The metabolism of triflumizole was investigated by analyzing fecal and urine samples retained from ... previous studies: single oral administration of 10 or 300 mg/kg bw and 14 consecutive oral doses of 10 mg/kg bw per day. ... Triflumizole is extensively metabolized: less than 2% of the radiolabel recovered from urine or feces was identified as parent compound. A few differences in metabolite pattern were observed between males and females after repeated low and single high doses, but not after a single low dose. The major urinary metabolites are the sulfate conjugates of FM-8-1 and FA-1-5, each representing approximately 20% of the radiolabel recovered after the single low dose from that matrix and, respectively, approximately 11% and 20% after the high dose. In feces, FD-2-1 is a major metabolite in all dose regimens (~6-10% of the recovered radiolabel). Considerable differences between dose regimens exist with respect to other major metabolites. FM-2-1 is the major metabolite after a single oral low dose (~9% of radiolabel recovered in feces), but represents less than 2% for the other dose regimens. FA-1-1 is a major metabolite after single and repeated low dosing (~5-10%), but not after single oral high dosing (<3%), whereas FD-1-1 is the major metabolite after a single oral high dose (~16%) and a minor metabolite after single and repeated low doses (<2%). The metabolite FM-6-1 was tentatively identified by TLC co-chromatography, and the radioactive band corresponding to the authentic FM-6-1 was obscure, because of its low radioactivity.
IDENTIFICATION AND USE: Triflumizole is a fungicide used for the control of powdery mildew, such as Sphaerotheca fuliginea, Sphaerotheca pannosa, Erysiphe cichoracearum, and others. HUMAN EXPOSURE AND TOXICITY: A report on the results of its yearly health examination of the personnel involved in the production of triflumizole at the Takaoka plant (Japan) during the period May 1996 to May 2002 was published. No adverse health effects attributable to chemical exposure were observed. In addition, it was reported that in the period covered, no events of acute poisoning by exposure or skin and/or eye irritation were observed. Repeated or prolonged contact may cause skin sensitization. The substance may have effects on the liver and blood. This may result in liver impairment and a decrease in hemoglobin. ANIMAL STUDIES: Triflumizole is sensitizing to the skin of guinea pigs. It is mildly irritating to the eye of rabbits. An acute inhalation toxicity test for triflumizole was conducted in rats. Symptoms of toxicity included hunched posture, lethargy and chromodacryorrhoea (head and/or snout) among the majority of the animals. Signs of oral toxicity from triflumizole observed in rats included ataxia, hypotonia, ventral position, lacrimation, urinary incontinence, decreased body temperature, decreased heart rate and respiration rate, and ptosis. Triflumizole did not produce tumors in rats after 104 weeks of treatment. In developmental studies in rats no statistically significant treatment-related external, visceral, or skeletal malformations or variations were noted. In a mouse study, prenatal triflumizole exposure increases adipose depot weight and diverts mesenchymal stromal stem cells fate toward the adipocyte lineage. Triflumizole was not mutagenic in the Ames test with or without metabolic activation. ECOTOXICITY STUDIES: Using rare minnow (Gobiocypris rarus) at early-life stages, the developmental toxicity of five widely used triazole fungicides including triflumizole was rated as highly toxic.
Triflumizole is classified as not likely to be carcinogenic to humans, based on the lack of evidence of carcinogenicity in studies in rats and mice and the absence of a mutagenicity concern.
In human, a neuromuscular impairment and decreased locomotor activity were observed following a single exposure of 100 mg/kg/day. The liver is the primary target organ of triflumizole in the rat, mouse, and dog. It increased liver weight, hepatocyte fatty vacuolization, hypertrophy, inflammation, fatty degeneration, and caused necrosis. Chronic effects of triflumizole included hepatocyte fatty vacuolization, hepatocyte hypertrophy, focal inflammation, and necrosi,; fatty degeneration, eosinophilic foci of hepatocyte alteration, hepatic nodules, bile duct hyperplasia, and hyaline degeneration/fibrosis of the bile duct. Liver effects were seen in rat and mouse subchronic and chronic/carcinogenicity studies. The fetal effects were also seen in rats. Triflumizole has a reproductive toxicity as well, the gestation length was increased in rats receiving high dose of triflumizole.
来源:Toxin and Toxin Target Database (T3DB)
毒理性
暴露途径
该物质可以通过吸入灰尘和摄入的方式被身体吸收。
The substance can be absorbed into the body by inhalation of dust and by ingestion.
来源:ILO-WHO International Chemical Safety Cards (ICSCs)
Following oral treatment of rats with /a single oral dose of 10 mg/kg/ [phenyl- U-(14)C]-NF-114, no sex-related differences were observed in absorption, metabolism, distribution or excretion. Maximum concentrations of radioactivity in plasma were attained within 1 hour of dosing in both sexes. Low levels of radioactivity were detectable in all tissue, organ, and blood samples. Radioactivity in urine accounted for 69.5-74.4% of the dose and feces accounted for 21.7-21.9% of the dose. /From table/
M&F: 10 or 300 mg/kg as single oral dose: Following oral treatment of rats with [phenyl- U-(14)C]-NF-114, approximately 93.8-100.6% of the administered dose was recovered. Urine was the major route of excretion. Low levels of radioactivity were detectable in all tissue, organ, and blood samples collected 2 days (10 mg/kg group) or 4 days (300 mg/kg group) post-dose with tissue concentrations generally higher in males than females. The metabolite profile in the excreta was quantitatively and qualitatively similar between the sexes and dose groups. /From table/
N-ARYLAMIDINE-SUBSTITUTED TRIFLUOROETHYL SULFIDE DERIVATIVES AS ACARICIDES AND INSECTICIDES
申请人：BAYER CROPSCIENCE AG
公开号：US20140315898A1
公开（公告）日：2014-10-23
The present invention relates to novel N-arylamide-substituted trifluoroethyl sulfide derivatives of the formula (I)
in which X
1
, X
2
, X
3
, X
4
, R
1
, R
2
, R
3
, n have the meanings given in the description—to their use as acaricides and insecticides for controlling animal pests and to processes and intermediates for their preparation
Compounds of the formula I Formula (I) wherein the substituents are as defined in claim 1, are useful as active ingredients, which have microbiocidal activity, in particular fungicidal activity.
ARYL SULFIDE DERIVATIVES AND ARYL SULFOXIDE DERIVATIVES AS ACARICIDES AND INSECTICIDES
申请人：BAYER CROPSCIENCE AKTIENGESELLSCHAFT
公开号：US20160145235A1
公开（公告）日：2016-05-26
The present invention relates to aryl sulphide and aryl sulphoxide derivatives, to the use thereof as acaricides and insecticides for controlling animal pests and to processes and intermediates for preparation thereof. The aryl sulphide and aryl sulphoxide derivatives have the general structure (I)
in which the respective radicals are as defined in the description.
