Mercaptodimethur is a white crystalline powder with a mild odor. Used as an insecticide and immobilizing agent for birds, acaricide and molluscicide. (EPA, 1998)
颜色/状态:
Colorless crystals
气味:
Phenol-like odor
蒸汽压力:
2.7X10-7 mm Hg @ 25 °C
亨利常数:
1.18e-09 atm-m3/mole
稳定性/保质期:
燃烧会产生有毒的氮氧化物和氧硫化物气体。
分解:
Hydrolysis DT50 (22 °C) >1 yr (pH 4), <35 day (pH 7), 6 hr (pH 9). Photodegradation contributes to the overall elimination of methiocarb from the environment; DT50 6-16 days.
WHEN RAT & HUMAN LIVER WAS INCUBATED WITH MESUROL, ABOUT A DOZEN METABOLITES WERE OBSERVED ... MAJOR METABOLITE WAS MESUROL SULFOXIDE. SEVERAL METABOLIC PRODUCTS ... FROM HUMAN LIVER STUDIES, WERE NOT OBSERVED IN RAT STUDIES. HYDROLYSIS YIELDED THE PHENOLIC MOIETY OF MESUROL.
来源:Hazardous Substances Data Bank (HSDB)
代谢
Methiocarb, a kind of aromatic alkyl sulfide insecticide, was enzymatically oxidized into sulfoxide by microsomes from soybean cotyledons. No further oxidation into sulfone was detected. The distribution of sulfoxidase activity was studied in soybean seedlings and found to be highest in the cotyledons. Subcellular fractionation of cotyledon homogenates indicated that the activity was almost entirely associated with the microsomal fraction. Methiocarb did not require cofactors such as NAD(P)H. Nevertheless, the sulfoxidase did not act as a peroxidase.
Methiocarb, an aromatic alkyl sulfide insecticide was enzymatically oxidized into sulfoxide by microsomes from soybean cotyledons. No further oxidation into sulfone was detected. Distribution of the sulfoxidase activity was studied in soybean seedlings & was maximal in cotyledons. Subcellular fractionation of cotyledon homogenates indicated that the activity was almost entirely associated with the microsomal fraction. Methiocarb did not require cofactors such as NAD(P)H. Nevertheless, the sulfoxidase did not act as a peroxidase.
The oxidation of sulfide-containing organophosphate & carbamate pesticides by the flavin-containing monooxygenase was measured in mammalian microsomes made devoid of cytochrome p450 dependent activity, primarily through the use of inhibitory antibodies against reduced nicotinamide adenine dinucleotide phosphate cytochrome p450 reductase. Rates of metab were determined for mouse, rabbit & rat liver, lung & kidney microsomes, & for pig liver microsomes. Substrate specificity of the enzyme in different species & tissues is similar. Lung & kidney microsomes have high flavin-containing monooxygenase levels, & this enzyme is important relative to cytochrome p450 in these tissues. Thioether-containing organophosphates are effective substrates for the flavin-containing monooxygenase in mouse liver microsomes, with Km values between 3.5 & 36 muM. Thioether-containing carbamates are less effective substrates having Km values near 280 muM. ... /Thioether-containing organophosphate & carbamate pesticides/
The ability of purified microsomal FAD-containing monooxygenase from mouse & pig liver to oxidize pesticides was investigated. The kinetic constants were determined for a number of pesticide substrates including thioether-containing organophosphorus cmpds, carbamates /thiofanox, methiocarb, aldicarb/ & (di)alkyldithiocarbamates. The thioether-containing organophosphorus cmpds were the best substances for both enzymes followed by the thioether-containing carbamates. The (di)alkyldithiocarbamates were relatively poor substrates for both pig & mouse liver microsomal FAD-containing monooxygenases.
来源:Hazardous Substances Data Bank (HSDB)
代谢
氨基甲酸酯通过肝脏酶促水解;降解产物通过肾脏和肝脏排出。
The carbamates are hydrolyzed enzymatically by the liver; degradation products are excreted by the kidneys and the liver. (L793)
Methiocarb is a cholinesterase or acetylcholinesterase (AChE) inhibitor. Carbamates form unstable complexes with chlolinesterases by carbamoylation of the active sites of the enzymes. This inhibition is reversible. A cholinesterase inhibitor suppresses the action of acetylcholine esterase. Because of its essential function, chemicals that interfere with the action of acetylcholine esterase are potent neurotoxins, causing excessive salivation and eye-watering in low doses. Headache, salivation, nausea, vomiting, abdominal pain and diarrhea are often prominent at higher levels of exposure. 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.
来源:Toxin and Toxin Target Database (T3DB)
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. Chronically high (>10 years) exposure leads to neuropsychological consequences including disturbances in perception and visuo-motor processing (A15321).
来源:Toxin and Toxin Target Database (T3DB)
毒理性
暴露途径
这种物质可以通过摄入和透过皮肤被身体吸收。
The substance can be absorbed into the body by ingestion and through the skin.
来源:ILO-WHO International Chemical Safety Cards (ICSCs)
In dermal toxicity studies, methiocarb was not readily absorbed via the skin, even in solvents expected to enhance dermal absorption. In a cow given 5 daily doses of ring-labeled methiocarb, radioactivity in the milk (due to methiocarb sulfoxide) peaked at 0.062 ppm after the third dose. Tissue residues were highest in the kidney (0.108 ppm) & liver (0.073 ppm); levels in other tissues did not exceed 0.02 ppm. Following subchronic dietary exposure of beef & dairy cattle to methiocarb, residues exceeded 0.005 ppm only in the liver (at dosages of 30 ppm or higher) & the kidney (at a dosage of 100 ppm); residues were not detected in the brain, heart, muscle, or fat. Milk collected on exposure days 28 & 29 contained methiocarb residues ranging from 0.005 ppm (at a dosage of 10 ppm) to 0.033 ppm (at a dosage of 100 ppm).
Of a single dose of carbonyl-labeled methiocarb to rats, more than 60% was eliminated as expired 14 CO2. In another study, about 66% was eliminated as 14 CO2, about 22% in the urine, & 2.5% in the feces; elimination was about 91% complete. Ring-labeled methiocarb was excreted almost entirely in the urine within 48 hr. Of a ring-labeled dose of methiocarb to a dairy cow, 96% appeared in the urine, 1% in the feces, and 1% in the milk within 144 hr.
来源:Hazardous Substances Data Bank (HSDB)
吸收、分配和排泄
在狗和老鼠中,口服给药后,甲硫羰基迅速被吸收并排出,主要在尿液中,只有一小部分在粪便中。
In dogs & mice, following oral admin, methiocarb is rapidly absorbed & excreted, principally in the urine, with only a small proportion in the feces.
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] 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.