SIGNIFICANT AMT OF N-HYDROXYMETHYLAMIDE ANALOG OF AZODRIN APPEARED FOLLOWING ADMIN TO RATS OF ... AZODRIN ... AND UNSUBSTITUTED AMIDE ... /WAS ALSO PRESENT/. IN RATS ADMIN AZODRIN ONLY TRACE AMT OF AZODRIN ACID WERE DETECTED IN EXTRACTS, INDICATING MINIMAL HYDROLYTIC DEGRADATION BY AMIDASE ACTION. DIMETHYL PHOSPHATE & O-DEMETHYL AZODRIN WERE MAJOR DEGRADATION PRODUCTS OF AZODRIN. IT WAS FELT THAT DEGRADATION FOLLOWED FORMATION OF N-HYDROXYMETHYL AZODRIN ... . THE FINDING OF ONLY TRACE AMOUNTS OF N-DEMETHYL AZODRIN & THE STABILITY OF THE PURE COMPOUND SEEMED TO INDICATE THAT DEMETHYLATION WAS MINOR REACTION.
来源:Hazardous Substances Data Bank (HSDB)
代谢
屋蝇和美洲蟑螂……代谢……偶氮氯磷形成N-羟基甲基和N-去甲基衍生物。
HOUSEFLIES & AMERICAN COCKROACHES ... METABOLIZED ... AZODRIN TO FORM N-HYDROXYMETHYL & N-DEMETHYLATED DERIVATIVES.
... ABSORBED AZODRIN WAS METABOLIZED MORE RAPIDLY IN HOUSEFLIES THAN IN WEEVILS. N-HYDROXYMETHYL AZODRIN WAS DETECTED AFTER 4-8 HR IN HOUSEFLIES BUT NOT UNTIL AFTER 24 HR IN WEEVILS. DIMETHYL PHOSPHATE WAS MAJOR HYDROLYSIS PRODUCT IN HOUSE FLIES; O-DEMETHYL AZODRIN PREDOMINATED IN WEEVILS.
来源:Hazardous Substances Data Bank (HSDB)
代谢
在植物中，N-羟基化合物以少量形成。
In plants, N-hydroxy compound is formed in small amounts.
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.
(E)-Monocrotophos 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
A4；不能归类为人类致癌物。
A4; Not classifiable as a human carcinogen.
来源:Hazardous Substances Data Bank (HSDB)
毒理性
致癌物分类
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)
毒理性
暴露途径
这种物质可以通过吸入、皮肤接触和摄入被身体吸收。
The substance can be absorbed into the body by inhalation, through the skin and by ingestion.
来源:ILO-WHO International Chemical Safety Cards (ICSCs)
GOATS TREATED ORALLY WITH ... AZODRIN EXCRETED IN URINE HIGH PROPORTION OF ADMIN ... N-METHYL (14)C LABEL. TRACE AMT OF ... AZODRIN, N-HYDROXYMETHYLAMIDE ANALOG OF AZODRIN, AND UNSUBSTITUTED AMIDE WERE PRESENT IN URINE. LABELED CMPD APPEARED IN GOAT MILK AFTER TREATMENT WITH ... (14)C-LABELED ... AZODRIN. ... TRACES OF N-HYDROXYMETHYLAMIDE & UNSUBSTITUTED AMIDE WERE ALSO PRESENT.
AFTER INJECTION INTO STEMS ... (32)P AZODRIN ... TRANSLOCATED IN BEAN PLANTS AND PERSISTED FOR SEVERAL WK UNDER GREENHOUSE CONDITIONS. ... TRACES OF N-HYDROXYMETHYLAMIDE & UNSUBSTITUTED AMIDE WERE PRESENT AT 8 DAYS BUT ONLY AZODRIN ... PRESENT AFTER 20 DAYS.
Excretion of radioactive phosphorus by rats injected ip with (32)P monocrotophos was rapid. In 6 hr, 45% was excreted, and in 24 hr, 58.4 and 5.1% had been recovered from urine and feces, respectively.
When radioactive monocrotophos was applied to human skin, the rate of excretion was maximal during the first 24-48 hr period, and it decr only slightly during the third and fourth days. A total of 14.7% of the radioactivity was recovered in the urine within 120 hr and only a small correction factor was involved.
[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.
