Metabolism of trifluralin in rats

Erkog, Figen Unlu; Menzer, Robert E.

doi:10.1021/jf00066a012

Cited by 21 publications

(29 citation statements)

References 12 publications

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“…While some authors have reported a very low absorption of the drug [9,11,16] , Dow et al [17] found high plasma trifluralin concentrations after oral administration of the drug in rats. At present there is no evidence of trifluralin pharmacokinetics in humans, and all assays performed in vivo by our group have been made using a mouse model [4,7,15,18] .…”

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confidence: 98%

“…Trifluralin metabolism has been studied by Erkog and Menzer [9] in rats using [ 14 CF 3 ] at 1 and 10 mg/kg doses in a continuous feeding experiment. Trifluralin is excreted in feces and urine, where 6 and 7 metabolites have been identified, respectively.…”

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confidence: 99%

“…Trifluralin is excreted in feces and urine, where 6 and 7 metabolites have been identified, respectively. The major metabolic pathway of trifluralin involves nitro reduction, N-dealkylation, cyclization, hydroxylation and conjugation [9] . The product of reduction of both nitro groups was the main metabolite identified in urine and feces of lactating goats [10] .…”

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confidence: 99%

“…In general, trifluralin is extensively and rapidly degraded by N-dealkylation, nitro reduction, aliphatic hydroxylation and cyclization, resulting in a continuous accumulation of an heterogeneous mixture of polar products [9,11] .…”

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confidence: 99%

“…Trifluralin pharmacokinetics has been previously studied in animal models [9,11,16,17] . While some authors have reported a very low absorption of the drug [9,11,16] , Dow et al [17] found high plasma trifluralin concentrations after oral administration of the drug in rats.…”

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Pharmacokinetics of Trifluralin in Blood and Heart Tissue of Mice

Zaidenberg¹,

Marra²,

Villagra³

et al. 2009

Chemotherapy

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Background: Trifluralin displays anti-Trypanosoma cruzi activity and a potential therapeutic effect for the treatment of Chagas disease. We assessed peroral and intramuscular trifluralin pharmacokinetics in mouse blood and heart tissue. Methods: A parallel experimental design was used. Healthy adult male CF1 albino mice (n = 108, 25–35 g bw) received a single peroral or intramuscular trifluralin dose (50 mg/kg in peanut oil). Blood and heart tissue samples were taken at set times after intramuscular and peroral trifluralin administration. Feces and tissue samples were taken 12 h after intramuscular trifluralin administration. Trifluralin concentrations in whole blood, feces and tissues were determined by HPLC. Results: After intramuscular and peroral administration, maximum whole blood concentration (C_max) was attained at 30 min and 2.0 h (t_max) (28.2 ± 0.7 and 7.8 ± 0.033 μg/ml; p < 0.05). C_max in heart tissue was attained at 1.0 and 2.0 h (0.6 ± 0.004 and 0.2 ± 0.002 μg/g; p < 0.05). Liver, perirenal and subcutaneous fat concentrations were 55.1, 66.3 and 59.7 ng/mg tissue protein. Peroral and intramuscular penetration ratios determined by comparing heart tissue areas under the curve were 6.3 and 4.0%, respectively. Conclusion: Intramuscular trifluralin could be a new alternative for the treatment of Chagas disease.

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Pharmacokinetics of Trifluralin in Blood and Heart Tissue of Mice

Zaidenberg¹,

Marra²,

Villagra³

et al. 2009

Chemotherapy

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Separation and identification of trifluralin metabolites by open-tubular liquid chromatography/negative chemical ionization mass spectrometry

Wit

Parker

Tomer

et al. 1988

Biol. Mass Spectrom.

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Interspecies scaling of the bioaccumulation of lipophilic xenobiotics in fish: An example using trifluralin

Schultz

Hayton

1999

Enviro Toxic and Chemistry

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A poorly understood factor that may influence differences in the accumulation of a xenobiotic among fishes is interspecies differences in physiology. We have extensively studied the uptake, distribution, and excretion kinetics of the lipophilic herbicide trifluralin (TF) in fish, using a static water exposure system and compartmental toxicokinetic models. We obtained quantitative estimates of physiologically based toxicokinetic parameters such as uptake clearance, apparent volume of distribution, and elimination clearance due to xenobiotic metabolism, in rainbow trout, channel catfish, and bluegill sunfish at two acclimation temperatures. In these and other species (largemouth bass, gizzard shad, fathead minnows, and lake sturgeon), oxygen consumption rate, total lipid content, plasma protein binding, and in vitro biotransformation rates from liver homogenates were determined and examined for their capacities to predict toxicokinetic parameter values. The uptake clearance of TF was predictable based on the oxygen consumption rate, and in vitro TF biotransformation rate was a useful predictor of the in vivo metabolic clearance of TF. Lipid content, however, did not predict the apparent volume of distribution of TF. Values of uptake and metabolism clearance were predicted in largemouth bass, gizzard shad, fathead minnows, and lake sturgeon, using the oxygen consumption and the in vitro TF biotransformation rates. These predicted parameters were then used to successfully simulate the toxicokinetics of TF in these species.

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Metabolism of trifluralin in rats

Cited by 21 publications

References 12 publications

Pharmacokinetics of Trifluralin in Blood and Heart Tissue of Mice

Pharmacokinetics of Trifluralin in Blood and Heart Tissue of Mice

Separation and identification of trifluralin metabolites by open-tubular liquid chromatography/negative chemical ionization mass spectrometry

Interspecies scaling of the bioaccumulation of lipophilic xenobiotics in fish: An example using trifluralin

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