The major metabolite in /the urine of/ rats was the des-S-phenyl hydrolysis product while in mice the mono-S-phenyl phosphorothioate was prevalent (further dealkylation of the major rat metabolite). In feces, small (< 2%) quantities of edifenphos were noted as well as diphenyl disulfide
...Edifenphos was degraded primarily by loss of the phenyl, thiophenyl and ethyl groups to give organophosphorus acids. The ultimate metabolites were phosphoric and sulfuric acids. Furthermore, oxidation and methylation were apparent in the later stage of metabolism, and conjugated metabolites were formed.
14C-Edifenphos was degraded in rice primarily by loss of phenyl, thiophenyl, and/or ethyl groups to give organophosphorus acids, the ultimate products being benzenesulfonic acid and presumably phosphoric acid.
Metabolism occurs principally by oxidation, hydrolysis by esterases, and by transfer of portions of the molecule to glutathione. Oxidation of organophosphorus insecticides may result in more or less toxic products. The glutathione transferase reactions produce products, that are, in most cases, of low toxicity. Hydrolytic and transferase reactions affect both thioates and their oxons. /Organophosphorus Pesticides/
来源:Hazardous Substances Data Bank (HSDB)
毒理性
副作用
其他毒物 - 有机磷
Other Poison - Organophosphate
来源:Haz-Map, Information on Hazardous Chemicals and Occupational Diseases
毒理性
毒性数据
大鼠LC50 = 650毫克/立方米/4小时
LC50 (rat) = 650 mg/m3/4h
来源:Haz-Map, Information on Hazardous Chemicals and Occupational Diseases
Because different classes of enzymes may be inhibited, the effects of organophosphorus pesticide poisoning may be complex and potentially at least could involve interactions with drugs as well as with other pesticides or chemicals. Potentiation may also involve solvents or other components of formulated pesticides. Certain drugs such a phenothiazines, antihistamines, CNS depressants, barbiturates, xanthines (theophylline), aminoglycosides and parasympathomimetic agents are to be avoided because of increased toxicity. /Organophosphorus pesticides/
Airway protection. Ensure that a clear airway exists. Intubate the patients and aspirate the secretions with a large-bore suction device if necessary. Administer oxygen by mechanically assisted pulmonary ventilation if respiration is depressed. Improve tissue oxygenation as much as possible before administering atropine, so as to minimize the risk of ventricular fibrillation. In severe poisonings, it may be necessary to support pulmonary ventilation mechanically for several days. /Organophosphate pesticides/
Atropine sulfate. Administer atropine sulfate intravenously, or intramuscularly if intravenous injection is not possible. Remember that atropine can be administered through an endotracheal tube if initial IV access if difficult to obtain. Depending on the severity of poisoning, doses of atropine ranging from very low to...high... . The objective of atropine antidotal therapy is to antagonize the effects of excessive concentrations of acetylcholine at end-organs having muscarinic receptors. Atropine does not reactivate the cholinesterase enzyme or accelerate disposition of organophosphate. Recrudescence of poisoning may occur if tissue concentrations of organophosphate remain high when the effect of atropine wears off. Atropine is effective against muscarinic manifestations, but it is ineffective against nicotinic actions, specifically muscle weakness and twitching, and respiratory depression. Despite the limitations, atropine is often a life-saving agent in organophosphate poisonings. Favorable response to a test dose of atropine can help differentiate poisoning by anticholinesterase agents from other conditions. However, lack of response, with no evidence of atropinization (atropine refractoriness) is typical of more severe poisonings. The adjunctive use of nebulized atropine has been reported to improve respiratory distress, decrease bronchial secretions, and increase oxygenation. ...Do not administer atropine or pralidoxime prophylactically to workers exposed to organophosphate pesticides. Prophylactic dosage with either atropine or pralidoxime may mask early signs and symptoms of organophosphate poisoning and thus allow the worker to continue exposure and possibly progress to more severe poisoning. Atropine itself may enhance the health hazards of the agricultural work setting: impaired heat loss due to reduced sweating and impaired ability to operate mechanical equipment due to blurred vision. This can be caused by mydriasis, one of the effects of atropine. /Organophosphate pesticides/
Edifenphos is rapidly absorbed following acute oral administration to rats. Within 8 hours of dosing the major part of an 35S-dose was absorbed. Within 72 hours of the administered dose, 96% in rats and > 97% in mice was excreted in the urine and feces. There were no significant sex differences noted in rats, while in mice females excreted somewhat more in the feces than corresponding males. Apart from this no sex differences in absorption and excretion were noted. Tissue residues (35S-labelled) in both rats and mice were extremely low at 72 hours. Residues in tissues following acute or sub-acute (10-daily) doses were generally low and associated with tissues concerned with distribution and excretion. Of the 6 tissues examined at various intervals after dosing (from 1 to 72 hours) the following sequence reflects tissue distribution: liver > kidney > lung > heart >> blood = brain. This same qualitative relationship of tissue distribution was reflected over the time for maximum tissue clearance.
Comparative studies on the metabolic fate of 35(S)-labeled edifenphos in rats and mice are described. Dose levels were 10 mg/kg in female rats and 20 mg/kg in mice and male rats. Only 15 to 30% of the administered radioactivity was detected in digestive organs 6 hr after administration. At 72 hr, only a trace amount of radioactivity was found over the whole body of the animals. The major part of the radioactivity was excreted via urine (75-90%) and feces (5-20%). The main metabolite of the rat is ethyl hydrogen S-phenyl phosphorothiolate (54-57%) and that of mice is dihydrogen S-phenyl phosphorothiolate (3 1-42%). Diphenyl disulfide was found in feces in both animals, but metabolites such as methyl phenyl sulfide and its derivatives were absent. Thus edifenphos is rapidly absorbed, metabolized and eliminated from mice and rats following oral administration.
[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.
[EN] SUBSTITUTED QUINAZOLINES AS FUNGICIDES<br/>[FR] QUINAZOLINES SUBSTITUÉES, UTILISÉES EN TANT QUE FONGICIDES
申请人：SYNGENTA PARTICIPATIONS AG
公开号：WO2010136475A1
公开（公告）日：2010-12-02
The present invention relates to a compound of formula (I) wherein wherein the substituents have the definitions as defined in claim 1or a salt or a N-oxide thereof, their use and methods for the control and/or prevention of microbial infection, particularly fungal infection, in plants and to processes for the preparation of these compounds.
