Paraquat was not metabolized by rats. After oral administration (gastric intubation) of single doses of paraquat dichloride or dimethylsulfate to Wistar strain male and female rats, most of the administered radioactivity (69-96%) was excreted in feces as unchanged paraquat. After subcutaneous injection of these compounds, unchanged paraquat appeared mostly in urine (73-96% of the administered radioactivity). Paraquat used in this study (radiochemical purity: 99-100%) was labeled with (14)C in the methyl groups. The doses used for gastric intubation ranged from 0.5 to 50 mg/kg and for subcutaneous injection, from 12.5 to 24 mg/kg. Most of the radioactivity was detected in feces within 2-3 days after dosing and in urine, within 1 day after dosing. Following oral administration of paraquat, up to 30% of the dose appeared in feces in a degraded form. This was due to the microbial degradation of paraquat in the gut. That microbial degradation of paraquat occurred in feces was shown in an in vitro experiment in which fecal homogenates were incubated with added paraquat for 24 hours. In that experiment, 40-50% of paraquat was destroyed. However, a similar experiment with sterilized fecal homogenates produced only minor loss (trace amounts) of added paraquat. /Paraquat dichloride/
Three Warren hens were given gelatin capsules containing (14)C-ring-labelled paraquat (purity, 99.7%; specific activity, 1.216 x 105 dpm/mg) at a daily dose of 4.52 mg of paraquat ion (0.247 mCi) for 10 days. ...Residues in tissues were generally unchanged paraquat. A small amount of a metabolite, 1-methyl-(4'-pyridyl), was found in the livers and kidneys.
来源:Hazardous Substances Data Bank (HSDB)
代谢
一只英国白保姆山羊通过饮食中添加了（14）C-环标记的百草枯（纯度99.7%；比活性2.28 x 10^4 dpm/ug），剂量相当于每克饲料100微克百草枯离子……持续7天。……组织中残留物通常是未改变的百草枯。在肝脏中，发现了少量的4-(1,2-二氢-1-甲基-2-氧代-4-吡啶基)-1-甲基吡啶离子和1-甲基-4-(4'-吡啶基)吡啶离子。后一种化合物也存在于腹膜脂肪中。
An English white nanny goat was dosed with (14)C-ring-labelled paraquat (purity, 99.7%; specific activity, 2.28 x 104 dpm/ug) in the diet at a dose equivalent to 100 ug of paraquat ion/g of diet ... for 7 days. ... Residues in tissues were generally unchanged paraquat. In the liver, small amounts of 4-(1,2-dihydro-1-methyl-2-oxo-4-pyridyl)-1-methyl pyridinium ion and 1-methyl-4-(4'-pyridyl) pyridinium ion were found. The latter compound was also found in peritoneal fat.
IDENTIFICATION AND USE: Paraquat is available as an odorless yellow solid, or off-white powder. The form marketed in the U.S. is a liquid with a blue dye added to keep it from being confused with beverages, a sharp odor to serve as a warning, and an agent to cause vomiting if someone drinks it. The U.S. Environmental Protection Agency classifies paraquat as "restricted use", so it can only be used by licensed applicators. It is used globally as a non-selective herbicide that kills all green plant tissue it contacts, especially grasses and weeds. It has been used for desiccation of seed crops; weed control in orchards; defoliation and desiccation of cotton; as a harvest aid in soybeans, sugarcane, guar, and sunflowers; and for killing dormant alfalfa and clover, potato vines, and marijuana plants. HUMAN EXPOSURE: Dermal exposure to paraquat usually results in minor skin or eye irritation. Rarely, with heavier exposures resulting from misuse, more serious effects may occur such as blistered or ulcerated skin, loss of fingernails, skin burns, and ulcers of the mouth, nosebleeds, and protracted or even permanent blindness. Several human deaths from ingestion or subcutaneous injection of paraquat have been reported, gradually developing lethal lung damage usually in 3 weeks (progressive fibrosis). It has been estimated that a lethal dose in man is about 14 mL of a 40% solution of paraquat. The symptoms of poisoning include burning of the mouth and throat, nausea and vomiting, respiratory distress, and transient effects on the kidneys, heart, and nervous system. In a study of 30 workers spraying paraquat over a 12 week period, approximately 50% of them had minor irritation of the eyes or nose; 1 worker had an episode of epistaxis. Of 296 spray operators with skin exposure described as gross and prolonged, 55 had damaged fingernails, the most common lesion was transverse white bands of discoloration, but loss of nail surface, transverse ridging, gross deformity of the nail plate, and loss of nails also occurred. Paraquat dichloride was weakly positive in human lymphocytes in culture cytogenetic assay, with and without metabolic activation. ANIMAL STUDIES: Two groups of rats were given a single ip dose of paraquat at 15 mg/kg. Three hr after injection, rats exhibited an uncoordinated gait and/or widely splayed limbs consistent with neurologic impairment. All paraquat-treated rats died within 42 to 96 hr. Toxicity included anorexia, adipsia, diarrhea, hyperpnea, dyspnea, and tachycardia, necrosis of liver, kidney, and GI tract with primary lesions in lungs. Paraquat provoked overt motor impairment (reduced home-cage activity and impaired vertical climbing) and signs of anxiety-like behavior (reduced open field exploration) in wild-type but not interferon-gamma (IFN-gamma) knockout mice. Correspondingly, paraquat promoted somewhat divergent variations in neurochemical activity among wild-type and IFN-gamma null mice at brain sites important for both motor (striatum) and co-morbid affective pathologies (dorsal hippocampus, medial prefrontal cortex, and locus coeruleus). In addition, the herbicide influenced serotonergic and noradrenergic activity within the dorsal hippocampus and medial prefrontal cortex; and elevated noradrenergic activity within the locus coeruleus. Paraquat has been found to have minimal to no genotoxic activity when evaluated in a variety of in vitro and in vivo test systems. In in vitro studies producing weakly positive results, paraquat genotoxicity was accompanied by high cytotoxicity. ECOTOXICITY STUDIES: Effects of the herbicide paraquat were assessed on the green freshwater alga Chlamydomonas reinhardtii. Paraquat concentrations above 0.25 uM induce toxic effects in C. reinhardtii, reflected in a significantly reduced growth rate and cell concentration with a corresponding median effective concentration (EC50) value of 0.26 uM. With increasing paraquat concentrations, an increase in cell volume was registered as well as an increase in reactive oxygen species. Several genes involved in oxidative stress defense mechanisms, such as L-ascorbate peroxidase, glutaredoxin, and a possible glutathione-S-transferase were differentially expressed. Signs of acute intoxication: Polydipsia, regurgitation, swallowing, ataxia, imbalance, wing-drop, hyporeactivity, slowness, asthenia, sitting, running and falling, and possible miosis occurred in birds exposed to paraquat. Polydipsia and regurgitation appeared as soon as 9 min and other signs of intoxication appeared 3 hr after treatment. Mortalities usually occurred between 3 and 20 hr after treatment. Remission took up to 12 days. Paraquat was found to provoke pseudo-feminization of the males during in vivo tests, where eggs were sprayed with 0.4-1.4% aqueous solution of paraquat, and in vitro tests were conducted on cultures prepared 8.5-9 days after the start of the incubation.
CLASSIFICATION: C; possible human carcinogen. BASIS FOR CLASSIFICATION: Paraquat produced squamous cell carcinoma, an uncommon tumor, in the head region in both sexes of Fischer 344 rats. HUMAN CARCINOGENICITY DATA: None. ANIMAL CARCINOGENICITY DATA: Limited. /Based on former classification system/
Occupational hepatotoxin - Secondary hepatotoxins: the potential for toxic effect in the occupational setting is based on cases of poisoning by human ingestion or animal experimentation.
Nephrotoxin - The chemical is potentially toxic to the kidneys in the occupational setting.
Dermatotoxin - Skin burns.
Toxic Pneumonitis - Inflammation of the lungs induced by inhalation of metal fumes or toxic gases and vapors.
Fibrogenic - Inducing tissue injury and fibrosis (scarring).
ACGIH Carcinogen - Not Classifiable.
来源:Haz-Map, Information on Hazardous Chemicals and Occupational Diseases
As a result of nuclear power plants accidents such as Chernobyl or Fukushima, some people were exposed to external and internal ionizing radiation (IR). Human brain is highly sensitive to IR during fetal and postnatal period when the molecular processes are not completely finished. Various studies have shown that exposure to low doses of IR causes a higher incidence of cognitive impairment. On the other hand, in industrialized countries, people are daily exposed to a number of toxicant pollutants. Exposure to environmental chemicals, such as paraquat (PQ), may potentiate the toxic effects induced by radiation on brain development. In this study, we evaluated the cognitive effects of concomitant exposure to low doses of internal radiation ((137)Cs) and PQ during neonatal brain development. At the postnatal day 10 (PND10), two groups of mice (C57BL/6J) were exposed to (137)Cs (4000 and 8000 Bq/kg) and/or PQ (7 mg/kg). To investigate the spontaneous behavior, learning, memory capacities and anxiety, behavioral tests were conducted in the offspring at two months of age. The results showed that cognitive functions were not significantly affected when (137)Cs or PQ were administered alone. However, alterations in the working memory and anxiety were detected in mice exposed to (137)Cs combined with PQ.
Superoxide dismutase (SOD), glutathione, and d-propranolol were evaluated for their ability to protect against paraquat dichloride toxicity in rats. SOD significantly prolonged and increased survival of exposed rats.
In a fatal case of paraquat poisoning in a pregnant woman, who developed the typical symptoms and signs of paraquat poisoning and at postmortem had the typical lung pathology of paraquat poisoning, the fetal lungs were normal. ...However, ...the details /as reported/ of nine pregnant women who deliberately ingested paraquat, stated that paraquat in one case was concentrated 4-6 times in the fetus. In another of the cases, the amniotic fluid contained paraquat at twice the concentration of that in the maternal blood.
Paraquat was poorly absorbed after oral administration to rats, dogs and mice. Once absorbed, paraquat was rapidly distributed to most tissues but especially to lungs and kidneys. Tissues other than lungs did not retain paraquat.
In a dermal absorption study with healthy adult male volunteers, 0.3% of the applied (14)C-paraquat dichloride was absorbed through the intact skin (forearms, and back of the hands and lower legs) during the 24-hour exposure period. /Paraquat dichloride/
Absorbed paraquat is distributed via the bloodstream to practically all organs and tissues of the body, but no prolonged storage takes place in any tissue. The distribution of paraquat is best described by a three-compartment open model with input to and elimination from the central compartment ... The lung then selectively accumulates paraquat from the plasma, by an energy dependent process.
[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.
Molecules having pesticidal utility, and intermediates, compositions, and processes, related thereto
申请人：Dow AgroSciences LLC
公开号：US20180279612A1
公开（公告）日：2018-10-04
This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”).
