Unchanged ring-labelled (14)-C bensulide could be detected in roots of lettuce plants after root application ... . A large part of the radioactive material in the leaves was evolved as radioactive carbon dioxide and some was present as labelled amino acids.
Metabolism of organophosphates occurs principally by oxidation, by hydrolysis via esterases and by reaction with glutathione. Demethylation and glucuronidation may also occur. Oxidation of organophosphorus pesticides may result in moderately toxic products. In general, phosphorothioates are not directly toxic but require oxidative metabolism to the proximal toxin. The glutathione transferase reactions produce products that are, in most cases, of low toxicity. Paraoxonase (PON1) is a key enzyme in the metabolism of organophosphates. PON1 can inactivate some organophosphates through hydrolysis. PON1 hydrolyzes the active metabolites in several organophosphates insecticides as well as, nerve agents such as soman, sarin, and VX. The presence of PON1 polymorphisms causes there to be different enzyme levels and catalytic efficiency of this esterase, which in turn suggests that different individuals may be more susceptible to the toxic effect of organophosphate exposure.
IDENTIFICATION AND USE: Bensulide is a viscous amber liquid above 34.4 °C, and a solid below that temperature. It is used for pre-emergence control of annual grasses and broad-leaved weeds in established turf, dichondra, brassicas, cucurbits, watermelons, cotton, lettuce, tomatoes, carrots, capsicums, rice, and herbage seed crops. HUMAN STUDIES: No data. ANIMAL STUDIES: Bensulide is a cholinesterase inhibitor and mild irritant in rabbit eyes. Rats tolerated 1 hr exposures to 8 mg/L air. In 90 day feeding trials, no-effect level for rats was 25 mg/kg/day, for dogs 2.5 mg/kg/day, and for mice 30 mg/kg/day. In a chronic toxicity study in dogs, bensulide (92.4% a.i.) was administered to 4 dogs/sex/dose by feeding at dose levels of 0, 0.5, 4, or 30 mg/kg/day for 52 weeks. No neoplastic tissue was observed in dogs in the treatment and control groups. Chronic toxicity in rats receiving 60 mg/kg/day was characterized in both sexes by reduced cholinesterase levels in plasma, erythrocytes, and brain, and, in the males, by increased absolute liver weights and mild histopathological changes of the liver (hepatocyte vacuolation and eosinophilic foci). In the 15 mg/kg/day animals, reduced plasma and erythrocyte cholinesterase activities were also observed. In developmental toxicity studies bensulide exerted no effects on maternal gross pathology, fertility, or cesarian parameters and the lack of any developmental effects. Bensulide was not mutagenic when evaluated for its ability to induce point mutations in the T4 bacteriophage/Escherichia coli B system. ECOTOXICITY STUDIES: Bensulide was toxic to fish and inhibited germination in grasses.
Bensulide is a cholinesterase or acetylcholinesterase (AChE) inhibitor. A cholinesterase inhibitor (or 'anticholinesterase') suppresses the action of acetylcholinesterase. Because of its essential function, chemicals that interfere with the action of acetylcholinesterase are potent neurotoxins, causing excessive salivation and eye-watering in low doses, followed by muscle spasms and ultimately death. Nerve gases and many substances used in insecticides have been shown to act by binding a serine in the active site of acetylcholine esterase, inhibiting the enzyme completely. Acetylcholine esterase breaks down the neurotransmitter acetylcholine, which is released at nerve and muscle junctions, in order to allow the muscle or organ to relax. The result of acetylcholine esterase inhibition is that acetylcholine builds up and continues to act so that any nerve impulses are continually transmitted and muscle contractions do not stop. Among the most common acetylcholinesterase inhibitors are phosphorus-based compounds, which are designed to bind to the active site of the enzyme. The structural requirements are a phosphorus atom bearing two lipophilic groups, a leaving group (such as a halide or thiocyanate), and a terminal oxygen.
来源:Toxin and Toxin Target Database (T3DB)
毒理性
致癌性证据
癌症分类：不太可能对人类致癌
Cancer Classification: Not Likely to be Carcinogenic to Humans
来源:Hazardous Substances Data Bank (HSDB)
毒理性
致癌物分类
对人类无致癌性（未列入国际癌症研究机构IARC清单）。
No indication of carcinogenicity to humans (not listed by IARC).
Acute exposure to cholinesterase inhibitors can cause a cholinergic crisis characterized by severe nausea/vomiting, salivation, sweating, bradycardia, hypotension, collapse, and convulsions. Increasing muscle weakness is a possibility and may result in death if respiratory muscles are involved. Accumulation of ACh at motor nerves causes overstimulation of nicotinic expression at the neuromuscular junction. When this occurs symptoms such as muscle weakness, fatigue, muscle cramps, fasciculation, and paralysis can be seen. When there is an accumulation of ACh at autonomic ganglia this causes overstimulation of nicotinic expression in the sympathetic system. Symptoms associated with this are hypertension, and hypoglycemia. Overstimulation of nicotinic acetylcholine receptors in the central nervous system, due to accumulation of ACh, results in anxiety, headache, convulsions, ataxia, depression of respiration and circulation, tremor, general weakness, and potentially coma. When there is expression of muscarinic overstimulation due to excess acetylcholine at muscarinic acetylcholine receptors symptoms of visual disturbances, tightness in chest, wheezing due to bronchoconstriction, increased bronchial secretions, increased salivation, lacrimation, sweating, peristalsis, and urination can occur. Certain reproductive effects in fertility, growth, and development for males and females have been linked specifically to organophosphate pesticide exposure. Most of the research on reproductive effects has been conducted on farmers working with pesticides and insecticdes in rural areas. In females menstrual cycle disturbances, longer pregnancies, spontaneous abortions, stillbirths, and some developmental effects in offspring have been linked to organophosphate pesticide exposure. Prenatal exposure has been linked to impaired fetal growth and development. Neurotoxic effects have also been linked to poisoning with OP pesticides causing four neurotoxic effects in humans: cholinergic syndrome, intermediate syndrome, organophosphate-induced delayed polyneuropathy (OPIDP), and chronic organophosphate-induced neuropsychiatric disorder (COPIND). These syndromes result after acute and chronic exposure to OP pesticides.
来源:Toxin and Toxin Target Database (T3DB)
吸收、分配和排泄
选择性除草剂，吸附在根部表面，少量被根部吸收。bensulide不会转移到叶片，但其代谢物会转移。
Selective herbicide, adsorbed on the root surfaces, and a small amount is absorbed by the roots. Translocation of bensulide to the leaves does not occur, but metabolites are translocated.
In a metabolism study, bensulide technical, labelled with C in the 14 phenyl ring (> 96.4% radiopurity; 925 MBq/mMole) was dissolved in corn oil (vehicle) and administered to Sprague-Dawley rats (5/sex/group; 7-8 weeks of age; 185-235 g body weight) following 3 treatment regimes. Animals in Group I received a single oral dose of radioactive bensulide at 1 mg/kg bw. Animals in Group II received 14 consecutive doses (1 mg/kg/day) of non-radioactive bensulide technical (99% a.i.) in corn oil, followed by a 1 mg/kg dose of radiolabelled bensulide technical in corn oil on day 15. Group III animals received a single oral dose of radiolabelled bensulide technical at 100 mg/kg bw. An additional group of animals (Group IV; 3/sex/group) were given a single oral dose of radiolabelled bensulide 18 technical at 1 mg/kg bw and were subseqently used for autoradiological radiolabelled carbon dioxide release determinations. ... In Group I, total urinary excretion of 7 days after admin of radioactive bensulide technical accounted for 70 and 75% of the administered dose in males and females, respectively. ... In Group III, total urinary excretion accounted for 75 and 87% of the administered dose in males and females, respectively. ... For Group II (prior 14-day admin of non-radioactive bensulide technical before radioactive bensulide admin, both at 1 mg/kg), total urinary excretion of radioactivity over 7 days past dosing with radioactive bensulide accounted for 79 and 88% of the administered dose in males and females, respectively. For Group IV, urinary excretion of 14-C radioactivity derived from bensulide technical over a 48-hr period accounted for 67% for one male and 86% in one male. For Group I, total fecal excretion of radioactivity derived from 14C-bensulide technical over 7 days post-dosing accounted for 22 and 20% of the administered dose in males and females, respectively. ... For Group III, total fecal elim over 7 days post-dosing of bensulide-derived radioactivity accounted for 22 and 11% of the administered dose for males and females, respectively. ... In Group II animals, total fecal excretion of radioactivity over 7 days post-dosing accounted for 14 and 8% of the administered dose for males and females, respectively. ... In Group IV, fecal excretion of radioactivity over 48 hrs post-dosing accounted for 12% of the administered dose in one male and 7% in one female. ... The radioactivity found in the carcasses and in other tissues accounted for 0.3% to 2.5% and <0.1% of the administered dose, respectively.
[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”).
