The in vitro metabolism of 2,2',4,4',5,5'-hexabromobiphenyl (BB 153) with liver microsomes of rats induced with either BB 153 or FireMaster BP-6 produced three major metabolic fractions: lipophilic ether soluble polar metabolites, trichloroacetic acid (TCA) soluble conjugates, and macromolecular adducts.
In contrast to the lower brominated congeners, no major metabolites were identified in the urine or feces of rats treated with a single ip dose of 2,2'4,4'5,5'-hexabromobiphenyl.
Feces of dogs fed BP-6 contained a metabolite identified as 6-hydroxy-2,4,5,2',4',5'-hexabromobiphenyl (hydroxy-HBB). MS analysis of synthetic hydroxy-HBB showed that, during GC on OV-101 columns at 230-260 °C, it decomposes into two pentabromodibenzofurans (PDBF).
PBBs can be absorbed via oral, inhalation, and dermal routes. Due to their lipophilic nature, PBBs, especially the highly brominated congeners, tend to accumulate in lipid-rich tissues such as the liver, adipose, skin, and breast milk. Certain PBB compounds are metabolized by the microsomal monooxygenase system catalyzed by cytochrome P-450 of the type induced by phenobarbital. The rate of metabolism may depends on the bromine substitution pattern. PBB congeners of low bromine content are transformed into hydroxylated derivatives that are predominately eliminated in the urine. Highly brominated congeners are either retained or excreted unchanged in the feces. (L628)
The exact mechanism of toxicty of PBBs varies depending on the specific congener. The predominant interaction is believed to involve the aryl hydrocarbon receptor (AhR). PBBs bind to and activate the AhR, which in turn initiates the transcriptional upregulation of a number of genes, affecting biochemical and endocrine pathways, cell cycle regulation, morphogenesis, oxidative stress response, and various other processes. This results in the numerous toxic responses characteristic of PBBs. Some of the known induced genes include the cytochrome P-450-dependent monooxygenases CYP1A1 and CYP1A2. (L628)
PBB exposure may cause weight loss, skin disorders (such as acne), nervous and immune systems effects, and effects on the liver, kidneys, and thyroid gland. (L628)
来源:Toxin and Toxin Target Database (T3DB)
毒理性
暴露途径
口服（L628）；吸入（L628）；皮肤给药（L628）
Oral (L628) ; inhalation (L628) ; dermal (L628)
来源:Toxin and Toxin Target Database (T3DB)
毒理性
症状
PBB暴露的症状可能包括恶心、腹痛、食欲不振、关节痛、疲劳和虚弱。
Symptoms of PBB exposure may include nausea, abdominal pain, loss of appetite, joint pain, fatigue, and weakness. (L629)
(14)C-labelled 2,2',4,4',5,5'-hexabromobiphenyl...administered to male rats was readily absorbed from intestine and distributed throughout body; it was stored principally in fat. Extrapolation of rate of excretion indicates that <10% of any dose would be excreted.
2,2',4,4',5,5'-Hexabromobiphenyl was most prevalent polybrominated biphenyl homolog in serum from Michigan chemical corp employees, serum from dairy farmers, and serum from rats exposed to Firemaster FF 1.
Timed-pregnant albino Hartley strain guinea pigs of approximately 65 days gestation or lactating animals within 6-12 hr of parturition received a single oral dose of Firemaster FF-1 (50 mg/kg bw). The pregnant animals and their fetuses were killed 2 days later at term while the lactating animals and their pups were killed at intervals of 2, 4, 7, 14, 28, 42, and 60 days. Tissues (liver, kidney, lung, perirenal fat) were /analyzed/ ...for 2,4,5,2',4',5'-hexabromobiphenyl (HBB)... content... . Transplacentally-acquired residues of the order of 45 ug HBB/g were found in both maternal and fetal adipose tissue and in fetal liver. HBB residues in maternal kidney, lung and liver were of the order of 4-7 ug/g while, in the fetuses and pups, levels in the kidney and lung were of the order of 1-2 ug/g. Levels of HBB in breast milk 2 days after treatment averaged 22.4 +/- 7.8 ug/g (mean +/- S.D.)... . HBB levels in the pup kidney, lung and adipose tissue reflected redistribution or sequestration in the body fat. The biological half-life of HBB in tissues of both dams and pups appeared to be approximately 22 days. /Firemaster FF-1/
In rats treated by gavage with one or four daily doses of 14C-2,2',4,4',5,5'-hexabromobiphenyl (BB 153), initial concentrations of radioactivity were highest in muscle, liver, and adipose tissue, but later redistribution to adipose tissue (4-7 days after the last dosing) resulted in lower concentrations in liver and muscle. In rats dosed daily with 14C-BB 153 over a 30-day period, tissue concentrations on day 31 were (in increasing order): blood, muscle, liver, skin, and adipose... .
来源:Hazardous Substances Data Bank (HSDB)
文献信息
[EN] PFKFB3 INHIBITORS AND THEIR USES<br/>[FR] INHIBITEURS DE PFKFB3 ET LEURS UTILISATIONS
申请人：GERO DISCOVERY LLC
公开号：WO2020080979A1
公开（公告）日：2020-04-23
This disclosure relates to new phthalimide and isoindolinone derivatives and other PFKFB3 inhibitors for use in the treatment of diseases. The invention further relates to pharmaceutical compositions containing such PFKFB3 inhibitors, methods of preparation thereof, methods for their use as therapeutic agents, and methods of preparation of a medicament for use in therapy, as well as kits and other inventiions comprising such PFKFB3 inhibitors. These PFKFB3 inhibitors are useful for the treatment and prophylaxis of cancer, neurodegenerative diseases, autoimmune diseases, inflammatory disorders, multiple sclerosis, metabolic diseases, inhibition of angiogenesis and other diseases and conditions, where the modulation of PFKFB3 and/or PFKFB4 has beneficial effect as well as neuroprotection.
Zinc borate, and production method and use thereof
申请人：——
公开号：US20030030042A1
公开（公告）日：2003-02-13
A zinc borate having a particular crystallite size and containing very little sodium components and a method of preparing the same. The zinc borate has a particular chemical composition, has a crystallite size of not smaller than 40 nm as found from diffraction peaks of indexes of planes of (020), (101) and (200) in the X-ray diffraction image (Cu-k&agr;) and contains sodium components in amounts of not larger than 100 ppm as measured by the atomic absorptiometric method.
Insulating material containing cycloolefin polymer
申请人：——
公开号：US20040157039A1
公开（公告）日：2004-08-12
An insulating material comprising a cycloolefin polymer, specifically, an interlayer insulating material for a high-density assembly board having interlayer-connecting via holes at most 200 &mgr;m in diameter, comprising a cycloolefin polymer containing at least 50 mol % of a repeating unit derived from a cycloolefin monomer; a dry film formed from a curable resin composition comprising a polymer having a number average molecular weight within a range of 1,000 to 1,000,000 as measured by gel permeation chromatography, and a hardener; and a resin-attached metal foil obtained by forming a film of a cycloolefin polymer on one side of a metal foil. Laminates, multi-layer laminates and build-up multi-layer laminates making use of these materials, and production processes thereof.
Phototropic photosensitive compositions containing a fluoran colorformer
申请人：Dynachem Corporation
公开号：EP0005380A2
公开（公告）日：1979-11-14
Compositions containing a polymerizable, curable or crosslinkable component, a photoinitiator, a fluoran colorformer and a latent activator that releases or promotes the release of a Lewis acid, will become insoluble and change color under the influence of actinic radiation. These compositions are particularly useful to make dry film photoresists, which are widely used in the electronics industry to manufacture printed circuits.
An organic high molecular composition having improved fire retardance, which is prepared by compounding a fire retardant composition comprising (a) organic high molecular material, (b) organic fire retardant, and (c) incombustible, polar, inorganic powder, with (d) a multi-functional compound and (e) an organic compound represented by the following formula
[wherein Z represents an oxygen atom or a sulfur atom, A represents a divalent hydrocarbyl group containing 2 to 20 carbon atoms, optionally having a substituent, and forming a ring together with the adjacent two carbon atoms and B, and B represents an oxygen atom or an imino group represented by -NY- (wherein Y represents a hydrogen atom, a halogen atom or an organic group containing 30 or less carbon atoms)] or the hydrolyzate thereof.
一种具有更佳阻燃性的有机高分子组合物，其制备方法是将包含(a)有机高分子材料、(b)有机阻燃剂和(c)不可燃极性无机粉末的阻燃组合物与(d)多功能化合物和(e)由下式表示的有机化合物复合在一起
[其中 Z 代表氧原子或硫原子，A 代表含有 2 至 20 个碳原子的二价烃基，可选择具有一 个取代基，并与相邻的两个碳原子和 B 一起形成一个环，B 代表氧原子或由 -NY- 代表的亚氨基（其中 Y 代表氢原子、卤素原子或含有 30 个或更少碳原子的有机基团））]或其水解物。
