Differences between induction effects of 1,4-bis[2-(3,5-dichloropyridyloxy)]benzene and phenobarbitone.

Abstract:

:The inductive effects of phenobarbitone (PB) and 1,4-bis[2-(3,5-dichloropyridyloxy)]benzene (TCPOBOP) were compared in C57BL/6J mice. Induction parameters included six substrates: ethylmorphine (EM), benzphetamine (Bph), biphenyl, ethoxycoumarin (EtoC), pentoxyresorufin and dichloro-p-nitroanisole (DPNA). In order to validate this descriptive approach the comparison was extended to diazepam, rifampicin, warfarin, and pregnenolone-16 alpha-carbonitrile (PCN). All inducers were clearly distinguishable from each other. Warfarin was similar to PB, rifampicin was similar to PCN. TCPOBOP differed significantly from PB in relative liver weight, cytochrome P-450 content of liver microsomes, EM-, Bph- and DPNA-demethylations, biphenyl-hydroxylations, EtoC de-ethylation and absorption maximum of reduced CO-cytochrome P-450. TCPOBOP, as an inducer, was less "specific" than PB: total metabolic rates were excessively increased due to microsomal protein (1.5 times) and cytochrome P-450 (4 times) augmentation, whereas cytochrome P-450-related metabolic rates were less increased than those after PB. Thus TCPOBOP does not seem to be as similar to PB as was suggested in the first description of its inducing potency.

journal_name

Biochem Pharmacol

journal_title

Biochemical pharmacology

authors

Heubel F,Reuter T,Gerstner E

doi

10.1016/0006-2952(89)90336-5

subject

Has Abstract

pub_date

1989-04-15 00:00:00

pages

1293-300

issue

8

eissn

0006-2952

issn

1873-2968

pii

0006-2952(89)90336-5

journal_volume

38

pub_type

杂志文章
  • Oxidative and mitochondrial toxic effects of cephalosporin antibiotics in the kidney. A comparative study of cephaloridine and cephaloglycin.

    abstract::Cephaloridine and cephaloglycin are the two most nephrotoxic cephalosporins released for human use. Cephaloridine has been shown to produce both oxidative and mitochondrial respiratory injury in renal cortex in patterns of dose (or concentration) and time that are consistent with pathogenicity. Cephaloglycin also prod...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(89)90233-5

    authors: Tune BM,Fravert D,Hsu CY

    更新日期:1989-03-01 00:00:00

  • Inactivation by acivicin of carbamoyl-phosphate synthetase II of human colon carcinoma.

    abstract::The effect of the anti-tumor, anti-glutamine drug acivicin, L-(alpha S,5S)-alpha-amino-3-chloro-4,5-dihydro-5-isoxazoleacetic acid, was determined on the activity of the rate-limiting enzyme of de novo pyrimidine biosynthesis, carbamoyl-phosphate synthetase II (glutamine-hydrolyzing) (EC 6.3.5.5), in human colon carci...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(85)90106-6

    authors: Sebolt JS,Aoki T,Eble JN,Glover JL,Weber G

    更新日期:1985-01-01 00:00:00

  • Subcellular localization of the camptothecin analogues, topotecan and gimatecan.

    abstract::Lipophilicity of camptothecins derivatives has been reported to improve the stability of the lactone ring and to favor rapid uptake and intracellular accumulation. Recently, a novel series of lipophilic camptothecins substituted at position 7 was developed, and gimatecan (ST1481) was selected for clinical development ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2003.10.034

    authors: Croce AC,Bottiroli G,Supino R,Favini E,Zuco V,Zunino F

    更新日期:2004-03-15 00:00:00

  • Comparison of the hepatic mixed function oxidase system of young, adult, and old non-human primates (Macaca nemestrina).

    abstract::The influence of age on the mixed function oxidase system from a non-human primate was studied. Microsomes were isolated from the livers of female Macaca nemestrina ranging from 2 to 21 years of age. No significant age-related change was observed in either the cytochrome P-450 content or the NADPH cytochrome c reducta...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(85)90025-5

    authors: Sutter MA,Wood WG,Williamson LS,Strong R,Pickham K,Richardson A

    更新日期:1985-08-15 00:00:00

  • Effects of chronic low-level lead exposure on mRNA expression, ADP-ribosylation and photoaffinity labeling with [alpha-32P]guanine triphosphate-gamma-azidoanilide of GTP-binding proteins in neurons isolated from the brain of neonatal and adult rats.

    abstract::The effects of chronic lead exposure on mRNA expression, ADP-ribosylation and photoaffinity labeling with [alpha-32P]guanine triphosphate-gamma-azidoanilide ([32P]GTP-A) of alpha i or alpha s subunit of G protein were investigated in neurons isolated from the brain of neonatal and adult rats exposed to lead acetate or...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(93)90255-u

    authors: Singh AK

    更新日期:1993-03-09 00:00:00

  • Intracellular glutathione as a determinant of responsiveness to antitumor drugs.

    abstract::The effect of glutathione depletion on cytotoxicity of the anthracycline daunorubicin, and of a copper:bis-thiosemicarbazone chelate, was examined in the P388 murine leukemia and its anthracycline-resistant subline, P388/ADR. Depletion of intracellular glutathione was accomplished through exposure to buthionine sulfox...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(86)90430-2

    authors: Romine MT,Kessel D

    更新日期:1986-10-01 00:00:00

  • Influence of chronic administration of valproate on ultrastructure and enzyme content of peroxisomes in rat liver and kidney. Oxidation of valproate by liver peroxisomes.

    abstract::Chronic administration to rats of the anticonvulsant drug, valproate, induced proliferation of liver peroxisomes and selectively increased the activity of the enzymes involved in beta-oxidation in these organelles. In kidney cortex, only a moderate increase in enzyme activity could be recorded. Valproate (1% w/w in th...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(91)90557-l

    authors: Ponchaut S,Draye JP,Veitch K,Van Hoof F

    更新日期:1991-05-15 00:00:00

  • Stereochemical aspects of para-chloroamphetamine metabolism. Rabbit liver microsomal metabolism of RS-, R(-)-. and S(+)-para-chloroamphetamine.

    abstract::With the aid of a chiral derivatizing reagent and a sensitive and specific nitrogen-phosphorus gas chromatographic assay, metabolism of para-chloroamphetamine (PCA) enantiomers has been studied following incubation of racemic (RS)-, R(-)- and S(+)-PCA with rabbit liver microsomal preparations. Significant metabolism o...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(82)90228-3

    authors: Ames MM,Frank SK

    更新日期:1982-01-01 00:00:00

  • Cooperation between Apo2L/TRAIL and bortezomib in multiple myeloma apoptosis.

    abstract::The proteasome inhibitor bortezomib is currently an important drug for treatment of relapsed and refractory multiple myeloma (MM) and for elderly patients. However, cells from some patients show resistance to bortezomib. We have evaluated the possibility of improving bortezomib therapy with Apo2L/TRAIL, a death ligand...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2008.11.024

    authors: Balsas P,López-Royuela N,Galán-Malo P,Anel A,Marzo I,Naval J

    更新日期:2009-03-01 00:00:00

  • Characterization of the muscarinic receptor subtype in isolated gastric fundic cells of the rabbit.

    abstract::The characteristics of the muscarinic receptor in isolated gastric fundic cells from rabbit were determined by radioligand binding techniques and functional tests. The dissociation constants (KDS) of selective (hexahydrosiladifenidol and pirenzepine) and non-selective (N-methylscopolamine and atropine) muscarinic rece...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(87)90209-7

    authors: Baudiere B,Monferini E,Giraldo E,Ladinsky H,Bali JP

    更新日期:1987-09-15 00:00:00

  • Effects of MCI-176, a new quinazolinone calcium antagonist, on myocardial energy and carbohydrate metabolism in ischemic dog hearts.

    abstract::The effect of 2-(2,5-dimethoxyphenylmethyl)-3-(2-dimethylaminoethyl)- 6-isopropoxy-4(3H)-quinazolinone hydrochloride (MCI-176), a calcium antagonist, on ischemic myocardial metabolism was studied in dog hearts subjected to an occlusion of the left anterior descending coronary artery (LAD) for 3 or 30 min. MCI-176 (0.0...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(91)90543-e

    authors: Abe Y,Ichihara K,Abiko Y

    更新日期:1991-02-01 00:00:00

  • Effect of superoxide dismutase on glomerular nephritis.

    abstract::The antiinflammatory effect of superoxide dismutase was studied in rats with kidney intoxication induced by the injection of nephrotoxic serum. The urinary excretion of protein was increased significantly by the administration of an intravenous injection of nephrotoxic serum. The daily injection of superoxide dismutas...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(86)90536-8

    authors: Adachi T,Fukuta M,Ito Y,Hirano K,Sugiura M,Sugiura K

    更新日期:1986-01-15 00:00:00

  • Modulation by verapamil of vincristine pharmacokinetics and toxicity in mice bearing human tumor xenografts.

    abstract::The effect of the calcium channel blocker verapamil (VRP) on the accumulation and retention of vincristine (VCR) has been examined in mice bearing xenografts of human rhabdomyosarcomas. The tumors were Rh18, moderately sensitive to VCR, and its subline, Rh18/VCR3, selected in vivo for primary resistance to VCR. Admini...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(89)90405-x

    authors: Horton JK,Thimmaiah KN,Houghton JA,Horowitz ME,Houghton PJ

    更新日期:1989-06-01 00:00:00

  • Kinetics of sulphate conjugation in extracts of human foetal liver cells in culture.

    abstract::Sulphate conjugation was investigated using extracts of human foetal liver cells in culture. The three reactions which are involved in sulphate conjugation were measured singly or in combination: they are (i) the PAPS generation catalyzed by ATP-sulphurylase and adenosine 5'-phosphosulphate (APS)-kinase, (ii) the phen...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(88)90331-0

    authors: Tan TM,Sit KH,Wong KP

    更新日期:1988-12-15 00:00:00

  • Regulation of adenylate cyclase by cannabinoid drugs. Insights based on thermodynamic studies.

    abstract::The abilities of lipophilic cannabinoid drugs to regulate adenylate cyclase activity in neuroblastoma cell membranes were analyzed by thermodynamic studies. Arrhenius plots of hormone-stimulated adenylate cyclase activity exhibited a break point at 20 degrees. The break point was reduced to 14 degrees by benzyl alcoho...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(89)90628-x

    authors: Howlett AC,Scott DK,Wilken GH

    更新日期:1989-10-01 00:00:00

  • Transcriptional regulators of the human multidrug resistance 1 gene: recent views.

    abstract::The multidrug resistance (MDR) phenotype is the major cause of failure of cancer chemotherapy. This phenotype is mainly due to the overexpression of the human MDR1 (hMDR1) gene. Several studies have shown that transcriptional regulation of this gene is unexpectedly complex and is far from being completely understood. ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/s0006-2952(02)01156-5

    authors: Labialle S,Gayet L,Marthinet E,Rigal D,Baggetto LG

    更新日期:2002-09-01 00:00:00

  • Effects of perfluorodecanoic acid on hepatic indices of thyroid status in the rat.

    abstract::Perfluorodecanoic acid (PFDA) alters the circulating level of thyroid hormones, but the physiological significance of this change at the target tissue remains to be defined. To this end, the activities of thyroid-responsive hepatic enzymes were examined in adult male rats 1 week after treatment with a single dose of P...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(87)90091-8

    authors: Kelling CK,Van Rafelghem MJ,Menahan LA,Peterson RE

    更新日期:1987-04-15 00:00:00

  • Stimulation of platelet serotonin transport by substituted 1,4-naphthoquinone-induced oxidant stress.

    abstract::The effect of oxidant stress produced by redox cycling of substituted 1,4-naphthoquinones on the activity of platelet (Na(+)-K+)ATPase and the active transport of serotonin (5-HT) was studied. 2-Methyl-1,4-naphthoquinone (menadione) produced a concentration-dependent (0-100 microM) and time-dependent (2-20 min) stimul...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(91)90203-h

    authors: Bosin TR,Schaltenbrand SL

    更新日期:1991-03-15 00:00:00

  • Interferon gamma enhances proteasome activity in recombinant Hep G2 cells that express cytochrome P4502E1: modulation by ethanol.

    abstract::We tested the influence of IFNgamma on proteasome activity in parental Hep G2 cells that do not metabolize ethanol, as well as in recombinant Hep G2-derived cells that express either or both alcohol dehydrogenase (ADH) and cytochrome P4502E1 (CYP2E1). IFNgamma treatment increased proteasome activity in VL-17A (ADH(+),...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0006-2952(03)00252-1

    authors: Osna NA,Clemens DL,Donohue TM Jr

    更新日期:2003-09-01 00:00:00

  • Clavilactones, a novel class of tyrosine kinase inhibitors of fungal origin.

    abstract::Targeting of deregulated protein tyrosine kinases has been proposed as a new approach in the therapeutic intervention against pathological processes including proliferative disorders and cancer. Using a screening approach based on a comparative evaluation of antiproliferative effects in a panel of tumor cells with dif...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0006-2952(00)00278-1

    authors: Cassinelli G,Lanzi C,Pensa T,Gambetta RA,Nasini G,Cuccuru G,Cassinis M,Pratesi G,Polizzi D,Tortoreto M,Zunino F

    更新日期:2000-06-15 00:00:00

  • Targeting cancer stem cells for more effective therapies: Taking out cancer's locomotive engine.

    abstract::Novel therapies for the treatment of solid tumors have generally failed to improve patient overall survival. These therapeutic approaches are typically focused on targeting signaling pathways implicated in cell growth and/or survival in order to shrink the malignant mass and achieve an objective clinical response; how...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2009.03.020

    authors: Winquist RJ,Boucher DM,Wood M,Furey BF

    更新日期:2009-08-15 00:00:00

  • Thrombin receptor antagonists. Structure-activity relationships for the platelet thrombin receptor and effects on prostacyclin synthesis by human umbilical vein endothelial cells.

    abstract::Structure-activity studies on a series of analogues of N-(3-methyl-S-(1-pyrrolidinyl carbonyl) butyl)-D-alanine ethyl ester hydrochloride (SC42619) have defined the features of this dipeptide analogue required for observation of thrombin receptor antagonist activity on the human platelet. The affinity for SC42619, and...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(90)90037-l

    authors: Ruda EM,Scrutton MC,Manley PW,Tuffin DP

    更新日期:1990-01-15 00:00:00

  • Regulation of carbohydrate metabolism by nitric oxide and hydrogen sulfide: Implications in diabetes.

    abstract::Nitric oxide (NO) and hydrogen sulfide (H2S) are two gasotransmitters that are produced in the human body and have a key role in many of the physiological activities of the various organ systems. Decreased NO bioavailability and deficiency of H2S are involved in the pathophysiology of type 2 diabetes and its complicat...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.bcp.2020.113819

    authors: Gheibi S,Samsonov AP,Gheibi S,Vazquez AB,Kashfi K

    更新日期:2020-06-01 00:00:00

  • Induction of human breast cancer cell apoptosis from G2/M preceded by stimulation into the cell cycle by Z-1,1-dichloro-2,3-diphenylcyclopropane.

    abstract::We have shown previously that Z-1,1-dichloro-2,3-diphenylcyclopropane (a.k.a. Analog II, A(II)) inhibits human breast cancer cell proliferation regardless of estrogen receptor status or estrogen sensitivity, and that its cellular targets include microtubules. In the present study, we investigated the apoptosis-inducin...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0006-2952(98)00289-5

    authors: Balachandran R,ter Haar E,Yalowich JC,Welsh MJ,Grant SG,Day BW

    更新日期:1999-01-01 00:00:00

  • The role of Raf kinase inhibitor protein (RKIP) in health and disease.

    abstract::Raf kinase inhibitor protein (RKIP) is a member of the phosphatidylethanolamine-binding protein (PEBP) family. RKIP plays a pivotal modulatory role in several protein kinase signaling cascades. RKIP binds inhibits Raf-1-mediated phosphorylation of MEK through binding to Raf-1. Protein kinase C (PKC) phosphorylates RKI...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.bcp.2004.04.024

    authors: Keller ET,Fu Z,Brennan M

    更新日期:2004-09-15 00:00:00

  • Peroxide-dependent amino acid oxidation and chemiluminescence catalysed by magnesium-pyridoxal phosphate-glutamate complex.

    abstract::Magnesium-pyridoxal-5'-phosphate-glutamate (MPPG) has been shown to ameliorate atherosclerotic symptoms in rabbits. In vitro, MPPG in the presence of peroxides such as cholesterolhydroperoxide or cumene hydroperoxide and Mn2+ ions produces "excited states" measurable as chemiluminescence or ethylene release from 1-ami...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(92)90442-l

    authors: Meyer BU,Schneider W,Elstner EF

    更新日期:1992-08-04 00:00:00

  • RACking up ceramide-induced islet β-cell dysfunction.

    abstract::The International Diabetes Federation predicts that by 2045 the number of individuals afflicted with diabetes will increase to 629 million. Furthermore, ∼352 million individuals with impaired glucose tolerance are at increased risk for developing diabetes. Several mechanisms have been proposed for the onset of metabol...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.bcp.2018.04.026

    authors: Kowluru A,Kowluru RA

    更新日期:2018-08-01 00:00:00

  • 5,10-Dideazatetrahydrofolic acid reduces toxicity and deoxyadenosine triphosphate pool, expansion in cultured L1210 cells treated with inhibitors of thymidylate synthase.

    abstract::5,10-Dideazatetrahydrofolic acid (DDATHF) reduces de nova purine biosynthesis by inhibiting glycinamide ribonucleotide transformylase. ICI D1964 and CB3717 are folate-based inhibitors of thymidylate synthase (TS). Fluorodeoxyuridine (FdUrd) following metabolism to FdUMP also inhibits TS. In cultured L1210 cells DDATHF...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(94)00458-x

    authors: Chong LK,Tattersall MH

    更新日期:1995-03-15 00:00:00

  • Effects of acute ethanol administration on the uptake of 59Fe-labeled transferrin by rat liver and cerebellum.

    abstract::The uptake of iron by the liver and cerebellum was measured in rats using [59Fe]transferrin. An acute ethanol load (50 mmol/kg body wt., i.p.) elicited a significant increase in the hepatic and cerebellar non-heme iron concentration. The uptake of 59Fe by the liver and the cerebellum was significantly greater in the e...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(94)90313-1

    authors: Rouach H,Houze P,Gentil M,Orfanelli MT,Nordmann R

    更新日期:1994-05-18 00:00:00

  • Heat shock protein 70 protects against bleomycin-induced pulmonary fibrosis in mice.

    abstract::Idiopathic pulmonary fibrosis (IPF) involves infiltration of leucocytes, pulmonary injury, fibrosis and resulting pulmonary dysfunction. Myofibroblasts and transforming growth factor (TGF)-beta1 have been suggested to play a major role in the pathology and the myofibroblasts are derived from both lung epithelial cells...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2010.05.025

    authors: Tanaka K,Tanaka Y,Namba T,Azuma A,Mizushima T

    更新日期:2010-09-15 00:00:00