Imazamox is a racemic mixture. No information on chiral conversion in the mammalian metabolism or toxicity of specific enantiomer is available. However, information available in the fate and behaviour and residues section indicated that chiral conversion does not occur and exposure would be only to the racemic mixture.
来源:Hazardous Substances Data Bank (HSDB)
代谢
Forty-four Sprague Dawley rats (5/sex/group) were dosed with (14)C-imazamox... Three components accounted for about 99% of the total urinary radioactivity (98.2%, parent; 0.6%, 5-hydroxymethyl-nicotinic acid metabolite; and 0.4%, 5-carboxy-nicotinic acid metabolite) and about 89% of the extractable radioactivity in the feces (76.4%, parent; 9.6%, 5-hydroxymethyl-nicotinic acid metabolite; and 2.5%, 5-carboxy-nicotinic acid metabolite). The radioactive residues in the tissues were low (<0.007%), and no (14)C-residues were detected in the expired air.
Forty-four Sprague Dawley rats (5/sex/group) were dosed with (14)C-/imazamox/ ...Three components accounted for ca. 99% of the total urinary radioactivity (98.2%, parent; 0.6%, 5- hydroxymethyl-nicotinic acid metabolite; and 0.4%, 5-carboxy-nicotinic acid metabolite) and ca. 89% of the extractable radioactivity in the feces (76.4%, parent; 9.6%, 5-hydroxymethyl-nicotinic acid metabolite; and 2.5%, 5-carboxy-nicotinic acid metabolite). The radioactive residues in the tissues were low (<0.007%), and no (14)C-residues were detected in the expired air.
(14)C-(15)N-labelled/unlabelled imazamox mix was incubated with dog, rabbit, rat, mouse or human liver microsomes in the presence of a nicotinamide adenine dinucleotide phosphate (NADPH)-generating system. With 90% recovered radioactivity and above, only the parent molecule was detected in all test systems by high-performance liquid chromatographic analysis in fresh samples after the incubation. Under the conditions of the study, imazamox was not metabolized by liver microsomes of dogs, rabbits, rats, mice or humans. No unique human metabolite was detected. Under the conditions of the study, the positive control, testosterone, was metabolized by the microsome samples originating from different species.
In rats, imazamox was rapidly absorbed, and the oral absorption was approximately 75% of the administered dose. Urine was the major route of excretion (>74%). Most of the elimination occurred within the first 24 hours after dosing, as unchanged parent compound. Smaller amounts of the test substance were excreted through faeces (>19% in animals receiving 10 mg/kg bw and approximately 10-20% in animals receiving 1000 mg/kg bw). Only trace amounts of tissue residue were detected. Imazamox appears not to be metabolized. Trace levels of imazamox-related compounds detected in the urine and faeces were attributed to the presence of impurities in the dosing solution, not to rat metabolism.
IDENTIFICATION AND USE: Imazamox is off-white powdered solid. It is a herbicide applied post-emergence in soybean. HUMAN STUDIES: In an in vitro study, human embryonic stem cells were treated with imazamox at a concentration of 0, 1, 10 or 100 umol/L, incubation did not induce cytotoxicity. ANIMAL STUDIES: In the acute toxicity studies, the substance has low acute toxicity when administered orally, dermally or by inhalation to rats. It is not a significant skin or eye irritant or a skin sensitizer. Imazamox showed no short-term and long-term toxicity after oral exposure to rats, mice and dogs up to the limit top dose level tested in each study. Based on available genotoxicity studies imazamox is unlikely to be genotoxic. The substance showed no carcinogenic potential in both species. In the multigeneration toxicity study, fertility and overall reproductive performance was not impaired. In developmental toxicity studies maternal toxicity in rats and in rabbits was observed. No developmental toxicity was observed in rats whereas agenesis of the intermediate lobe of lung and cervical hemivertebra was observed in rabbits. ECOTOXICITY STUDIES: Imazamox is practically nontoxic to avian species, finfish, aquatic invertebrates, and honeybees following acute exposure.
来源:Hazardous Substances Data Bank (HSDB)
毒理性
致癌性证据
癌症分类:不太可能对人类致癌
Cancer Classification: Not likely to be carcinogenic to humans
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).
来源:Toxin and Toxin Target Database (T3DB)
毒理性
毒性数据
LC50 (大鼠) > 6,300 毫克/立方米
LC50 (rat) > 6,300 mg/m3
来源:Haz-Map, Information on Hazardous Chemicals and Occupational Diseases
Immediate first aid: Ensure that adequate decontamination has been carried out. If patient is not breathing, start artificial respiration, preferably with a demand valve resuscitator, bag-valve-mask device, or pocket mask, as trained. Perform CPR if necessary. Immediately flush contaminated eyes with gently flowing water. Do not induce vomiting. If vomiting occurs, lean patient forward or place on the left side (head-down position, if possible) to maintain an open airway and prevent aspiration. Keep patient quiet and maintain normal body temperature. Obtain medical attention. /Poisons A and B/
来源:Hazardous Substances Data Bank (HSDB)
吸收、分配和排泄
植物吸收:吸收通过叶子和根部进行。
Plant absorption: Absorption occurs through both the foliage and roots.
Forty-four Sprague Dawley rats (5/sex/group) were dosed with (14)C-/imazamox/ by a single intravenous (iv) dose at 10 mg/kg or a single oral gavage dose according to the following regiments: (1) 10 mg/kg body weight; (2) 14-day preconditioning with 10 mg/kg non-radiolabelled /imazamox/, followed by 10 mg/kg (14)C-/imazamox/; or (3) 1000 mg/kg body weight. The elimination patterns indicated that the radioactive residue were rapidly cleared from the body (ca. 95%) excreted in urine and recovered within 12 hours after dosing for all dose groups. Approximately, 74-75% of the radioactivity was absorbed via oral administration at 10 mg/kg dose and 74.4-74.5% excreted in urine and 18.7- 24.0% in feces. Much higher proportion of the dose was excreted in feces following oral dose (18.7- 24.0%) compared to iv injection (1.9-2.7%), most likely due to incomplete absorption. Three components accounted for ca. 99% of the total urinary radioactivity (98.2%, parent; 0.6%, 5- hydroxymethyl-nicotinic acid metabolite; and 0.4%, 5-carboxy-nicotinic acid metabolite) and ca. 89% of the extractable radioactivity in the feces (76.4%, parent; 9.6%, 5-hydroxymethyl-nicotinic acid metabolite; and 2.5%, 5-carboxy-nicotinic acid metabolite). The radioactive residues in the tissues were low (< 0.007%), and no (14)C-residues were detected in the expired air.
来源:Hazardous Substances Data Bank (HSDB)
吸收、分配和排泄
在大鼠中,甲氧咪唑迅速被吸收,口服吸收率约为给药剂量的75%。尿液是主要的排泄途径(>74%)。
In rats, imazamox was rapidly absorbed, and the oral absorption was approximately 75% of the administered dose. Urine was the major route of excretion (>74%).
[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] 3-[(HYDRAZONO)METHYL]-N-(TETRAZOL-5-YL)-BENZAMIDE AND 3-[(HYDRAZONO)METHYL]-N-(1,3,4-OXADIAZOL-2-YL)-BENZAMIDE DERIVATIVES AS HERBICIDES<br/>[FR] DÉRIVÉS DE 3-[(HYDRAZONO))MÉTHYL]-N-(TÉTRAZOL-5-YL)-BENZAMIDE ET DE 3-[(HYDRAZONO)MÉTHYL]-N-(1,3,4-OXADIAZOL-2-YL)-BENZAMIDE UTILISÉS EN TANT QU'HERBICIDES
申请人:SYNGENTA CROP PROTECTION AG
公开号:WO2021013969A1
公开(公告)日:2021-01-28
The present invention related to compounds of Formula (I): or an agronomically acceptable salt thereof, wherein Q, R2, R3, R4, R5 and R6 are as described herein. The invention further relates to compositions comprising said compounds, to methods of controlling weeds using said compositions, and to the use of compounds of Formula (I) as a herbicide.
[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.