Aldicarb appears as white crystals with a slightly sulfurous odor. Commercial formulations are granular Used as an insecticide, acaricide, and nematocide. (EPA, 1998)
颜色/状态：
Crystals from isopropyl ether
气味：
Slightly sulfurous odor
沸点：
Decomposes (NTP, 1992)
熔点：
99.0 °C
溶解度：
350 g/kg, acetone; 300 g/kg, dichloromethane; 150 g/kg, benzene; 150 g/kg, xylene; all at 25 °C
蒸汽压力：
2.9X10-5 mm Hg at 20 °C
稳定性/保质期：
Aldicarb is stable under normal storage conditions and in acidic media but decomposes rapidly in alkaline media and at temperatures above 100 °C.
分解：
... Decomposes rapidly in alkaline media & at temperatures above 100 °C.
Within 48 hours of administration of carbonyl-(14)C labelled aldicarb rats eliminated over 60% of the (14)C as carbon dioxide, less than 30% was found in the urine. In other (14)C-studies rats excreted more than 80% of the degradation products in urine and less than 10% in faeces (an excretion pattern favoured by enterohepatic cycling of glucuronides which may also serve to extend the systemic activity of the toxic metabolites). The major urinary metabolites were aldicarb sulfoxide (40% of the dose), its oxime and nitrile forms (over 30%); the sulfone and related oxime and nitrile; and, the aldehyde and acid analogues. Aldicarb is not commonly found in the excreta. Bound residues of ingested plant tissues are not absorbed and therefore are found in the faeces. In single dose and short-term diet studies, lactating cows eliminated aldicarb metabolites as rapidly as rats and in the same array of metabolites. Approximately 1% of the dose was excreted in the milk, sulfone and sulfoxide were the major metabolites at 15 and 4% of the total milk residue content respectively.
... Aldicarb is metabolized by both oxidative pathways and hydrolytic processes. Oxidation results in cmpd which are also active cholinesterase inhibitors, while hydrolysis produces cmpd of little or no insecticidal activity or toxicity to other organisms.
The major route of elimination of Temik-(35)S /aldicarb/ ... admin to lactating cow was by way of urine. Extracted and tentatively identified in milk were 11 compounds, incl temik sulfoxide and sulfone, oxime sulfoxide and sulfone, nitrile sulfoxide & sulfone, temik oxime, and 4 unidentified compounds. Metabolites identified in urine were qualitatively identical but differed quantitatively. Only 5 metabolites were identified in feces: temik oxime, oxime sulfoxide, temik sulfoxide, temik sulfone and nitrile sulfone.
In rats, sulfoxide accounted for 40% of dose /of aldicarb/ and sulfone for 1%; both ... are more potent anticholinesterases than aldicarb. Metabolite in cow's milk and urine was hydroxymethyl analogue of sulfone; two other bovine metabolites were 2-methyl-2-(methylsulfinyl)propanol and 2-methyl-2-(methylsulfonyl)propanol.
IDENTIFICATION: Aldicarb is a carbamate ester pesticide. It is a white crystalline solid, moderately soluble in water, and susceptible to oxidation and hydrolytic reactions. HUMAN EXPOSURE: Exposure of the general population to aldicarb and its toxic metabolites (the sulfoxide and sulfone) occurs mainly through food. The ingestion of contaminated food has led to poisoning incidents from aldicarb and its toxic metabolites (the sulfoxide and sulfone). Due to the high acute toxicity of aldicarb, both inhalation and skin contact under occupational exposure conditions may be dangerous for workers if preventive measures are inadequate. There have been a few incidents of accidental exposure of workers due to improper use or lack of protective measures. Aldicarb is efficiently absorbed from the gastrointestinal tract and, to a lesser extent, through the skin. It could be readily absorbed by the respiratory tract if dust were present. It is metabolically transformed to the sulfoxide and the sulfone (both of which are toxic), and is detoxified by hydrolysis to oximes and nitriles. The excretion of aldicarb and its metabolites is rapid and primarily via the urine. A minor part is also subject to biliary elimination and, consequently, to enterohepatic recycling. Aldicarb does not accumulate in the body as a result of long-term exposure. The inhibition of cholinesterase activity in vitro by aldicarb is spontaneously reversible, the half-life being 30-40 min. The inhibition of acetylcholinesterase at the nervous synapse and myoneural junction is the only recognized effect of aldicarb in humans and is similar to the action of organophosphates. The carbamyolated enzyme is unstable, and spontaneous reactivation is relatively rapid compared with that of a phosphorylated enzyme. Non-fatal poisoning in man is rapidly reversible. Recovery is aided by the administration of atropine. ANIMAL STUDIES: Aldicarb is a potent inhibitor of cholinesterases and has a high acute toxicity. Recovery from its cholinergic effects is spontaneous and complete within 6 hr, unless death results. There is no substantial evidence to indicate that aldicarb is teratogenic, mutagenic, carcinogenic, or immunotoxic. Birds and small mammals have been killed as a result of ingesting aldicarb granules not fully incorporated into the soil as recommended. In laboratory tests, aldicarb is acutely toxic to aquatic organisms.
Aldicarb 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.
Evaluation: No data were available from studies in humans. There is inadequate evidence for the carcinogenicity of aldicarb in experimental animals. Overall evaluation: Aldicarb is not classifiable as to its carcinogenicity to humans (Group 3).
来源:Hazardous Substances Data Bank (HSDB)
毒理性
致癌性证据
癌症分类：E组 人类非致癌性证据
Cancer Classification: Group E Evidence of Non-carcinogenicity for Humans
CLASSIFICATION: D; not classifiable as to human carcinogenicity. BASIS FOR CLASSIFICATION: Aldicarb was not found to induce statistically significant increases in tumor incidence in mice or rats in feeding studies or mice in a skin painting study. In the feeding studies there were, however, significant trends in pituitary tumors in female rats and fibrosarcomas in the male mouse. This evidence, together with the fact that less than maximum tolerated doses were used, indictes that the available assays are inadequate to assess the carcinogenic potential of aldicarb. HUMAN CARCINOGENICITY DATA: None. ANIMAL CARCINOGENICITY DATA: Inadequate. /Based on former classification system/
Male rats (Carworth Farms-Elias Stock) were treated orally or ip with labeled Temik in ethanol or Temik sulfoxide in water. Excretion of s-methyl-(14)C & tert-butyl-(14)C temik was completed, essentially, in 4 days. N-methyl-(14)C was excreted in urine & feces up to 11 days.
Aldicarb is readily absorbed from GI tract of treated animals. Excretion of radiolabeled cmpd admin to rats is primarily in urine, as approx 80% appears within 24 hr, with additional 1% in feces. Only traces of unchanged parent cmpd were found in excreta. When aldicarb is labeled on n-methyl carbon or carbonyl carbon large portion of radioactivity is found in expired air as (14)CO2. Very little aldicarb residues are found in tissues or carcasses of treated animals.
To measure the excretion of aldicarb admin repeatedly, dogs were maintained on diets determining an intake of 0.75 mg/dog/day for 20 days before & 10 days after being given a single (14)C-labeled dose. Of the radioactivity recovered in the urine, 90% was found within 24 hr after admin of the radiolabeled aldicarb.
Aldicarb is readily absorbed through the gut in rats and cows and through the skin in rats and rabbits. It is rapidly metabolized and excreted within 24 hours of exposure, almost all of the toxic and nontoxic metabolites being excreted in urine.
[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.
