites was indicated when 9 to 17% of intravenously administered drug radioactivity was excreted via the feces. Examination of urinary metabolites from each dog showed unchanged parent drug 5.7 to 20.7% (iv), 18.6 to 20.2% (oral); p aminophenol 45.9 to 66.5% (iv), 40.7 to 45.5% (oral). Urine from one dog was examined for other metabolites, and the following were found: p hydroxyphenylthiourea, 3.2 to 5.6%; p hydroxyphenylurea, 7.1 to 10.5%; APAP, 1.5 to 1.8%; unknown metabolite, 16.2 to 23.9%.
- Ikeda,Estep,Wiemeler,Alter
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- Aromatic amine substituted - 1, 2, 3, 4 - thiadiazole and triazole derivatives, their preparation and use
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The invention relates to synthesis of a novel arylamine substituted-1,2,3,4-thiatriazole derivative (I) and an application of the derivative as a disease-resistant plant activator. As proved by activity study, the series of compounds has good prevention and control effects on various plant diseases.
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Paragraph 0074; 0075; 0076; 0121; 0122; 0123
(2017/07/23)
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