Moderately soluble in acetone, cyclohexanone, N,N-dimethylformamide (400–450 g/kg), and
isophorone (Windholz et al., 1983; Worthing and Hance, 1991)
暴露限值:
NIOSH REL: TWA 5 mg/m3, IDLH 100 mg/m3; OSHA PEL: TWA 5
mg/m3; ACGIH TLV: TWA 5 mg/m3.
物理描述:
Carbaryl appears as a white crystalline solid. Insoluble in water. Combustible, although difficult to ignite. Toxic by inhalation (dust, etc.). Produces toxic oxides of nitrogen during combustion.
Sevin, labeled with (14)C, is metabolized in insects, in rat, and by microsomal prepn of mouse, rat & rabbit liver, by aromatic hydroxylation, n-methyl hydroxylation, hydrolysis of carbamyl grouping, & by conjugation.
Of the metabolites identified in livestock commodities, five are considered significant ... : carbaryl; 5,6-dihydro-5,6-dihydroxy carbaryl; and 5-methoxy-6-hydroxy carbaryl and all residues which can be hydrolyzed to carbaryl, 5,6-dihydro-5,6-dihydroxy carbaryl, or 5-methoxy-6-hydroxy carbaryl under acidic conditions. The /EPA/ included these compounds in the dietary risk assessment for carbaryl, and in the reassessment of carbaryl tolerances for livestock commodities only.
Single oral dose of carbaryl was admin to rats. After extraction of ... urine, column & TLC chromotography, tentative identification was made for 1,5-naphthalenediol with small amt of carbaryl, 5-hydroxycarbaryl, & trace of n-hydroxymethylcarbaryl was also present. A major metab ... identified as 5,6-dihydro-5,6-dihydroxycarbaryl, was found free (1.4% of the dose) & as the glucuronide (10.5% of the dose). Naphthyl glucuronide & sulfate were also observed.
In urine of rats in addn to 1-naphthol, 1-naphthyl methylcarbamate N-glucuronide, 1-naphthyl methylimido-carbonate O-glucuronide, 4-(methylcarbamoyloxy)-1-naphthyl glucuronide, 1-naphthyl glucuronide, 1-naphthyl sulfate, 4-(methylcarbamoyloxy)-1-naphthyl sulfate, 3 unidentified cmpd & cmpd believed to be 1-naphthyl N-hydroxymethylcarbamate were observed. Similar results were observed with guinea pigs.
来源:Hazardous Substances Data Bank (HSDB)
代谢
卡巴立尔已知的人类代谢物包括4-羟基卡巴立尔、5-羟基卡巴立尔和卡巴立尔甲基酚。
Carbaryl has known human metabolites that include 4-hydroxycarbaryl, 5-hydroxycarbaryl, and carbaryl methylol.
Food represents the major source of carbaryl intake for the general population. ... The general population can be exposed to carbaryl during pest control operations in both the home & recreation areas. Workers can be exposed to carbaryl during its manufacture, formulation, packing, transportation, storage, & during & after application. ... Significant dermal exposure may occur in industrial & agricultural workers if protective measures are inadequate. Carbaryl is rapidly absorbed in the lungs & digestive tract. ... The principal metabolic pathways of carbaryl are ring hydroxylation & hydrolysis. As a result, numerous metabolites are formed & subjected to conjugation with the formation of water-soluble sulfates, glucuronides, & mercapturates, excreted in the urine. Hydrolysis results in the formation of 1-naphthol, carbon dioxide & methylamine. Hydroxylation produces 4-hydroxycarbaryl, 5-hydroxycarbaryl, N-hydroxymethylcarbaryl, 5-6-dihydro-5-6-dihydroxycarbaryl & 1,4-naphthalendiol. The principal metabolite in humans is 1-naphthol. Under normal exposure conditions, the accumulation of carbaryl in animals is unlikely. Carbaryl is excreted primarily via the urine, since the product of its hydrolysis, 1-naphthol, is mainly detoxified to water-soluble conjugates. Enterohepatic cycling of carbaryl metabolites is also considerable, especially after oral administration. ... Carbaryl metabolites are also present in a small percentage of the absorbed doses in saliva & milk. ... The acute toxicity for birds is low. ... Carbaryl is very toxic for honey-bees & earthworms. ... The acute toxicity ... varies considerably according to species, formulation & vehicle. ... Carbaryl is a mild eye irritant & has little or no sensitizing potential. ... Carbaryl has a low cumulative potential. Carbaryl has been shown to affect mammalian reproduction & perinatal development adversely in a number of species. Effects on reproduction include impairment of fertility, decreased litter size, & reduced postnatal viability. Developmental toxicity is seen as increased in utero death, reduced fetal weight, & the occurrence of malformation. With the exception of a small number of studies, all adverse reproductive & developmental effects were noted only at doses that caused overt maternal toxicity, &, in a number of cases, the maternal animal was more sensitive to carbaryl than the conceptus. The maternal toxic effects included lethality, decreased growth, & dystocia. ...The available evidence indicates that carbaryl does not have any DNA-damaging properties. ... Negative results were obtained in tests for gene mutations in a large number of bacterial assays ... The available database does not support the presumption that carbaryl poses a risk of inducing genetic changes in ... humans. Carbaryl has been studied for its carcinogenic potential in numerous studies on rats & mice. The results of most of these studies were negative ... The effects of carbaryl on the nervous system are primarily related to cholinesterase inhibition & are usually transitory. ... Carbaryl has been reported to affect coagulation ... Carbaryl binds free blood amino acids. Disturbances have been reported in the carbohydrate metabolism & protein synthesis & detoxification function of the liver in mammals. Carbaryl is a weak inducer of hepatic microsomal drug-metabolizing activity. ... Carbaryl has been reported to incr the gonadotropic function of the hypophysis of rats. Carbaryl is an inhibitor of cholinesterase activity. This effect is dose-related & quickly reversible. ... All identified metabolites of carbaryl are appreciably less active cholinesterase inhibitors than carbaryl itself. Carbaryl is easily absorbed /in humans/ through inhalation & via the oral route & less readily by the dermal route. Since the inhibition of cholinesterase is the principal mechanism of carbaryl action, the clinical picture of intoxication is dominated by ... symptoms, such as: increased bronchial secretion, excessive sweating, salivation, & lacrimation; pinpoint pupils, bronchoconstriction, abdominal cramps (vomiting & diarrhea); bradycardia; fasciculation of fine muscles (in severe cases, diaphragm & respiratory muscles also involved); tachycardia; headache, dizziness, anxiety, mental confusion, convulsions, & coma; & depression of the respiratory center. Signs of intoxication develop quickly after absorption & disappear rapidly after exposure ends.... In cases of occupational overexposure to carbaryl, mild symptoms are observed long before a dangerous dose is absorbed, which is why severe cases of occupational intoxication with carbaryl are rare. During agricultural application, dermal exposure may play an important role. ... The appearance of a skin rash after accidental splashing with carbaryl formulations has been described. ... The most sensitive biological indicator of carbaryl exposure is the appearance of 1-naphthol in the urine & the decr of cholinesterase activity in the blood. ... The hazards of carbaryl for human beings are judged to be low, because of its low vapor pressure, rapid degradation , rapid spontaneous recovery of inhibited cholinesterase, & the fact that symptoms usually appear well before a dangerous dose has accumulated in the body. ...
Carbaril 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:可能对人类致癌
Cancer Classification: Likely to be Carcinogenic to Humans
来源:Hazardous Substances Data Bank (HSDB)
毒理性
致癌性证据
A4;不可归类为人类致癌物。
A4; Not classifiable as a human carcinogen.
来源:Hazardous Substances Data Bank (HSDB)
毒理性
致癌物分类
国际癌症研究机构致癌物:卡巴立尔
IARC Carcinogenic Agent:Carbaryl
来源:International Agency for Research on Cancer (IARC)
An in vitro dermal penetration study was conducted using both rat and human skin . This study showed that rat skin was 2.8 times more permeable to carbaryl than human skin.
Excretion--retention of ... carbaryl labeled in 3 different positions ... studied 48 hr after ip admin to rats. 65% of (14)C of carbonyl-(14)C-carbaryl was excreted in urine, 25% in expired air, 2% in feces, & 10% was retained ... highest levels of (14)C were present in liver, kidneys, heart, & corpuscles (erythrocytes & leukocytes). 58% of (14)C of n-methyl-(14)C-carbaryl was excreted in urine, 12% in expired air, 4% in feces, & 13% was retained ... (14)C was maximal in liver, kidneys, heart, lungs, & spleen, organs with high blood flow. 77% of (14)C of naphthyl-(14)C-carbaryl was excreted in urine, 9% in feces, & 7% was retained ... levels of (14)C in tissue were highest in kidneys, spleen, bone, & fat ... about 50% of (14)C had been excreted in 4 hr ... .
Of oral dose of (1-naphthyl-1-(14)C)-N-methylcarbamate given to rats, 53% & 82% were absorbed after 20 min & 1 hr, respectively. Carbaryl is absorbed very rapidly from lung, 2.5 times faster than from small intestine.
(14)C-carbaryl labeled in n-methyl group has been found in fetuses of pregnant rats, & mice. ... Autoradiographic study of (14)C-methyl-carbaryl in pregnant rat has shown that radiolabel was localized in eye, liver, & brain of fetus.
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.