Pirimicarb's major urinary metabolites in rats, dogs, & cows were similar, resulting from oxidative & hydrolytic mechanisms & consisting primarily of hydroxypyrimidines with modifications of the alkyl constituents of the heterocyclic moiety. Of the administered dose, 2-dimethylamino-5,6-dimethyl-4-hydroxypyrimidine accounted for 10-16.3%, 2-methylamino-5,6-dimethyl-4-hydroxypyrimidine for 20.5-41%, 2-amino-5,6-dimethyl-4-hydroxypyrimidine for 12.9-21%, & 2-dimethylamino-6-hydroxymethyl-5-methyl-4-hydroxypyrimidine for 1.8-5.7%. The major metabolites were eliminated unconjugated.
... During ... metabolism /of pirimicarb/ in mammals the carbamate moiety is hydrolyzed & subsequent demethylation at the dimethylamino group which is attached to the heterocyclic moiety results in the following major metabolites which are excreted in urine: 2-dimethylamino-5,6-dimethyl-4-hydroxypyrimidine (DDHP), 2-methylamino-5,6-dimethyl-4-hydroxypyrimidine (MDHP), & 2-amino-5,6-dimethyl-4-hydroxypyrimidine (ADHP). These metabolites were detected in every urine sample of seven workers who had applied pirimicarb. Concns of the 2-methylamino-5,6-dimethyl-4-hydroxypyrimidine & 2-amino-5,6-dimethyl-4-hydroxypyrimidine were much higher than that of 2-dimethylamino-5,6-dimethyl-4-hydroxypyrimidine indicating a considerable demethylation capacity in humans. No metabolites were found in urine specimens of controls. The investigated pyrimidines represent sensitive & specific parameters for biological monitoring of exposure to pirimicarb.
来源:Hazardous Substances Data Bank (HSDB)
代谢
甲酰胺通过肝脏酶促水解;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)
Pirimicarb 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
致癌物分类
对人类不具有致癌性(未被国际癌症研究机构IARC列名)。
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).
In rats given carbonyl-labeled [14C]pirimicarb by gavage or ip injection, >50% of the dose was expired as 14CO2 within 5 hr, & 15% was eliminated in the urine; essentially no residues were detected at sacrifice 8 days after admin. Up to 4 daily admins of pirimicarb to rats resulted in no accumulation in adipose tissue. In dogs, 86-94% of a ring-14C-labeled dose of pirimicarb was recovered, 79-88% in the urine & 6-7% in the feces; recovery was 74-86% after 1 day. Of a carbonyl-labeled dose to dogs, 15-26% was recovered, primarily in the urine; the unrecovered portion was thought to be expired rapidly as 14CO2. Of pirimicarb admin to a lactating dairy cow, 96% of the dose appeared in the urine, 4% in the feces, & <0.3% in the milk.
Mode of action: Selective systemic insecticide with contact, stomach, and respiratory action. Absorbed by the roots, and translocated through the xylem. Penetrates the leaves, but is not translocated extensively.
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.