The development of several hepatic microsomal drug-metabolizing enzyme activities in rats was studied in relation to its androgen dependence during the neonatal period. Rats with their androgen deprived during the neonatal period (female rats and male rats castrated at birth) respond less to androgen treatment at adulthood for the metabolism of aminopyrine, ethylmorphine and hexobarbital as compared to rats exposed to neonatal androgen (male rats, male rats castrated at birth but neonatally treated with androgen and male rats castrated at the age of 20 days). This difference in the degree of hepatic responsiveness, however, varied with the substrates: ethylmorphine N-demethylase activity was affected the most whereas aminopyrine N-demethylase and hexobarbital oxidase activities were only marginally affected. Furthermore, these differences in responsiveness seem to be a delayed event, since hepatic aminopyrine N-demethylase activity in rats castrated at birth did respond to androgen stimulation ...
We have previously described the development of genetic models to study the in vivo functions of the hepatic cytochrome P450 system, through the hepatic deletion of either cytochrome P450 oxidoreductase (POR; HRN line) or cytochrome b5 (Cyb5; HBN line). However, HRN mice still exhibit low levels of mono-oxygenase activity, in spite of the absence of detectable reductase protein. To investigate whether this is because cytochrome b5 and cytochrome b5 reductase can act as sole electron donors to the P450 system, we have crossed HRN with HBN mice to generate a line lacking hepatic expression of both electron donors (HBRN). HBRN mice exhibited exacerbation of the phenotypic characteristics of the HRN line - liver enlargement, hepatosteatosis and increased expression of certain cytochrome P450s. Also, drug metabolising activities in vitro were further reduced relative to the HRN model, in some cases to undetectable levels. Pharmacokinetic studies in vivo demonstrated that midazolam half-life, Cmax and ...
Biochemical, histopathological and ultrastructural changes occurring at different time points after intraperitoneal administration of a single dose of pulegone (300 mg/kg) were studied. Significant decreases in the level of liver microsomal cytochrome P-450 (67%), heme (37%), aminopyrine N-demethylase (60%) and glucose-6-phosphatase (58%), were noticed 24 hr after pulegone treatment. Alanine amino transferase (ALT) levels increased in a time dependent manner, following exposure of rats to pulegone. Light microscopic studies of liver tissues showed dilation of central veins and distention of sinusoidal spaces 6 hr after pulegone treatment. Initial centrilobular necrosis was noticed at 12 hr. Centrilobular necrosis became severe at 18 hr and nuclear changes included karyorrhexis and karyolysis. Midzonal and periportal degenerative changes in addition to centrilobular necrosis was observed 24 hr after pulegone administration. Electron microscopic changes showed severe degeneration of endoplasmic ...
2 major biochemical reactions that occur in the peroxisome is the mixed function oxidase and the other is a catalase but what 2 enzymes are involved in these reactions?...beta oxidation one of them ...
Clotrimazole, an N-substituted imidazole widely used as an antifungal agent, has been shown to both inhibit and induce hepatic cytochrome P-450 and related monooxygenase activities. In this study the profile of hepatic cytochrome P-450 isozyme(s) induced by clotrimazole treatment of male Sprague-Dawley rats was investigated. Clotrimazole administration (100 mg/kg, daily for 4 days, ig) resulted in 86% induction of spectrally detectable cytochrome P-450 in hepatic microsomes. In these microsomes 7-ethoxycoumarin O-deethylase (126%), aminopyrine N-demethylase (176%), benzphetamine N-demethylase (117%), p-nitrophenol hydroxylase (89%), and 7-ethoxyresorufin O-deethylase (62%) activities were significantly induced, whereas aryl hydrocarbon hydroxylase activity remained unchanged. Characterization of cytochrome P-450 isozyme(s) in hepatic microsomes prepared from clotrimazole-treated animals was based on the immunoreactivity of these microsomes with highly specific monoclonal antibodies (MAbs) raised ...
MARUMO, Sativa (1997) Regio- and stereoselective propranolol metabolism by 3 forms of purified cytochrome P450 from rat liver and the effect of cytochrome b5 on these metabolisms. Japanese Journal of Veterinary Research, 45(2): 135-136. MAEDA, Yutaka (1997) Strain differences in age-associated change in Testosterone 6β-hydroxylation in Wistar and Dark Agouti rats. Japanese Journal of Veterinary Research, 45(2): 135-135. NIKAIDOU, Satoshi (1997) Effect of green tea on hepatic enzyme activities and mutagenic transformation of benzo[a]pyrene. Japanese Journal of Veterinary Research, 45(2): 134-134. OHKURA, Kaori (1997) Three-dimensional visualization of abdominal and thoracic organs of rodents by superimposing MRI multislices with a computer-graphic technique. Japanese Journal of Veterinary Research, 45(2): 133-133. UI, Masahiro (1997) Transcriptional analysis of Mareks disease virus (MDV) genes in MDV-transformed lymphoblastoid cells without activated cells. Japanese Journal of Veterinary ...
Safrole, a hepatocarcinogen, is converted by the microsomal mono-oxygenase system to a reactive intermediate which interacts with cytochrome P-450 to form a ligand complex. The formation of this complex is accompanied by loss of mono-oxygenase activity. The present study describes the interaction of the safrole reactive intermediate with microsomes from phenobarbital, 3-methylcholanthrene and safrole pretreated animals.. ...
Ethanol-inducible cytochrome P450 (P450IIE) is reported to be induced by ketosis. In the present study, the effects of a high fat diet on P450IIE induction and the relationship between ketone body concentration and P450IIE induction were studied by the following: 1) measurement of the activity of aniline hydroxylase, 2) immunoblot analysis for P450IIE protein, and 3) Northern blot analysis for P450IIE mRNA. The enzyme activities (aniline hydroxylase) in hepatic and renal microsomes were elevated about 2-3-fold by feeding with a high fat diet for 3 days. The increases in enzyme activities were also accompanied by 3-fold increases in immunoreactive P450IIE protein and its mRNA. In contrast, no differences were observed for the catalytic activities of N-alkoxyresorufin dealkylases or the amounts of immunoreactive P450IA and P450IIC, indicating a specific induction of P450IIE by high fat feeding. Furthermore, the increases in the levels of P450IIE mRNA correlated positively (r = 0.73) with plasma ...
Modern medical science has made such tremendous strides in the field of therapeutics that many older drugs, especially if potentially productive of untoward and dangerous side-effects, have been discredited and have fallen into disuse. Admittedly, many such drugs have marked therapeutic value and are deserving of further investigation and clinical trial before they are completely discarded.. Aminopyrine, by force of historical circumstances, has been such a discredited drug for many years.1, 2a, 3c, 4b, 5, 6, 7, 8 The danger of agranulocytosis resulting from its use is real and well established, but undoubtedly has been overemphasized.1, 2a, 4b, 5, 6, ...
Synonyms for amidopyrine in Free Thesaurus. Antonyms for amidopyrine. 1 synonym for amidopyrine: aminopyrine. What are synonyms for amidopyrine?
Oldenlandia diffusa (OD) and Scutellaria barbata (SB) have been used in traditional Chinese medicine for treating liver, lung and rectal tumours. We previously showed that they inhibited mutagenesis, DNA binding and metabolism of aflatoxin B1 (AFB1) and benzo(a)pyrene (BaP) bioactivated by Aroclor 1254-induced rat S9. The purpose of this study was to investigate the effects of OD and SB on the mutagenicity of AFB1 in Salmonella typhimurium TA100 using dexamethasone (DXM)-induced rat hepatic S9, on cytochrome P450-linked aminopyrine N-demethylase (APND) activity in DXM-induced hepatic microsomes and on the metabolism of AFB1 by DXM-induced S9 using high-performance liquid chromatography (HPLC). The experimental results showed that OD and SB consistently inhibited the mutagenicity of AFB1 bioactivated by either non-induced or DXM-induced S9. These effects correlated with the inhibition of cytochrome P450-linked APND activity in DXM-induced microsomes and with an inhibition of DXM-induced S9 mediated
Lee, S.-M. and Clemens, M. G. (1992), Effect of α-tocopherol on hepatic mixed function oxidases in hepatic ischemia/reperfusion. Hepatology, 15: 276-281. doi: 10.1002/hep.1840150217 ...
The N-demethylation of N,N-dimethylphenobarbital by isolated rat hepatocytes was increased severalfold by pretreatment of animals with sodium phenobarbital (75 mg/kg/day ip for 3 days). The apparent extent of induction depended on the length of the cell incubation, being 3-fold when calculated after a 5-min incubation and 5-fold when calculated after a 60-min incubation. This difference was due to the fact that metabolism by "induced" hepatocytes more closely approached linearity over a 60-min period. Microsomal cytochrome P-450 levels were increased 3-fold upon phenobarbital treatment; during incubations of less than 30 min duration, increased N-demethylase activity could be entirely accounted for by this increase in cytochrome P-450. When protein levels were measured directly in microsomes isolated from hepatocyte homogenates, the levels in "induced" hepatocytes were approximately 45% higher than control. However, phenobarbital treatment had no significant effects on total cellular protein or ...
Phenytoin is extensively bound to plasma proteins and is prone to competitive displacement. Phenytoin is metabolized by hepatic cytochrome P450 enzymes CYP2C9 and CYP2C19, and is particularly susceptible to inhibitory drug interactions because it is subject to saturable metabolism. Inhibition of metabolism may produce significant increases in circulating phenytoin concentrations and enhance the risk of drug toxicity. Monitoring of phenytoin serum levels is recommended when a drug interaction is suspected.. Phenytoin is a potent inducer of hepatic drug-metabolizing enzymes. ...
BR-4935: cardiotonic; a non-adenosine analog adenosine1-receptor agonist with a substituted 2-thio-3,5-dicyano-4-phenyl-6-aminopyrine
Abstract Several parameters related to mono-oxygenase activity were followed in a population of chemical workers and controls. Workers exposed to toluene and xylene had a significant increase of urinary glucaric acid, that was correlated with hippuric acid excretion. On the other hand, workers exposed to pigments showed a marked increase of antipyrine half-life. A dose-related decrease of liver N-demethylase was induced in rats by the administration of a mixture of three of the pigments in use in the plant. Serum gamma-glutamyltranspeptidase was decreased in the workers exposed to pigments, but this variation was not statistically significant. The exposure to different chemicals in the workplace seemed to induce a complicated variation of mono-oxygenase levels, some enzyme being inhibited and others induced in the same group of workers. The sensitivity of these workers to toxic effects of chemicals, carcinogenic compounds and drugs seems to differ markedly from the control population. © 1982 ...
Learn about Tridione (Trimethadione Tablets) may treat, uses, dosage, side effects, drug interactions, warnings, patient labeling, reviews, and related medications.
ETHNOPHARMACOLOGICAL RELEVANCE: Shikonin, a naphthoquinone pigment abundant in the root of the Chinese herb Lithospermum erythrorhizon, has been widely used to treat inflammatory diseases for thousands of years. Whether shikonin changes drug metabolism remains unclear. AIM OF THE STUDY: We investigated whether shikonin modulates the expression of hepatic drug-metabolizing enzymes and transporters as well as the possible mechanisms of this action. MATERIALS AND METHODS: Primary hepatocytes isolated from Sprague-Dawley rats were treated with 0-2 μM shikonin and the protein and mRNA levels of drug-metabolizing enzymes and transporters as well as the activation of aryl hydrocarbon receptor (AhR) and NF-E2-related factor 2 (Nrf2) were determined ...
Rats of either sex as intact or partially hepatectomized (two-thirds liver removal) were injected s.c. daily for 7 days post-operatively with natural and synthetic estrogens, androgens or anabolic steroids, progesterone and adrenal cortical hormones
MF:C13H17N3O MW:231.29 CAS:58-15-1 EINECS:200-365-8 Apperance:White fronds crystal or crystalline powder. No smell, taste slightly bitter. Product use: Antipyretic and analgesic, used for fever and headache, joint pain, neuralgia, dysmenorrhea and...
Bardag-Gorce, F., Yuan, Q.X., Li, J., French, B.A., Fang, C., Ingelman-Sundberg, M., French, S.W., 2000. The effect of ethanol-induced cytochrome p4502E1 on the inhibition of proteasome activity by alcohol. Biochem. Biophys. Res. Commun. 279, 23-29.. Bondoc, F.Y., Bao, Z., Hu, W.Y., Gonzalez, F.J., Wang, Y., Yang, C.S., Hong, J.Y., 1999. Acetone catabolism by cytochrome P450 2E1: studies with CYP2E1-null mice. Biochem. Pharmacol. 58, 461-463.. Cederbaum, A.I., 2014. Methodology to assay CYP2E1 mixed function oxidase catalytic activity and its induction. Redox Biol. 2C, 1048-1054.. Cheng, J., Chen, C., Kristopher, K.W., Manna, S.K., Scerba, M., Friedman, F.K., Luecke, H., Idle, J.R., Gonzalez, F.J., 2013. Identification of 2-piperidone as a biomarker of CYP2E1 activity through metabolomic phenotyping. Toxicol. Sci. 135, 37-47.. Cheung, C., Gonzalez, F.J., 2008. Humanized mouse lines and their application for prediction of human drug metabolism and toxicological risk assessment. J. Pharmacol. Exp. ...
Product Name: 2,8-diiododibenzofuranFormula: C12H6OI2Weight: 419.98344SMILES: IC1=CC2C3=C(C=CC(I)=C3)OC=2C=C1CAS NO: 127-48-0 Product: Trimethadione &
Autori: Lefter LP, Sunamura M, Furukawa T, Yastsuoka T, Abe H, Inoue H, Abe T, Egawa S, Miura K, Morita R, Horii A, Matsuno S.. Editorial: Asian J Surg. 2004 Apr;27(2):85-92., 2004.. Rezumat:. BACKGROUND: In a previous work, we demonstrated that loss of heterozygosity of 18q is a frequent event significantly associated with poor prognosis in pancreatic cancer. We hypothesized that restoration of heterozygosity of chromosome 18 in pancreatic cancer cells would reduce their tumorigenicity. This study was intended to provide functional evidence for the existence of new tumour suppressor gene(s) located on chromosome 18. METHOD: Restoration of heterozygosity was achieved by introducing a normal copy of chromosome 18 into pancreatic ductal carcinoma using a microcell-mediated chromosome transfer technique. The tumorigenicity and metastatic ability of both the parental cells and resulting hybrids were assessed in vitro and in vivo. RESULTS: In vitro growth of hybrid clones was significantly delayed ...
Earlier we demonstrated that meta-iodobenzylguanidine (MIBG), a specific inhibitor of arginine mono-ADP-ribosylation blocks proliferation and differentiation of chick skeletal myogenic cells in...
Although the aminopyrine breath test has received much attention, the question has not yet been settled whether pharmacological or tracer doses of the drug should be used. Nine volunteers were given14...
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In toxicological research, immortalized human hepatocytes provide a useful alternative to primary hepatocytes because interindividual variability in the expression of drug-metabolizing enzymes and drug transporters can largely be eliminated. However, it is essential that the cell line retain the original phenotype. The purpose of this study was to characterize a novel spontaneously immortalized human hepatocyte cell line, HC-04, with respect to the transcript and functional protein expression profile for the major drug-metabolizing enzymes and transmembrane transporters. HC-04 cells retained hepatocyte-specific function including albumin production and ornithine transcarbamoylase and glucose-6-phosphatase activity. Most of the major CYP forms were expressed at basal levels and responsive to inducing agents. In particular, CYP3A4 was expressed abundantly, and HC-04 cells were able to metabolize the CYP3A4 probe, midazolam, at a rate similar to primary human hepatocytes. Furthermore, the major ...
DNA Demethylase Activity/Inhibition Assay Kit is use for measuring DNA demethylase activity/inhibition. (KA0677) - Products - Abnova
The effect of ethanol on N-demethylation of aminopyrine in rat liver slices and in the microsomal fraction and on microsomal hydroxylation of pentobarbital and aniline was studied. With liver slices N-demethylation of aminopyrine was stimulated by 35-40% at low ethanol concentrations (2mm), whereas no stimulation occurred at high concentrations (100mm). With the liver microsomal fraction, an inhibitory effect was observed only at high ethanol concentrations (100mm). This was also observed with the other drugs studied. In agreement with these results, only at a high concentration did ethanol interfere with the binding of drug substrates to cytochrome P-450. Further, as previously reported, ethanol produced a reverse type I spectral change when added to the liver microsomal fraction. Evidence that this spectral change is due to removal of substrate, endogenously bound to cytochrome P-450, is reported. A dual effect of ethanol is assumed to explain the present findings; in liver slices, at a low ...
dentification of the fundamental polypeptide difference between yellow (Ay/-, Avy/-) and non-yellow mice is important for biomedical research because of the influence of the yellow genotype on normal and neoplastic growth and obesity. The complexity of the "yellow mouse syndrome" makes attainment of this objective dependent on the separation of those pleiotropic enzyme differences which are secondary, and depend on the background genome, from those which are primary, and depend primarily on the agouti locus genotype.-Four of nine hepatic enzyme activities assayed simultaneously differed between eight-week-old yellow (Ay/-, Avy/-) and non-yellow (A/-, a/a) male inbred and F1 hybrid mice. Among these four, only cytoplasmic malic enzyme activity was elevated in all yellow mice, as compared with the non-yellow sibs, regardless of background genome. Glucokinase, serine dehydratase, and tyrosine α-ketoglutarate transaminase activities were also changed in yellow mice, but these alterations depended ...
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Chemicals - Coatings China, Formic Acid Rubber Pulp Disinfest, Uses: 1. Pharmaceutical industry: Caffeine, Enzimes, Aminopyrine, Vitamin B1 2. Pesticide industry: Triazolone, Disinfes...
N-Nitrosodimethylamine is a procarcinogen that is activated by cytochrome P450 dependent N-nitrosodimethylamine N-demethylase to labile alpha-carbon hydroxylated products further resulting in active methylating agents. In vivo intraperitoneal administration of pyridine to rabbits significantly increased N-nitrosodimethylamine N-demethylase activity by 6.9- and 5.2-fold in liver and lung microsomes, respectively. Although, p-nitrophenol hydroxylase and aniline 4-hydroxylase activities were markedly enhanced by pyridine treatment in liver about 4.4- and 5.8-fold, respectively, no change was observed in the activities of these enzymes in lung microsomes. Pyridine treatment also elevated P450 contents of liver and lung by 2.04- and 1.4-fold, respectively. SDS-PAGE of pyridine-induced liver microsomes revealed a protein band of enhanced intensity having M-r of 51,000 migrating in the region of cytochrome P4502E1. The results obtained in this study demonstrated for the first time, a significant ...
Trimethadione anticonvulsant drug molecule. Used in treatment of seizures. Atoms are represented as spheres with conventional colour coding: hydrogen (white), carbon (black), oxygen (red), nitrogen (blue). - Stock Image F011/3640
Rph1 and Gis1 are two related yeast zinc finger proteins that function as downstream effectors in the Ras/PKA, TOR and Sch9 nutrient signaling pathways. Both proteins also contain JmjC histone demethylase domains, but only Rph1 is known to be an active enzyme, demethylating lysine 36 of histone H3. We have studied to what extent the demethylase activity of Rph1 contributes to its role in nutrient signaling by performing gene expression microarray experiments on a yeast strain containing a catalytically inactive allele of RPH1. We find that the enzymatic activity of Rph1 is not essential for its role in growth phase dependent gene regulation. However, the ability of Rph1 to both activate and repress transcription is partially impaired in the active site mutant, indicating that the demethylase activity may enhance its function in vivo. Consistent with this, we find that the Rph1 mutation and a deletion of the histone H3 methylase Set2 affect the same target genes in opposite directions. Genes that ...
With that encouragement Axelrod quickly showed that amphetamine was rapidly metabolized in rabbit liver slices. He went on to define the co-factor requirements for the reaction finding that NADPH was required; similar to observations of Bert LaDu in his studies on aminopyrine demethylation9.Axelrod then determined the sub-cellular location of the activity by using methods developed by Hogeboom and Schneider10. This newly defined microsomal oxidizing system was soon shown to be responsible for the metabolism of a wide variety of drugs and other chemicals.. Ref: 1V.R.Potter and C.A.Elvehjem, J.Biol. Chem. ,114:495-504 (1936) 2A.Claude, Cold String Harbor Symposium Quant.Biol.,9:263-270 (1941)3 W.C.Schneider,J.Biol.Chem. 165:585-593 (1949) 4E.C.Miller and J.A.Miller, Cancer Res. 7:468-480 (1947)5 E.S.Stevenson, K. Dobriner, and C.P.Rhoads, Cancer Research 2:160-167 (1942)6 G.C.Mueller and J.A.Miller, J.Biol.. Chem. 176:535-544 (1948) 7G.C.Mueller and J.A. Miller, J.Biol. Chem. ,180:1125-1236 ...
Algorithm for the management of hepatic enzyme elevations in the INPULSIS® trials. *Defined as increase in hepatic transaminases (AST or ALT) to ≥3 x ULN, an
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Oral The metabolism of nonyl phenol ethoxylates takes place by shortening the ethylene oxide chain, carboxylation of the alkyl chain by omega oxidation and subsequent glucoronide and sulphate conjugation (CIR, 1983). Knaak et al. (1966) fed 67 mg/kg of NP-14C TP-9 (a commercial product containing on average 9 moles of EO per mole of NP, i.e. NPE-9) or 14C-NP to rats and followed urinary, faecal over a period of 7 days and CO2 excretion over a period of 4 days. Within the observed time period, 20% of the NP-14C TP-9 was excreted in urine, 78% in faeces and none as14CO2 14C-NP per se was found to be excreted in a similar manner. In the same study, Knaak et al. also exposed rats to 7, 10, 12 and 15 mole adducts of NP isolated from ethylene oxide-labelled TP-9. The 12 and 15 mole adducts were excreted to a greater extent in the feces than the 7 and 10 mole adducts, while the reverse situation occurred in urine. Modelling the metabolism of NPE-2 and NPE-4 in liver using the using prediction tools ...
Hasegawa R, St John MK, Cano M, Issenburg P, Klein DA, Walker BA, Jones JW, Schnell RC, Merrick BA, Davies MH, McMillan DA, Cohen SM. 1984. Bladder freeze ulceration and sodium saccharin feeding in the rat, examination for urinary nitrosamines, mutagens, and bacteria, and effects on hepatic microsomal enzymes. Food Chem Toxicol 22:935-942.. View Abstract ...
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Nitrogen assimilation during growth of Candida boidinii on methylated amines as sole nitrogen source involves NADP-dependent glutamate dehydrogenase. Changes in enzyme activities during the adaptation of the yeast from growth on ammonium to growth on trimethylamine were examined. No ammonia, dimethylamine or monomethylamine could be detected in the medium during growth on trimethylamine. When two methylated amines were supplied together, they were used simultaneously, although monomethylamine was metabolized more quickly than the others. When cells were grown on a low concentration of ammonium plus higher concentrations of di- or trimethylamine, the ammonium was used first. NADP-dependent glutamate dehydrogenase was the first enzyme to be derepressed, followed by methylamine oxidase and formaldehyde dehydrogenase. Di- and trimethylamine mono-oxygenase activities only appeared when the ammonium concentration fell below 0.5 mM. At this point amine utilization could be detected and no diauxic lag was