DURING THE DECOMPOSITION OF SODIUM PENTACHLOROPHENOLATE BY ALCALIGENES EUTROPHUS, AEROMONAS HYDROPHILIA VARIETY HYDROPHILIA AND VARIETY ANAEROGENES, AZOTOBACTER CHROOCOCCUM, AZOTOBACTER VINELANDII, FLAVOBACTERIUM AQUATILE, PSEUDOMONAS FLUORESCENS, CYTOPHAGA JOHNSONAE, CORYNEBACTERIUM AQUATICUM, BREVIBACTERIUM TESTACEUUM, AND ARTHROBACTER GLOBIFORMIS THE FOLLOWING /METABOLITES WERE IDENTIFIED/: PENTACHLOROANISOLE, 2,3,4,5-TETRACHLOROANISOLE, 2,3,4,6-TETRACHLOROANISOLE, 2,3,5,6-TETRACHLOROANISOLE, 2,3,4,5-TETRACHLOROPHENOL, 2,3,5,6-TETRACHLOROPHENOL, TETRACHLORORESORCINOL, TETRACHLOROHYDROQUINONE, AND TETRACHLOROACETECHOL DIACETATE, THE PRINCIPAL METABOLITE BEING PENTACHLOROPHENOL ACETATE. UP TO 6.2% OF THE SODIUM PENTACHLOROPHENOLATE WAS RECOVERED AS PENTCHLOROPHENOL ACETATE, WHILE ALL OTHER METABOLITES WERE FOUND IN AMT LESS THAN 1% OF STARTING CMPD.
Spent sawdust cultures of the Shiitake mushroom (Lentinus edodes) metabolized pentachlorophenol in soil to a significant (p<0.05) extent with 60.5, 57.3 and 44.4 % disappearance recorded for strains LE2 866 and R26 respectively. Addition of H202 markedly enhanced pentachlorophenol metabolism. Analysis of metabolites by GC/MS showed that pentachloroanisole was a metabolic product. These results suggest that there is potential for commercial application ln bioremediation.
来源:Hazardous Substances Data Bank (HSDB)
毒理性
副作用
职业性肝毒素 - 第二性肝毒素：在职业环境中的毒性效应潜力是基于人类摄入或动物实验的中毒病例。
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.
来源:Haz-Map, Information on Hazardous Chemicals and Occupational Diseases
毒理性
非人类毒性摘录
将五氯苯甲醚添加到大鼠饲料中似乎并未改变尿和粪便中卟啉的排泄。
ADDN OF PENTACHLOROANISOLE TO FEED OF RATS DID NOT APPEAR TO ALTER URINARY & FECAL PORPHYRIN EXCRETION.
PENTACHLOROANISOLE WAS MUCH LESS TOXIC THAN PENTACHLOROPHENOL TO TRICHODERMA VIRGATUM, CEPHALOASCUS FRAGRANS & PENICILLIUM SP, AS WELL AS TO FISH, IN LAB TOXICITY TESTS.
Pentachloroanisole was evaluated for its mutagenic potential in the L5178Y TK+/TK- mouse lymphoma forward mutation assay using established procedures. Six experiments were conducted: two without metabolic activation and four with metabolic activation. The dose levels tested in these experiments ranged from 0-500 ug/ml. The two experiments without metabolic activation were discarded because no clear mutagenic response was obtained at dose levels where pentachloroanisole did not percipitate. Significant mutagenic responses were obtained in the remaining four experiments. Thus, pentachloroanisole was positive in these tests and the lowest effective dose tested was 31.25 ug/ml.
Male and female Sprague-Dawley (Spartan) rats were exposed to dietary levels of 60, 200 or 600 ppm purified pentachlorophenol (PCP) or pentachloroanisole (PCA) for 181 days, through mating and pregnancy. The daily intakes of PCP were 0, 4, 13 or 43 mg/kg body weight and of PCA were 0, 4, 12 or 41 mg/kg body weight. Animals exposed to PCP generally consumed more food than control animals during pregnancy. Dams at the high dose level of both compounds showed evidence of toxicity, weighing less on day 0 of gestation and gaining less throughout pregnancy than did the controls. Dams exposed to the high dose of PCP gained less weight during pregnancy (exclusive of the gravid uterus) than control dams. At the 43 mg/kg/day dose level PCP was embryolethal. Fetuses at the lower dose levels of PCP exhibited dose related decreases in body weights. A reduction in crown-rump length and an increase in fetal skeletal variations were seen at 13 mg/kg/day in PCP animals only. An intake of 41 mg PCA/kg/day was associated with a decrease in the number of corpora lutea and in embryolethality. PCA exposure also resulted in reductions in fetal body weight and crown-rump lengths of males at 4 and 41 mg/kg/day. Female fetuses were unaffected.
RELATIVE TISSUE CONCN & TOTAL BIRD LEVELS OF CHLOROANISOLES IN COMMERCIAL BROILERS REARED ON LITTER REPORTED. ALTHOUGH HIGHEST CONCN OCCURRED IN BONE & ADIPOSE TISSUE, GREATEST CONTRIBUTION TO WHOLE BIRD LEVELS IN EDIBLE TISSUE WAS PREDOMINANTLY PENTACHLOROANISOLE.
PENTACHLOROANISOLE (PCA) TAKEN UP RAPIDLY BY RAINBOW TROUT @ 0.025 MG/L IN WATER. AFTER 24 HR, CONCN IN LIVER, BLOOD, FAT & MUSCLE WERE 16, 6.5, 80, & 1.0 UG/G, RESPECTIVELY; T/2 OF 6.9, 6.3, 23, & 6.3 DAYS, RESPECTIVELY.
Tissue distribution, excretion and metabolism studies of pentachloroanisole (PCA), an environmental metabolite of pentachlorophenol (PCP), were conducted in the beagle dog and miniature pig following single oral doses (25 mg/kg) of radiolabelled PCA. PCA was readily demethylated by both species, with a half-life of 5-8 min. The resultant PCP was the major metabolite in dogs and pigs. In the dog, an average of 21.9% of the administered radiolabel was excreted in the urine and 62.3% in the feces during a 7 day period. Of the tissues analyzed, an average of 3.2% of the radiolabel remained in the liver, and blood and muscle accounted for averages of 3.0 and 2.3%, respectively, of the dose. Free and conjugated PCP were found in the urine of dogs; no PCA or tetrachlorohydroquinone (TCH) were found. In dog feces, PCP and a trace of polar material were observed; no PCA was excreted in dog feces. In the miniature pig, an average of 25.8% of the administered radiolabel was excreted in the urine and 32.0% in the feces during a 2-wk period. An average of 4.4% of the radiolabel was found in the liver, 8.8% in the blood, 7.1% in the muscle and 6.4% in the fat. In pig urine, PCP and conjugated PCP were the only metabolites observed; no PCA or TCH was found. Pig feces contained a trace of unchanged PCA; PCP and polar metabolites were also found. Since pig tissues retained a sizeable residue 2 wk after a single dose of PCA, various agents were used in an attempt to decrease the tissue level of radiolabel in pigs; anion exchange resin was found to be the most effective.
Toxicokinetics of pentachloroanisole (PCA) were studied in F344 rat and B6C3F1 mouse of both sexes by gavage at doses of 10, 20 and 40 mg/kg and by iv at 10 mg/kg. PCA was rapidly demethylated to pentachlorophenol (PCP) in both rat and mouse and the resulting PCP plasma concentrations were much higher than that of parent PCA due to the much smaller apparent volume of distribution of PCP. Peak plasma concentrations of PCA and PCP increased with dose in both rat and mouse. Bioavailability of PCA was low in both rat and mouse and was sex independent. The high plasma concentrations and relatively long biological half-life of PCP in both species after both iv and oral dosing with PCA indicate possible bioaccumulation of PCP upon multiple oral administrations of PCA.
Male Sprague-Dawley rats and New Zealand White rabbits were admin (14)C-labelled pentachloroanisole (PCA) in corn oil by gavage as single doses of 25 mg/kg and were then placed in individual metabolism cages for as long as 4 days. Peak blood level of radioactivity occurred 6 hr after admin of the dose to rats and between 3 and 4 hr in rabbits; the blood elimination half-life ranged from 8 to 15 hr in rats and averaged 6 hr in rabbits. Rats excreted an average of 54.2% of the admin radiolabel in the urine and 32.4% in the feces during the 96 hr following the dose; rabbits excreted an average of 84.2 and 13.1% of the radiolabel in the urine and faces, respectively, during this time. Examination of the metabolites in the rat showed that 60% of the urinary radioactivity was attributable to tetrachlorohydroquinone (TCH), 3% to free pentachlorophenol (PCP) and 29% to conjugated PCP; fecal metabolites were PCP (85.7%), TCH (4.3%) and polar metabolites (10.0%). In the rabbit, 58% of the urinary radioactivity was attributable to TCH, 8% to free PCP and 34% to conjugated PCP. Fecal metabolites consisted of PCP and conjugated material
[EN] IONIC LIQUID SUPPORTED ORGANOTIN REAGENTS FOR THE MANUFACTURING OF RADIOPHARMACEUTICALS COMPOUNDS<br/>[FR] RÉACTIFS ORGANOSTANNIQUES SUPPORTÉS SUR LIQUIDE IONIQUE POUR LA PRODUCTION DE COMPOSÉS RADIOPHARMACEUTIQUES
申请人：CENTRE NAT RECH SCIENT
公开号：WO2015104300A1
公开（公告）日：2015-07-16
The present invention relates to an ionic liquid supported organotin reagent of formula (I). The invention further relates to a process for manufacturing the ionic liquid supported organotin reagent of formula (I) and to a process for manufacturing an halogenated or radio-halogenated compound using compound of formula (I). The invention also relates to a device for implementing the halogenating process of the invention and to a kit comprising the compound of formula (I).
New compounds are provided that may be used to chelute a metal. The compound comprise polyazamacrocyclic compound with at least one phosphonic group substituted on at least one of the aza groups of the polyazamacrocyclic compound. Methods for preparing the compounds are also provided. Methods for preparing a diagnostic imaging agent using the compounds and methods for diagnostic imaging are further provided. Methods for preparing a therapeutic agent using the compounds and methods for therapy are further provided.
Electroreduction of Organic Compounds, 34 [1]. Cathodic Dehalogenation of Chloroarenes with Electron-Donating Substituents
作者：Olaf Kranz、Jürgen Voss
DOI：10.1515/znb-2003-1206
日期：2003.12.1
The electrochemical reduction of chlorinated arenes with electron-donating substituents, i. e. chlorotoluenes, -anisoles and -phenols, is studied. Preparative electrolyses are run in various solventsupporting electrolytes under potentiostatic and galvanostatic conditions at lead or carbon cathodes. A partial and mostly regioselective hydrodechlorination of compounds with two or more chloro substituents is possible under suitable conditions. The replacement of one single chloro substituent, in particular in a para-position, is difficult. Highly toxic and persistent oligochloro derivatives are thus transformed into less problematic compounds with a low degree of chlorination. The chlorine content of real-life materials such as extracts of soil contaminated with chlorinated phenols and Nitrofen® can also be significantly decreased by electroreduction.
Disposition and metabolism of radiolabelled pentachloroanisole in rats and rabbits
作者：G.J. Ikeda、P.P. Sapienza、P.I. Warr
DOI：10.1016/0278-6915(94)90129-5
日期：1994.12
in rats and averaged 6 hr in rabbits. Rats excreted an average of 54.2% of the administered radiolabel in the urine and 32.4% in the faeces during the 96 hr following the dose; rabbits excreted an average of 84.2 and 13.1% of the radiolabel in the urine and faeces, respectively, during this time. Examination of the metabolites in the rat showed that 60% of the urinary radioactivity was attributable
ALBUMIN BINDING PROBES AND DRUG CONJUGATES THEREOF
申请人：Shechter Yoram
公开号：US20150202310A1
公开（公告）日：2015-07-23
The present invention provides a long chain fatty acid (LCFA)-like albumin-binding probe/ligand containing no hydrolysable bond and having an enhanced associating affinity with human serum albumin, which upon conjugation with an amino- or mercapto-containing short-lived drug and administration of the conjugate, significantly prolongs the life time of said drug without substantially interfering with its pharmacological activity. The invention further provides conjugates of said probe with amino- or mercapto-containing drugs, as well as pharmaceutical compositions and uses thereof.
