... In male and female rats intubated with the radioactive compound in olive oil at a dose of 0.56 mg/rat (equivalent to 3.1-4.3 mg/kg bw per day) for 12 consecutive days. ... The main urinary metabolite was urea-14C, representing 85% of the radioactivity excreted by this route. Other metabolites detected in the urine were (3-14C)1-phenyl-1,2,4-triazol-3-ol, (3-14C)1-phenylsemicarbazide and (14C)semicarbazide, all conjugated with glucuronic acid. Each of these three metabolites accounted for 3-5% of the 14C eliminated in urine. Low concentrations of two unidentified metabolites were also found. In the feces, unchanged (14C)triazophos (40% of the total activity in feces) and (3-14C)1-phenyl-1,2,4-triazol-3-ol (60% of the activity) were identified. ...
The metabolic fate of triazophos was examined in beagle dogs ... two female dogs were treated by gastric intubation with (14C)triazophos at a dose of 4.4-4.8 mg/kg bw in sesame oil. Urinary excretion predominated, representing an average of 85% of the administered dose after 24 hr and 92% after 48 hr. Fecal elimination accounted for 0.3% of the administered dose after 24 hr and and 7.2% after 48 hr. Maximal blood concentrations were attained after 2 hr. After 48 hr, no radioactivity was detectable in blood. ... Residual concentrations in tissues were not determined because the animals were not killed at termination. Qualitatively, the metabolic fate of triazophos in dogs was similar to that in rats. The urine contained the same three metabolites as in rats, namely 1-phenyl-3-hydroxy-(1H)-1,2,4-triazole (18% of the administered dose) and its glucuronide (60%) and sulfate (5%) conjugates. One metabolite was found only in dog urine (representing 11% of the administered dose), which was thought to be another sulfate ester conjugate of the 1-phenyl-3-hydroxy-(1H)-1,2,4-triazole metabolite. Quantitatively, less of this metabolite was present in dog urine (18% of the administered dose) at the time of analysis than in rats (43%). The instability of the glucuronide conjugate and its potential conversion to the free metabolite were also observed in dogs, and the somewhat higher concentration of the glucuronide metabolite in the urine of dogs (60% of the administered dose) than of rats (36%) was considered not to be significant. Unchanged triazophos was not detected in urine. The feces contained low concentrations of triazophos and the free 1-phenyl-3-hydroxy-(1H)-1,2,4-triazole metabolite as well as five unidentified metabolites at about 0.7, 0.3 and 7.3% of the administered dose, respectively. ...
The metabolic fate of triazophos was studied in 23 female Wistar (WISKf (SPF 71)) rats given triazophos labeled at the 3 position (radiochemical purity, 98%) as a single oral dose of about 5 mg/kg bw in sesame oil by gastric intubation...The glucuronide was unstable and was apparently converted to the parent compound at room temperature. Unchanged triazophos was not detected in urine. ...
来源:Hazardous Substances Data Bank (HSDB)
毒理性
副作用
其他毒物 - 有机磷
Other Poison - Organophosphate
来源:Haz-Map, Information on Hazardous Chemicals and Occupational Diseases
毒理性
毒性数据
大鼠LC50 = 450毫克/立方米/4小时
LC50 (rat) = 450 mg/m3/4h
来源:Haz-Map, Information on Hazardous Chemicals and Occupational Diseases
A comatose patient who is diaphoretic, has pinpoint pupils and the odor of an insecticide on clothing or breath, and is noted to have muscle fasciculations represents the classic presentation of organophosphate poisoning. ... Specific steps in management include the following. 1. Decontamination. ... 2. Airway. Establish an airway if necessary. ... 3. Respiratory Status. Respiratory distress, in fact, is commonly found in these patients from multiple causes. ... 4. Cardiac Monitoring. ... 5. Cholinesterase Level. ... 6. Pralidoxime. Pralidoxime is the treatment of choice for organophosphate poisoning and should be used for nearly all patients with clinically significant organophosphate poisoning, particularly those patients with muscular fasciculations and weakness. ... 7. Atropine. Atropine is the physiologic antidote for organophosphate poisoning. A trial dose of atropine should be instituted on clinical ground when one suspects organophosphate intoxication. /Organophosphate poisoning/
Atropine is the antidote of choice as in organophosphate poisoning. Although the total amount of atropine required usually is less, the same initial doses are recommended. Pralidoximine usually is necessary and may reduce the effectiveness of atropine (especially with carbaryl). ... Patients require approximately 6-12 hr of atropine treatment, but all significantly poisoned patients should be observed at least 24 hr after the last atropine dose. /Organophosphate poisoning/
Airway protection. Ensure that a clear airway exists. Intubate the patients and aspirate the secretions with a large-bore suction device if necessary. Administer oxygen by mechanically assisted pulmonary ventilation if respiration is depressed. Improve tissue oxygenation as much as possible before administering atropine, so as to minimize the risk of ventricular fibrillation. In severe poisonings, it may be necessary to support pulmonary ventilation mechanically for several days. /Organophosphate pesticides/
The metabolic fate of triazophos was examined in beagle dogs ... two female dogs were treated by gastric intubation with (14C)triazophos at a dose of 4.4-4.8 mg/kg bw in sesame oil. Urinary excretion predominated, representing an average of 85% of the administered dose after 24 hr and 92% after 48 hr. Fecal elimination accounted for 0.3% of the administered dose after 24 hr and 7.2% after 48 hr. Maximal blood concentrations were attained after 2 hr. After 48 hr, no radioactivity was detectable in blood. ... Residual concentrations in tissues were not determined because the animals were not killed at termination. Qualitatively, the metabolic fate of triazophos in dogs was similar to that in rats. The urine contained the same three metabolites as in rats, namely 1-phenyl-3-hydroxy-(1H)-1,2,4-triazole (18% of the administered dose) and its glucuronide (60%) and sulfate (5%) conjugates. One metabolite was found only in dog urine (representing 11% of the administered dose), which was thought to be another sulfate ester conjugate of the 1-phenyl-3-hydroxy-(1H)-1,2,4-triazole metabolite. Quantitatively, less of this metabolite was present in dog urine (18% of the administered dose) at the time of analysis than in rats (43%). The instability of the glucuronide conjugate and its potential conversion to the free metabolite were also observed in dogs, and the somewhat higher concentration of the glucuronide metabolite in the urine of dogs (60% of the administered dose) than of rats (36%) was considered not to be significant. Unchanged triazophos was not detected in urine. The feces contained low concentrations of triazophos and the free 1-phenyl-3-hydroxy-(1H)-1,2,4-triazole metabolite as well as five unidentified metabolites at about 0.7, 0.3 and 7.3% of the administered dose, respectively. ...
The metabolic fate of triazophos was studied in 23 female Wistar (WISKf (SPF 71)) rats given triazophos labeled at the 3 position (radiochemical purity, 98%) as a single oral dose of about 5 mg/kg bw in sesame oil by gastric intubation. Twenty animals were used to investigate excretion and metabolism and the three others for blood assays. Pooled urine and fecal samples were collected after 24, 48, and 96 hr, and blood samples were taken 0, 0.5, 2, 4, 6, 8, 24 and 48 hr after administration. The maximal concentrations in blood were attained after about 4 hr. ... The recovery rate of 98% after 96 hr indicates that excretion was relatively complete. The predominant route of excretion was urinary, with > 90% of the administered radioactivity excreted within 48 hr. Fecal elimination accounted for 4.5% of the administered dose after 48 hr. The residual concentrations of radioactivity in the tissues analyzed (liver, kidney, lung, heart, brain, spinal cord and retroperitoneal and subcutaneous fat) were highest in kidney and liver but were still relatively low: <0.004 ppm. Pooled urine contained three identifiable metabolites, 1-phenyl-3-hydroxy-(1H)-1,2,4-triazole (43% of the administered dose) and its glucuronide (36%) and sulfate conjugates (13%). The glucuronide was unstable and was apparently converted to the parent compound at room temperature. Unchanged triazophos was not detected in urine. ...
Groups of five male and five female Wistar SPF rats given a single oral dose of (14C)triazophos (labeled at the 3 position of the triazole ring) in olive oil by intubation at a dose of 2.8 mg/rat (equivalent to 15-21 mg/kg bw), excreted 76% of the administered dose in urine and 21% in feces within 48 hr. No significant difference in the rate or route of elimination was found between the sexes. Analysis of tissues from animals killed 4 days after treatment showed that 14C residues represented < 0.04% of the administered dose in kidneys, gonads, brain, muscle and skin, 0.089% in liver and 0.31% in the gastrointestinal tract. Rapid elimination of (14C)triazophos was also observed in male and female rats intubated with the radioactive compound in olive oil at a dose of 0.56 mg/rat (equivalent to 3.1-4.3 mg/kg bw per day) for 12 consecutive days, with 70-83% of the administered dose recovered in urine and 18-31% in feces during the dosing period. Four days after the end of the 12-day treatment, the concentration of 14C residues in most of the tissues analyzed (subcutaneous fat, kidney, gonads, liver, brain, muscle and skin) did not exceed 0.0008% of the administered dose. The exception was the gastrointestinal tract, which still contained 0.5% of the dose. It is not clear whether urine and feces from the study with single and multiple doses were analyzed for metabolites separately and whether the metabolic profiles were qualitatively or quantitatively similar.
(14)C-Triazophos, dissolved in oil, was administered to white rats in single and repeated doses. When given as a single dose, 76% of the applied label was excreted within 4 days in urine and 21% in feces. When given repeatedly on 12 consecutive days, 69-83% of the daily applied label was excreted in urine and 18-30% in feces. The feces contained unchanged triazophos and the hydrolysis product 1-phenyl-glucuronide, phenylsemicarbazide glucuronide and semicarvazide glucuronide. Identification of metabolites was made with TLV, IR and MS. Two other metabolites were observed but not identified. Neither triazophos nor the oxon analog were observed in urine.
Comprehensive multi-omics investigation of sub-chronic toxicity induced by Cadmium and Triazophos Co-exposure in hook snout carps (Opsariichthys bidens)
[EN] ACC INHIBITORS AND USES THEREOF<br/>[FR] INHIBITEURS DE L'ACC ET UTILISATIONS ASSOCIÉES
申请人：GILEAD APOLLO LLC
公开号：WO2017075056A1
公开（公告）日：2017-05-04
The present invention provides compounds I and II useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, and methods of using the same.
[EN] BICYCLYL-SUBSTITUTED ISOTHIAZOLINE COMPOUNDS<br/>[FR] COMPOSÉS ISOTHIAZOLINE SUBSTITUÉS PAR UN BICYCLYLE
申请人：BASF SE
公开号：WO2014206910A1
公开（公告）日：2014-12-31
The present invention relates to bicyclyl-substituted isothiazoline compounds of formula (I) wherein the variables are as defined in the claims and description. The compounds are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to a method for controlling invertebrate pests by using these compounds and to plant propagation material and to an agricultural and a veterinary composition comprising said compounds.
The present invention relates to azoline compounds of formula (I) wherein A, B1, B2, B3, G1, G2, X1, R1, R3a, R3b, Rg1 and Rg2 are as defined in the claims and the description. The compounds are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to a method for controlling invertebrate pests by using these compounds and to plant propagation material and to an agricultural and a veterinary composition comprising said compounds.
