Disposition and metabolism of (14)C-triclopyr acid (98.8% a.i.) was investigated in male and female rats at a low oral dose (3 mg/kg), repeated low oral doses (3 mg/kg x 14 days), and a high dose (60 mg/kg). ... Urinary metabolites of (14)C-triclopyr were isolated and identified by HPLC and GC/MS. Unmetabolized parent chemical represented >90% of urinary radioactivity, with the remainder accounted for by the metabolite 3,5,6-trichloro-2-pyridinol (3,5,6-TCP), and possible glucuronide and/or sulfate conjugates of 3,5,6-TCP. ...
IDENTIFICATION AND USE: Triclopyr is a solid. It is used as an herbicide that acts via the auxin system in plants. HUMAN EXPOSURE AND TOXICITY: Triclopyr is irritating to skin and eyes. One case report describes patient who ingested triclopyr and developed metabolic acidosis and coma with cardiovascular impairment. ANIMAL STUDIES: In male mice, triclopyr (480 mg/kg/day) caused single cell necrosis of the liver, significant increases in alkaline phosphatase, aspartate transaminase, and alanine transaminase, and enlargement of the liver with dark color. Centrilobular swelling and degeneration of hepatocytes were observed in a dose-dependent fashion at 120 mg/kg/day and above in male mice, along with mild increases in liver enzymes at 240 mg/kg/day. Degeneration of the proximal tubules of the kidneys of male and female rats was observed in increased incidence at 20 mg/kg/day and above for both sexes. Absolute and relative kidney weight was significantly increased in male rats at the 50 mg/kg/day dose, while relative kidney weight was increased in male and female rats at 250 mg/kg/day. In a chronic toxicity/carcinogenicity study in mice, there were no compound-related tumors observed in male mice. Female mice had a significant increasing trend in mammary gland adenocarcinomas. In an Ames assay, the mutagenic potential of triclopyr was negative in Salmonella tester strains TA-1535, TA-1537, TA-1538, TA-98, and TA-100 in the absence and presence of metabolic activation. Rats maintained on diets supplying 0, 3, 10, or 30 mg/kg/day over three generations exhibited no consistent treatment-related effects on reproductive performance, pregnancy, parturition, or neonatal survival. ECOTOXICITY STUDIES: Experiments on zebrafish embryos demonstrated that 3,5,6-trichloro-2-pyridinol, a metabolite of triclopyr, appears to be more toxic during development compared to the parent compound.
来源:Hazardous Substances Data Bank (HSDB)
毒理性
致癌性证据
癌症分类:D组 不可归类为人类致癌性
Cancer Classification: Group D Not Classifiable as to Human Carcinogenicity
来源:Hazardous Substances Data Bank (HSDB)
毒理性
致癌物分类
对人类不具有致癌性(未被国际癌症研究机构IARC列名)。
No indication of carcinogenicity to humans (not listed by IARC).
来源:Toxin and Toxin Target Database (T3DB)
毒理性
暴露途径
该物质可以通过吸入其气溶胶、通过皮肤接触以及吞食被身体吸收。
The substance can be absorbed into the body by inhalation of its aerosol, through the skin and by ingestion.
来源:ILO-WHO International Chemical Safety Cards (ICSCs)
毒理性
吸入症状
咳嗽。
Cough.
来源:ILO-WHO International Chemical Safety Cards (ICSCs)
In the province of Quebec (Canada), the phytocide Garlon 4, whose active ingredient is triclopyr, is often used to prevent trees from reaching electrical conductors. The object of this paper is to assess the potential health risks in workers coming into contact with Garlon 4. Ten workers collected their urine during the 22 hr following the beginning of a work shift. Measured urinary amounts of triclopyr varied between 1 and 13 mg. The absorbed daily doses were estimated from the amounts of triclopyr in urine through the use of a kinetic model that links the rates of triclopyr elimination to absorbed doses. These estimated doses were compared with the no-observed-effect level (NOEL) observed in rats: 5 mg per kg of body weight. The upper-bound estimations of the worker's daily absorbed doses were found to be 13.3% or less of the rat NOEL.
Two herbicides, 2,4-D and triclopyr esters (application ratio 1.6:1 acid equivalents) were applied as a tank mix by a crew of 8 backpack sprayer applicators, a mixer/loader, and a field supervisor. The crew was employed in a conifer release program in northern California during the summer of 2002. Biomonitoring (urine, 24 hr) utilized 2,4-D and triclopyr (a.e.) as rapidly excreted exposure biomarkers. The absorbed dosages of 2,4-D and triclopyr were calculated based upon cotton whole body suits and biomonitoring. Dosages based upon accumulation of the herbicides on body suits averaged 42.6 ug (a.e.) 2,4-D/kg-d and 8.0 ug (a.e.) triclopyr/kg-d. Six consecutive days of concurrent urine collections showed that backpack applicators excreted an average of 11.0 ug (a.e.) 2,4-D/kg-d and 18.9 ug (a.e.) triclopyr/kg-d. Estimates based upon curve fitting were 17.1 and 29.3 ug (a.e.)/kg-d, respectively. Results suggest that passive dosimetry for 2,4-D consistently overestimated the dosage measured using biomonitoring by a factor of 2-3 fold, while for triclopyr, passive dosimetry underestimated the absorbed dose based on biomonitoring by a factor of 2-4 fold.
Disposition and metabolism of (14)C-triclopyr acid (98.8% a.i.) was investigated in male and female rats at a low oral dose (3 mg/kg), repeated low oral doses (3 mg/kg x 14 days), and a high dose (60 mg/kg). Comparison of disposition data in intravenously dosed and orally dosed rats demonstrated that triclopyr was well absorbed after oral administration. Excretion was relatively rapid at the low dose, with a majority of radioactivity eliminated in the urine by 24 hours. At 60 mg/kg, urinary elimination of (14)C-triclopyr derived radioactivity was decreased in male and female rats from 0-12 hours, due to apparent saturation of renal elimination mechanisms. Fecal elimination of (14)C-triclopyr derived radioactivity was a minor route of excretion, as was elimination via exhaled air. No significant effect was observed on metabolism or disposition of (14)C-triclopyr from repeated low oral dosing in male or female rats. Residual (14)C-triclopyr derived radioactivity was minimal in all dose groups, but measurable levels of tissue radioactivity were detected in perirenal fat of both sexes and ovaries of female rats which apparently increased with dose. Thus, potential accumulation of (14)C-triclopyr derived radioactivity may occur in these tissues. Urinary metabolites of (14)C-triclopyr were isolated and identified by HPLC and GC/MS. Unmetabolized parent chemical represented >90% of urinary radioactivity, with the remainder accounted for by the metabolite 3,5,6-trichloro-2-pyridinol (3,5,6-TCP), and possible glucuronide and/or sulfate conjugates of 3,5,6-TCP. Plasma elimination following intravenous administration of (14)C-triclopyr was consistent with a one-compartment model with an elimination half-life of 3.6 hr and zero-order kinetics from 0-12 hours at the 60 mg/kg dose. Kinetic parameters were optimized using SIMUSOLV modeling software. The model showed an apparent "flip-flop" phenomenon, in which absorption at the 3 mg/kg dose was rate limiting in elimination of (14)C-triclopyr derived radioactivity, but renal excretion was saturated and therefore limiting in elimination of (14)C-triclopyr derived radioactivity at the 60 mg/kg dose.
Blood levels and urinary excretion of triclopyr, the active ingredient in Garlon herbicides, were followed in six volunteers given single oral doses of 0.1 and 0.5 mg/kg body weight. Five of these volunteers later received dermal applications of Garlon 4 herbicide formulation equivalent to 3.7 mg triclopyr/kg body weight applied to the forearm. Following oral administration blood levels peaked at 2-3 hr and declined to undetectable levels within 48 hr; more than 80% of the dose was found as unchanged triclopyr in the urine. An average of 1.37% of the applied dose was recovered in the urine; when corrected for recovery after oral administration this was equivalent to an absorption of 1.65%. Triclopyr is slowly absorbed through skin and is rapidly eliminated. It has very low potential to accumulate in man or to be absorbed through the skin in acutely toxic amounts.
1.周国泰,化学危险品安全技术全书,化学工业出版社,1997 2.国家环保局有毒化学品管理办公室、北京化工研究院合编,化学品毒性法规环境数据手册,中国环境科学出版社.1992 3.Canadian Centre for Occupational Health and Safety,CHEMINFO Database.1998 4.Canadian Centre for Occupational Health and Safety, RTECS Database, 1989
[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] 3-[(HYDRAZONO)METHYL]-N-(TETRAZOL-5-YL)-BENZAMIDE AND 3-[(HYDRAZONO)METHYL]-N-(1,3,4-OXADIAZOL-2-YL)-BENZAMIDE DERIVATIVES AS HERBICIDES<br/>[FR] DÉRIVÉS DE 3-[(HYDRAZONO))MÉTHYL]-N-(TÉTRAZOL-5-YL)-BENZAMIDE ET DE 3-[(HYDRAZONO)MÉTHYL]-N-(1,3,4-OXADIAZOL-2-YL)-BENZAMIDE UTILISÉS EN TANT QU'HERBICIDES
申请人:SYNGENTA CROP PROTECTION AG
公开号:WO2021013969A1
公开(公告)日:2021-01-28
The present invention related to compounds of Formula (I): or an agronomically acceptable salt thereof, wherein Q, R2, R3, R4, R5 and R6 are as described herein. The invention further relates to compositions comprising said compounds, to methods of controlling weeds using said compositions, and to the use of compounds of Formula (I) as a herbicide.
[EN] INSECTICIDAL TRIAZINONE DERIVATIVES<br/>[FR] DÉRIVÉS DE TRIAZINONE INSECTICIDES
申请人:SYNGENTA PARTICIPATIONS AG
公开号:WO2013079350A1
公开(公告)日:2013-06-06
Compounds of the formula (I) or (I'), wherein the substituents are as defined in claim 1, are useful as pesticides.
式(I)或(I')的化合物,其中取代基如权利要求1所定义的那样,可用作杀虫剂。
[EN] HERBICIDALLY ACTIVE HETEROARYL-S?BSTIT?TED CYCLIC DIONES OR DERIVATIVES THEREOF<br/>[FR] DIONES CYCLIQUES SUBSTITUÉES PAR HÉTÉROARYLE À ACTIVITÉ HERBICIDE OU DÉRIVÉS DE CELLES-CI
申请人:SYNGENTA LTD
公开号:WO2011012862A1
公开(公告)日:2011-02-03
The invention relates to a compound of formula (I), which is suitable for use as a herbicide wherein G is hydrogen or an agriculturally acceptable metal, sulfonium, ammonium or latentiating group; Q is a unsubstituted or substituted C3-C8 saturated or mono-unsaturated heterocyclyl containing at least one heteroatom selected from O, N and S, or Q is heteroaryl or substituted heteroaryl; m is 1, 2 or 3; and Het is an optionally substituted monocyclic or bicyclic heteroaromatic ring; and wherein the compound is optionally an agronomically acceptable salt thereof.
The present invention provides triazole compounds useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, and methods of using the same.