Physiological disposition and metabolism of O-ethyl-O-4-nitrophenyl phenylphosphonothioate in male cats following a single dermal administration. 1983

M B Abou-Donia, and C G Kinnes, and K M Abdo, and T D Bjornsson

The pharmacokinetics and metabolism of a single dermal 20.0 mg/kg of uniformly phenyl-labeled [14C]EPN (O-ethyl O-4-nitrophenyl [14C]phenylphosphonothioate) were investigated in adult male cats. Three treated cats were killed at each time interval: 0.5, 2, 4, 8, and 12. Radioactivity disappeared exponentially from administration site at a rate constant of 0.46 day-1, corresponding to a half-life of 1.5 days. Most of the absorbed radioactivity was excreted in the urine (29.9%). Only 3.2% of the 14C was recovered in the feces. No radioactivity was detected in expired CO2. Only traces of EPN were detected in the urine and feces. Most of the excreted 14C materials were identified as O-ethyl phenylphosphonothioic acid (EPPTA), O-ethyl phenylphosphonic acid (EPPA), and phenylphosphonic acid (PPA). The disposition studies showed that EPN was the major compound identified 0.5 day after administration in the brain, spinal cord, sciatic nerve, adipose tissue, plasma, muscle, liver, and kidney. Most of the radioactivity in the liver and kidney was identified after 4 days as EPPTA, EPPA, and PPA. Kinetic and distribution studies showed that EPN was eliminated from the tissues and plasma according to exponential kinetics. The half-life of the elimination of EPN from plasma was 9.1 days corresponding to a constant rate value of 0.076 day-1. Relative residence (RR) of EPN relative to plasma was longest in the sciatic nerve and shortest in the kidney.

UI MeSH Term Description Entries
D007306 Insecticides Pesticides designed to control insects that are harmful to man. The insects may be directly harmful, as those acting as disease vectors, or indirectly harmful, as destroyers of crops, food products, or textile fabrics. Insecticide
D007700 Kinetics The rate dynamics in chemical or physical systems.
D008297 Male Males
D008658 Inactivation, Metabolic Reduction of pharmacologic activity or toxicity of a drug or other foreign substance by a living system, usually by enzymatic action. It includes those metabolic transformations that make the substance more soluble for faster renal excretion. Detoxication, Drug, Metabolic,Drug Detoxication, Metabolic,Metabolic Detoxication, Drug,Detoxification, Drug, Metabolic,Metabolic Detoxification, Drug,Metabolic Drug Inactivation,Detoxication, Drug Metabolic,Detoxication, Metabolic Drug,Detoxification, Drug Metabolic,Drug Inactivation, Metabolic,Drug Metabolic Detoxication,Drug Metabolic Detoxification,Inactivation, Metabolic Drug,Metabolic Drug Detoxication,Metabolic Inactivation
D008954 Models, Biological Theoretical representations that simulate the behavior or activity of biological processes or diseases. For disease models in living animals, DISEASE MODELS, ANIMAL is available. Biological models include the use of mathematical equations, computers, and other electronic equipment. Biological Model,Biological Models,Model, Biological,Models, Biologic,Biologic Model,Biologic Models,Model, Biologic
D002415 Cats The domestic cat, Felis catus, of the carnivore family FELIDAE, comprising over 30 different breeds. The domestic cat is descended primarily from the wild cat of Africa and extreme southwestern Asia. Though probably present in towns in Palestine as long ago as 7000 years, actual domestication occurred in Egypt about 4000 years ago. (From Walker's Mammals of the World, 6th ed, p801) Felis catus,Felis domesticus,Domestic Cats,Felis domestica,Felis sylvestris catus,Cat,Cat, Domestic,Cats, Domestic,Domestic Cat
D004849 Phenylphosphonothioic Acid, 2-Ethyl 2-(4-Nitrophenyl) Ester An organothiophosphorus cholinesterase inhibitor that is used as an insecticide and as a acaricide. ENT-17,798,EPN-300,O-Ethyl-O-(4-nitrophenyl)phenylphosphonothioate,ENT 17,798,ENT17,798,EPN 300,EPN300
D005243 Feces Excrement from the INTESTINES, containing unabsorbed solids, waste products, secretions, and BACTERIA of the DIGESTIVE SYSTEM.
D006207 Half-Life The time it takes for a substance (drug, radioactive nuclide, or other) to lose half of its pharmacologic, physiologic, or radiologic activity. Halflife,Half Life,Half-Lifes,Halflifes
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia

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