Male and female Sprague-Dawley rats received 200 and 2000 mg neat (14)C-DEGBE/kg bw and 200 mg of a 10% aqueous solution/kg bw. 2-(2-butoxyethanol)acetic acid was the major urinary metabolite identified and the glucuronide conjugate was present at levels of 5.2% to 8.2% of the urinary (14)C.
The metabolism of diethylene glycol monobutyl ether acetate was studied in vitro and in vivo in male Sprague-Dawley rats. The extent of conversion of diethylene glycol monobutyl ether acetate to diethylene glycol monobutyl ether was determined. In vitro, diethylene glycol monobutyl ether acetate was rapidly hydrolyzed by rat blood to diethylene glycol monobutyl ether; the biological half-life was less than 3 min. The urine was the major pathway for eliminating diethylene glycol monobutyl ether acetate derived (14)C activity; 80% was eliminated after 24 hr. Only 2 to 3% of each dose was eliminated in the feces. About 5% of each dose was eliminated in the expired air, mostly as radioactive carbon dioxide. Only 1-3% doses were found in the tissues and ied. No unchanged diethylene glycol monobutyl ether acetate or diethylene glycol monobutyl ether or 2-butoxyacetic acid, a putative hematotoxic diethylene glycol monobutyl ether acetate metabolite, was found. Diethylene glycol monobutyl ether acetate is rapidly hydrolyzed to diethylene glycol monobutyl ether by rat blood. The biological effects of diethylene glycol monobutyl ether acetate and diethylene glycol monobutyl ether would be indistinguishable. No 2-butoxyacetic acid is produced.
In the present study, floor lacquerers' (n = 22) inhalation and total exposure to 2-(2-alkoxy)ethoxyethanols was measured. The measurements of inhalation exposure were done with charcoal tubes, and total exposure was biomonitored by urinalysis of 2-(2-alkoxyethoxy)acetic acids. The 8hr inhalation exposures of floor lacquerers to 2-(2-methoxyethoxy)ethanol (DEGME), 2-(2-ethoxyethoxy)ethanol (DEGEE) and 2-(2-butoxyethoxy)ethanol (DEGBE) were in average 0.23 +/- 0.07 ppm (average+/-S.D., n = 3), 0.08 +/- 0.07 ppm (n = 16), and 0.05 +/- 0.03 ppm (n = 16), respectively. The excretions of 2-(2-methoxyethoxy)acetic acid (MEAA), 2-(2-ethoxyethoxy)acetic acid (EEAA) and 2-(2-butoxyethoxy)acetic acid (BEAA) were in average 4.9 +/- 4.3 mmol/mol creatinine, 9.3 +/- 8.0 mmol/mol creatinine and 9.2 +/- 7.4 mmol/mol creatinine, respectively. A linear relationship was found between the urinary 2-(2-alkoxyethoxy)acetic acid concentrations and the preceding 8-hr occupational exposure to 2-(2-alkoxyethoxy)ethanol. /2-(2-Alkoxyethoxy)ethanol/
来源:Hazardous Substances Data Bank (HSDB)
毒理性
毒性总结
二乙二醇单正丁醚（DGBE）是一种无色液体，具有淡的正丁基气味。它被用作一种惰性成分，目前在美国没有注册用作杀虫剂，但在杀虫剂产品中使用。它还用作乳胶涂料的凝聚剂；印台墨水的溶剂；染料溶剂；高温烤漆的溶剂；分散剂；液压制动液的稀释剂；以及家用清洁剂中肥皂、油和水的相互溶剂。人类暴露和毒性：二乙二醇的醚类毒性低于乙二醇的醚类，但它们具有许多相似的特征。暴露于一些乙二醇和二乙二醇醚衍生物可能会引起中枢神经系统抑制，无低钙血症性手足搐搦或代谢性酸中毒，恶心，呕吐，有时腹泻，头痛，后期腹部和腰痛，肋椎角压痛，暂时多尿然后少尿，发展为无尿，急性肾衰竭，并且在大脑、肺、肝、脑膜和心脏可能出现病理病变。动物研究：动物观察表明，至少对于一些乙二醇和二乙二醇醚衍生物，可能会出现肺水肿、血管内溶血和骨髓抑制。在350毫克/立方米和1000毫克/立方米的DGBE蒸气或气溶胶中暴露2周的大鼠，雄性大鼠的脾脏重量减轻。观察到所有处理组的肺部出现包括血管周围和支气管周围粒细胞积聚以及最小的支气管化在内的组织病理学变化。当通过灌胃给予大鼠DGBE时，DGBE确实引起了轻度溶血，在13周的大鼠饮水研究中，当以100毫克/千克/天的DGBE给药时，观察到红细胞计数、血红蛋白和血细胞比容的减少。DGBE对大鼠的子代在出生前和出生后发育没有不良影响。基于行为和组织病理学评估，DGBE的皮肤应用不会导致神经毒性。DGBE不具有致突变性，在沙门氏菌typhimurium TA 98、TA 100、TA 1535、TA 1537和TA 1538以及果蝇的性别连锁隐性致死突变试验中，无论是否进行代谢激活，Ames反向突变试验均为阴性。
IDENTIFICATION AND USE: Diethylene glycol mono-n-butyl ether (DGBE) is a colorless liquid with a faint butyl odor. It is used as an inert ingredient that is not registered for current use as a pesticide in the U.S., but is used in pesticide products. It is also used as a coalescing agent in latex paints; solvent for stamp pad inks; dye solvent; solvent in high baked enamels; dispersant; diluent for hydraulic brake fluids; and a mutual solvent for soap, oil, and water in household cleaners. HUMAN EXPOSURE AND TOXICITY: The ethers of diethylene glycol are lower in toxicity than the ethers of ethylene glycol, but they have many similar characteristics. Exposure to some ether derivatives of ethylene and diethylene glycols can cause central nervous depression, no hypocalcemic tetany or metabolic acidosis, nausea, vomiting, & sometimes diarrhea, headache, later abdominal and lumbar pain, costovertebral angle tenderness, transient polyuria & then oliguria, progressing to anuria, acute renal failure, and pathological lesions may appear in brain, lung, liver, meninges & heart. ANIMAL STUDIES: Observations in animals suggest a possibility of pulmonary edema, intravascular hemolysis and bone marrow depression, at least with some ether derivative of ethylene and diethylene glycols. Rats exposed to DGBE vapor or aerosol (350 and 1000 mg/ cu m) for 2-weeks had a reduction of spleen weight in males. Histopathological changes including perivascular and peribronchial accumulation of granulocytes as well as minimal bronchiolization in the lungs were observed in all treatment groups. DGBE did cause mild hemolysis when administered to rats by gavage and a reduction in red blood cell count, hemoglobin, and hematocrit was seen when 100 mg/kg/day of DGBE was administered in a 13-week drinking study in rats. DGBE had no adverse effects on the pre- and postnatal development of the offspring in rats. Dermal application of DGBE does not result in neurotoxicity based on behavioral and histopathological evaluations. DGBE is not genotoxic, testing negative in the Ames reverse mutation assay with Salmonella typhimurium TA 98, TA 100, TA 1535, TA 1537 and TA 1538 with and without metabolic activation and the sex linked recessive lethal mutation assay in Drosophila.
来源:Hazardous Substances Data Bank (HSDB)
毒理性
皮肤症状
干燥的皮肤。
Dry skin.
来源:ILO-WHO International Chemical Safety Cards (ICSCs)
毒理性
眼睛症状
红斑。疼痛。
Redness. Pain.
来源:ILO-WHO International Chemical Safety Cards (ICSCs)
Neurotoxin - Acute solvent syndrome
Occupational hepatotoxin - Secondary hepatotoxins: the potential for toxic effect in the occupational setting is based on cases of poisoning by human ingestion or animal experimentation.
Nephrotoxin - The chemical is potentially toxic to the kidneys in the occupational setting.
Hemolytic anemia - Decreased hemoglobin or number of red blood cells.
Reproductive Toxin - A chemical that is toxic to the reproductive system, including defects in the progeny and injury to male or female reproductive function. Reproductive toxicity includes developmental effects. See Guidelines for Reproductive Toxicity Risk Assessment.
Skin Sensitizer - An agent that can induce an allergic reaction in the skin.
来源:Haz-Map, Information on Hazardous Chemicals and Occupational Diseases
/SRP:/ 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 as necessary. Immediately flush contaminated eyes with gently flowing water. Do not induce vomiting. If vomiting occurs, lean patient forward or place on 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. /Ethers and related compounds/
来源:Hazardous Substances Data Bank (HSDB)
吸收、分配和排泄
丁基卡必醇可以通过皮肤吸收，但只有在长时间连续使用且用量达到有毒程度时才会发生。
Butyl carbitol can be absorbed through skin, but only in toxic amt if application is prolonged & continuous.
In vitro percutaneous absorption studies were carried out for ... /tritiated water, 2-ethoxyethyl acetate, diethylene glycol monobutyl ether, urea, di(2-ethylhexyl) phthalate, 2-ethylhexanol, ethyl 3-ethoxypropionate, and 2-propoxyethanol/ using full thickness rat skin and human stratum corneum. The purpose of the studies was to compare the rates of absorption for the two species. For each of the chemicals, the observed rate using full thickness rat skin was greater than that observed for human stratum corneum. The ratios of the rates (rat/human) varied from 1.7 to 5.8 with a mean value of 3.1. ... It was concluded that rat skin was more permeable than human skin for each of these eight chemicals. ...
Male and female Sprague-Dawley rats received 200 and 2000 mg neat (14)C-DEGBE/kg bw and 200 mg of a 10% aqueous solution/kg bw. Dermal adsorption rate was 0.73 and 1.46 mg/sq cm/hr for males and females respectively.
To assist the evaluation of the hazards of skin contact with selected undiluted glycol ethers, their absorption across isolated human abdominal epidermis was measured in vitro. Epidermal membranes were set up in glass diffusion cells and, following an initial determination of permeability to tritiated water, excess undiluted glycol ether was applied to the outer surface for 8 hr. The appearance of glycol ether in an aqueous "receptor" phase bathing the underside of the epidermis was quantified by a gas chromatographic technique. A final determination of tritiated water permeability was compared with initial values to establish any irreversible alterations in epidermal barrier function induced by contact with the glycol ethers. 2-Methoxyethanol was most readily absorbed (mean steady rate 2.82 mg/sq cm/hr), and a relatively high absorption rate (1.17 mg/sq cm/hr) was also apparent for 1-methoxypropan-2-ol. There was a trend of reducing absorption rate with increasing molecular weight or reducing volatility for monoethylene glycol ethers (2-methoxyethanol, 2.82 mg/sq cm/hr; 2-ethoxyethanol, 0.796 mg/sq cm/hr; 2-butoxyethanol, 0.198 mg/sq cm/hr) and also within the diethylene glycol series: 2-(2-methoxyethoxy) ethanol (0.206 mg/sq cm/hr); 2-(2-ethoxyethoxy) ethanol (0.125 mg/sq cm/hr) and 2-(2-butoxyethoxy) ethanol (0.05 mg/sq cm/hr). The rate of absorption of 2-ethoxyethyl acetate was similar to that of the parent alcohol, 2-ethoxyethanol. Absorption rates of diethylene glycol ethers were slower than their corresponding monoethylene glycol equivalents. Combination of intrinsic toxicity and ability to pass across skin contribute to assessment of hazards of contact with undiluted glycol ethers.
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] 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.
Compounds of the formula (I) wherein the substituents are as defined in claim 1, useful as a pesticides, especially fungicides.
式(I)的化合物，其中取代基如权利要求1所定义，作为杀虫剂特别是杀菌剂有用。
SILICON PHTHALOCYANINE COMPLEX, PREPARATION METHOD AND MEDICINAL APPLICATION THEREOF
申请人：Shenzhen China Resources Gosun Pharmaceutical Co., Ltd.
公开号：US20170002028A1
公开（公告）日：2017-01-05
The present invention relates to a silicon phthalocyanine complex, the preparation method and the medicinal application thereof. The present invention particularly relates to a silicon phthalocyanine complex of formula (I), the preparation method thereof and a pharmaceutical composition comprising the same, as well as the use thereof as a photosensitizer, in particular the use in the treatment of cancers, wherein each substituent in formula (I) is the same as defined in the description.
TAU-PROTEIN TARGETING PROTACS AND ASSOCIATED METHODS OF USE
申请人：Arvinas, Inc.
公开号：US20180125821A1
公开（公告）日：2018-05-10
The present disclosure relates to bifunctional compounds, which find utility as modulators of tau protein. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a VHL or cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds tau protein, such that tau protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of tau. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of tau protein. Diseases or disorders that result from aggregation or accumulation of tau protein are treated or prevented with compounds and compositions of the present disclosure.
Pyroglutamic Acid Esters With Improved Biodegradability
申请人：FEUSTEL Michael
公开号：US20120088942A1
公开（公告）日：2012-04-12
The invention relates to compounds of formula (1) in which A represents a C
2
to C
4
alkylene group; x represents a number from 1 to 100; R′ represents an aliphatic, cycloaliphatic or aromatic radical that contains at least one structural unit of formula 2, and; y represents a number from 1 to 100. The invention also relates to the use of these compounds in quantities of 0.01 to 2% by weight for preventing the formation of gas hydrates in aqueous phases that are connected to a gaseous, liquid or solid organic phase.
