Benomyl is rapidly metabolized & eliminated in urine of rats & dogs as methyl-5-hydroxy-2-benzimidazole-carbamate (5HBC). Residue data on dog & rat tissues from 2 yr feeding studies indicate that benomyl & its metabolites do not accumulate in animal tissues.
ANALYSIS OF COMPOSITE URINE SAMPLES FROM RATS FED DUPONT FUNGICIDE 1991 WAS PERFORMED. METHYL S-HYDROXY-2-BENZIMIDAZOLECARBAMATE WAS FOUND AFTER ENZYME HYDROLYSIS TO LIBERATE GLUCURONIDE &/OR SULFATE CONJUGATES. IT WAS NOT DETERMINED WHETHER HYDROXYLATION OCCURRED PRIOR TO OR AFTER LOSS OF BUTYLCARBAMOYL GROUP ... .
In animal systems, benomyl is metabolized to carbendazim and other polar metabolites, which are rapidly excreted. ... The main source of exposure for the general human population is residues of benomyl and carbendazim in food crops. ... Agricultural workers engaged in pesticide mixing and loading or re-entering benomyl-treated fields are expected to be exposed dermally ... Since dermal absorption is expected to be low, the probability of benomyl having systemic toxic effects on human populations through this route is very low. Benomyl is readily absorbed in animal experiments after oral and inhalation exposure, but much less so following dermal exposure. Absorbed benomyl is rapidly metabolized and excreted in the urine and feces. ... Benomyl does not inhibit acetyl cholinesterase in vitro. It has been shown to induce liver epoxyhydrolase, gamma-glutamyl transpeptidase and glutathione-S-transferase in in vivo studies ... Benomyl has low acute toxicity ... in the rat ... Application to the skin of the rabbit and guinea pig produced either mild or no irritation and moderate skin sensitization. Application to the eyes of rats produced temporary mild conjunctival irritation. ... Benomyl causes a decrease in testis and epididymis weight, a reduction in caudal sperm reserves, a decrease in sperm production and a lowering of male fertility rates. At higher doses, there is hypospermatogenesis with generalized disruption of all stages of spermatogenesis. Benomyl does not affect copulatory behavior, seminal vesicles, sperm motility or related reproductive hormones. ... When administered via gavage ... benomyl was found to be teratogenic ... The effects were microphthalia, hydrocephaly, and encephaloceles. ... In mice, gavage dosing ... induced supernumerary ribs and other skeletal and visceral anomalies. ... Studies in somatic and germ cells show that benomyl does not cause gene mutations or structural chromosomal damage (aberrations) and it does not interact directly with DNA (causing DNA damage and repair). This has been demonstrated in both mammalian and non-mammalian systems. Benomyl does, however, cause numerical chromosome aberrations (aneuploidy and/or polyploidy) in experimental systems in vitro and in vivo. ... The biological effects of benomyl and carbendazim are thought to be the result of their interaction with cell microtubules. These structures are invovlved in vital functions, such as cell division, which is inhibited by benomyl and carbendazim. Benomyl and carbendazim toxicity in mammals is linked with microtubular dysfunction. Benomyl and carbendazim, like other benzimidazole compounds, display selective toxicity for species. This selectivity is, at least in part, explained by the different binding of benomyl and carbendazim to tubulins of target and non-target species. /In humans/ benomyl causes contact dermatitis and dermal sensitization. ... Both benomyl and carbendazim represent a very low risk for acute poisoning in humans. Given the current exposures and the low rate of dermal absorption of these two compounds, it is unlikely that they would cause systemic toxicity effects either in the general population or in occupationally exposed subjects.
来源:Hazardous Substances Data Bank (HSDB)
毒理性
毒性总结
Benomyl targets beta tubulin in actively dividing cells. It binds to microtubules, interfering with cell functions, such as meiosis and intracellular transportation (A15332). Benomyl binds to brain tubulin with a dissociation constant of 11.9 +/- 1.2 microM. Further, benomyl binds to a novel tubulin beta binding site, distinct from the well-characterized colchicine and vinblastine binding sites. Benomyl inhibits the polymerization of brain tubulin into microtubules, with 50% inhibition occurring at a concentration of 70-75 microM (A15103)
本尼米yl靶向活细胞中的β微管蛋白。它与微管结合,干扰细胞功能,如减数分裂和细胞内运输(A15332)。本尼米yl与脑微管蛋白结合,解离常数为11.9±1.2微米。此外,本尼米yl与一种新型的β微管蛋白结合位点结合,该位点与已知的秋水仙碱和长春碱结合位点不同。本尼米yl抑制脑微管蛋白聚合成微管,50%的抑制发生在70-75微米的浓度下(A15103)
Benomyl targets beta tubulin in actively dividing cells. It binds to microtubules, interfering with cell functions, such as meiosis and intracellular transportation (A15332). Benomyl binds to brain tubulin with a dissociation constant of 11.9 +/- 1.2 microM. Further, benomyl binds to a novel tubulin beta binding site, distinct from the well-characterized colchicine and vinblastine binding sites. Benomyl inhibits the polymerization of brain tubulin into microtubules, with 50% inhibition occurring at a concentration of 70-75 microM (A15103)
来源:Toxin and Toxin Target Database (T3DB)
毒理性
致癌性证据
癌症分类:C组可能的人类致癌物
Cancer Classification: Group C Possible Human Carcinogen
来源:Hazardous Substances Data Bank (HSDB)
毒理性
致癌性证据
A3:已确认的动物致癌物,对人类的相关性未知。
A3: Confirmed animal carcinogen with unknown relevance 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).
In a pretreated dog, >99% of the activity from (14)C benomyl was excreted in 72 hr, but in this species most of the excretion was by the feces. Mice excreted >94% of ingested benomyl within 96 hr. In mice, rabbits, & sheep, about 20% of the dose was excreted in conjugated form. In these 3 species, urine contained 44-71% & feces 21-46% of the excreted metabolites. ... Residue data on rat & dog tissues after 2 yr feeding studies demonstrated that benomyl & its metabolites do not accumulate in animal tissues.
来源:Hazardous Substances Data Bank (HSDB)
吸收、分配和排泄
在用含有(3)H MBC的苯菌灵处理后,大多数标签在3周后在叶子中被回收。
AFTER MELON PLANTS WERE TREATED WITH BENOMYL CONTAINING (3)H MBC, MOST OF LABEL WAS RECOVERED IN LEAVES AFTER 3 WK.
来源:Hazardous Substances Data Bank (HSDB)
吸收、分配和排泄
通过叶片和根部吸收,主要进行顶向运输。
Absorbed through the leaves & roots, with translocation principally acropetally.
Absorption in ChR-CD rats was monitored after dermal application of 0.1, 1, 10, & 100 mg benomyl (as 2-C14-Benlate 50 WP) at 0.5, 1, 2, 4 & 10 hr intervals. Benomyl was slowly absorbed across an area of skin (16% of the animal), appearing in the blood & urine within 30 min after treatment & reaching a max between 2 & 4 hr after dosing. The concn of benomyl & its metabolites in the blood peaked at 0.05 mg/liter (2 hr sample) in the low-dose group (0.1 mg) & at 0.1 mg/liter (4 hr sample) in the high-dose group (100 mg). This represented a 20-fold dose incr. Thus, absorption into the bloodstream was non-linear with respect to dose.
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.
[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.