AFTER TREATMENT OF GROWING BEAN LEAVES WITH LABELED MATACIL, @ LEAST 8 COMPOUNDSWERE DETECTED. OF THESE, 4 ... IDENTIFIED AS 4-FORMAMIDO-, 4-METHYLFORMAMIDO-, 4-AMINO, & 4-METHYLAMINO-3-CRESYLMETHYLCARBAMATES.
AFTER EXPOSURE OF FLIES TO LABELED MATACIL, (14)CO2 AROSE THROUGH N-DEALKYLATION& HYDROLYSIS TO RESPECTIVE PHENOL & METHYLCARBAMIC ACID. LATTER DECOMP TO CO2 VIA FORMATE ... INCUBATION ... WITH FLY HOMOGENATES & NADPH2 GAVE RISE TO 4-FORMAMIDO-, 4-METHYLFORMAMIDO-, 4-AMINO-, & 4-METHYLAMINO-3-CRESYL METHYLCARBAMATES.
WHEN LABELED MATACIL WAS ADMIN TO RATS, (14)CO2 WAS OBSERVED. AFTER INCUBATION WITH RAT LIVER MICROSOME-NADPH SYSTEM, MATACIL WAS DEGRADED TO N-HYDROXYMETHYL MATACIL, 4-AMINO-3-CRESYL N-METHYLCARBAMATE, 4-METHYLAMINO-3-CRESYL N-METHYLCARBAMATE.
Aminocarb 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
这种物质可以通过皮肤接触和摄入被身体吸收。
The substance can be absorbed into the body through the skin and by ingestion.
来源:ILO-WHO International Chemical Safety Cards (ICSCs)
Uptake and clearance of aminocarb by Caecidolea racovitzai racovitzai were shown to be proportional to exposure temp, indicating that they may be active processes. Control of clearance may be a function of the rate of metab of aminocarb in vivo. Both uptake and clearance were shown to occur in two compartments.
Novel thienylpyridylcarboxamides of the formula (I)
The present application is also directed to a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and also novel intermediates and their preparation.
Compounds of formula I
wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula I can be used as insecticides and can be prepared in a manner known per se.