Selective androgen insensitivity of hepatic drug-metabolizing enzymes in senescent mice.

Abstract:

:The normal sexual dimorphism in murine hepatic hexobarbital metabolism (i.e. females greater than males) was found to be absent in senescent animals. Hexobarbital metabolism, expressed as microsomal activity of hexobarbital hydroxylase and hexobarbital-induced sleep time, in senescent male mice was similar to that in females, but significantly greater than that found in young adult males. No age-related changes in hexobarbital metabolism were observed in intact females. In addition, experiments involving gonadectomies and testosterone administration indicated that both male and female senescent mice were insensitive to the normally repressive effects of androgens on hexobarbital hydroxylase. In contrast, the sexual dimorphism in the activity of p-nitrophenol UDP-glucuronosyltransferase was maintained in the senescent mice as well as the usual responsiveness to testosterone regulation. Furthermore, the growth-promoting effects of androgen on the kidneys and seminal vesicles were similarly expressed in young and old mice. Thus, our results suggest the development of an age-dependent and selective insensitivity of hexobarbital hydroxylase to androgenic regulation in the aging mouse.

journal_name

Biochem Pharmacol

journal_title

Biochemical pharmacology

authors

Niedermeyer TM,Shapiro BH

doi

10.1016/0006-2952(88)90724-1

subject

Has Abstract

pub_date

1988-01-15 00:00:00

pages

241-6

issue

2

eissn

0006-2952

issn

1873-2968

pii

0006-2952(88)90724-1

journal_volume

37

pub_type

杂志文章
  • 3-(13-Hydroxytridecyl)-1-[13-(3-pyridyl)tridecyl]pyridinium chloride (YM-53792), a novel inhibitor of NF-AT activation.

    abstract::A compound, YM-53792, was identified as an inhibitor of interleukin-2 (IL-2) gene promoter activity, using a Jurkat cell-based reporter system in which the luciferase gene is regulated by the IL-2 gene promoter. Production of IL-2, interleukin-4 (IL-4) and interleukin-5 (IL-5) from human peripheral blood mononuclear c...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0006-2952(97)00289-x

    authors: Kuromitsu S,Fukunaga M,Lennard AC,Masuho Y,Nakada S

    更新日期:1997-11-01 00:00:00

  • Allosteric regulation of arylamine N-acetyltransferase 1 by adenosine triphosphate.

    abstract::In the present study, a screen of adenosine analogs as potential modulators of arylamine-N-acetyltransferase 1 activity identified ATP as an inhibitor within its range of physiological concentrations. Kinetically, ATP was a non-competitive inhibitor with respect to the acetyl acceptor but a competitive inhibitor with ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2018.10.013

    authors: Minchin RF,Rosengren KJ,Burow R,Butcher NJ

    更新日期:2018-12-01 00:00:00

  • Transport and metabolism of double-labelled CDPcholine in mammalian tissues.

    abstract::Double-labelled [methyl-14C,5-3H]CDPcholine has been synthesized and subjected to a pharmacokinetic analysis in several biological systems. In transport experiments with intact human erythrocytes no incorporation of radioactivity is observable. On the other hand the results obtained with perfused rat liver suggest a r...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(85)90204-7

    authors: Galletti P,De Rosa M,Nappi MA,Pontoni G,del Piano L,Salluzzo A,Zappia V

    更新日期:1985-12-01 00:00:00

  • Purification of the human blood platelet thromboxane A2/prostaglandin H2 receptor protein.

    abstract::The human platelet thromboxane A2/prostaglandin H2 receptor has been purified 6100-fold to apparent homogeneity by a three-step chromatographic procedure with an overall yield of 6%. A 6-fold purification of the receptor was first achieved by chromatography of 3-[(3-cholamidopropyl)dimethyl-ammonio]-1-propanesulfonate...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(92)90294-s

    authors: Kim SO,Lim CT,Lam SC,Hall SE,Komiotis D,Venton DL,Le Breton GC

    更新日期:1992-01-22 00:00:00

  • Aspirin and indomethacin reduce lung inflammation of mice exposed to cigarette smoke.

    abstract::Neutrophil accumulation response to cigarette smoke (CS) in humans and animal models is believed to play an important role in pathogenesis of many tobacco-related lung diseases. Here we evaluated the lung anti-inflammatory effect of aspirin and indomethacin in mice exposed to CS. C57BL/6 mice were exposed to four ciga...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2008.12.012

    authors: Castro P,Nasser H,Abrahão A,Dos Reis LC,Riça I,Valença SS,Rezende DC,Quintas LE,Cavalcante MC,Porto LC,Koatz VL

    更新日期:2009-03-15 00:00:00

  • Synthesis and pharmacological evaluation of the novel pseudo-symmetrical tamoxifen derivatives as anti-tumor agents.

    abstract::Four pseudo-symmetrical tamoxifen derivatives, RID-B (13), RID-C (14), RID-D (15), and bis(dimethylaminophenetole) (16), were synthesized via the novel three-component coupling reaction, and the structure-activity relationships of these pseudo-symmetrical tamoxifen derivatives were examined. It was discovered that 13 ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2007.11.005

    authors: Shiina I,Sano Y,Nakata K,Kikuchi T,Sasaki A,Ikekita M,Nagahara Y,Hasome Y,Yamori T,Yamazaki K

    更新日期:2008-03-01 00:00:00

  • The selective 5-HT2A receptor agonist 25CN-NBOH: Structure-activity relationship, in vivo pharmacology, and in vitro and ex vivo binding characteristics of [3H]25CN-NBOH.

    abstract::The remarkable effects exhibited by classical psychedelics in recent clinical trials have spawned considerable interest in 5-HT2A receptor (5-HT2AR) activation as a treatment strategy for several psychiatric/cognitive disorders. In this study we have continued our development of 25CN-NBOH, one of the most 5-HT2AR-sele...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2020.113979

    authors: Jensen AA,Halberstadt AL,Märcher-Rørsted E,Odland AU,Chatha M,Speth N,Liebscher G,Hansen M,Bräuner-Osborne H,Palner M,Andreasen JT,Kristensen JL

    更新日期:2020-07-01 00:00:00

  • Endogenous monoamine oxidase inhibitor-like substances in monkey brain.

    abstract::The extraction and partial purification of endogenous "monoamine oxidase (MAO) inhibitor-like" material from the monkey brain are described. The endogenous material (F-1 and F-2) obtained after Bio-Gel P-2 gel filtration and silica column chromatography inhibited MAO in the monkey brain mitochondria toward 5-hydroxytr...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(89)90204-9

    authors: Egashira T,Obata T,Nagai T,Kimba Y,Takano R,Yamanaka Y

    更新日期:1989-02-15 00:00:00

  • Bromodomains: Structure, function and pharmacology of inhibition.

    abstract::Bromodomains are epigenetic readers of histone acetylation involved in chromatin remodeling and transcriptional regulation. The human proteome comprises 46 bromodomain-containing proteins with a total of 61 bromodomains, which, despite highly conserved structural features, recognize a wide array of natural peptide lig...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.bcp.2015.12.005

    authors: Ferri E,Petosa C,McKenna CE

    更新日期:2016-04-15 00:00:00

  • Tetradecanoyl phorbol-13-acetate counteracts the responsiveness of cultured thyroid cells to thyrotropin.

    abstract::We have studied the effects of TPA on the metabolism of porcine thyroid cells cultured for 1-4 days in the absence (control cells) and in the presence of 0.1 mU/ml TSH (TSH cells). The phospholipid turnover, evaluated after a 2 hr incorporation of 32P-phosphate into phospholipids, is markedly modified by the presence ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(85)90427-7

    authors: Haye B,Aublin JL,Champion S,Lambert B,Jacquemin C

    更新日期:1985-11-01 00:00:00

  • Protective effect of erythropoietin on the oxidative damage of erythrocyte membrane by hydroxyl radical.

    abstract::Treatment of red blood cells with the copper (II) ascorbate system causes increased lipid peroxidation, increased membrane microviscosity, and phospholipid translocation with a concurrent decrease in cytosolic catalase and glutathione peroxidase activities. All these changes are prevented if the cells are treated with...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0006-2952(99)00277-4

    authors: Chattopadhyay A,Choudhury TD,Bandyopadhyay D,Datta AG

    更新日期:2000-02-15 00:00:00

  • Stimulation of drug and carcinogen metabolism by prolonged oral tobacco consumption.

    abstract::Oral administration of tobacco to rats for 21 days caused remarkable stimulation of the metabolism of phenacetin, aniline and benzo[a]pyrene, a carcinogen, by hepatic microsomal mixed function oxidases (MFO). Such treatment for 6 days resulted in a small increase in the activities of phenacetin O-dealkylase and aromat...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(82)90386-0

    authors: Kaur S,Ali B

    更新日期:1982-04-15 00:00:00

  • Preparation and characterization of subcellular fractions from the liver of the Northern Pike, Esox lucius.

    abstract::The present study was designed to prepare and characterize subcellular fractions from the liver of the Northern pike (Esox lucius), with special emphasis on the preparation of microsomal fractions suitable for studying xenobiotic metabolism. The purity of the different fractions obtained by differential centrifugation...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(82)90371-9

    authors: Balk L,Meijer J,Bergstrand A,Aström A,Morgenstern R,Seidegård J,DePierre JW

    更新日期:1982-04-15 00:00:00

  • Regulation of cyclic AMP metabolism in bovine adrenal medullary cells.

    abstract::The capacity of cultured bovine adrenal medullary cells to metabolize and export cyclic AMP has been studied. Basal cellular cyclic AMP levels were increased 50% by 100 microM 3-isobutyl-1-methylxanthine (IBMX) and rolipram, a class IV (cyclic AMP-specific) phosphodiesterase (PDE) inhibitor. They were not affected by ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(92)90335-g

    authors: Marley PD,Thomson KA

    更新日期:1992-12-01 00:00:00

  • Evidence for the involvement of a carboxyl group in the vicinity of the MK801 and magnesium ion binding site of the N-methyl-D-aspartate receptor.

    abstract::A series of protein modifying reagents were tested for their effects on the specific binding of [3H]MK801 to adult rat brain membranes. N-Bromosuccinimide, acetyl imidazole, 2,3-butanedione, 5,5'-dithiobis-(2-nitrobenzoic acid) and dithiothreitol all had no significant effect on binding. The carboxylic acid residue mo...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(93)90133-h

    authors: Chazot PL,Fotherby A,Stephenson FA

    更新日期:1993-02-09 00:00:00

  • Lawsone derivatives target the Wnt/β-catenin signaling pathway in multidrug-resistant acute lymphoblastic leukemia cells.

    abstract::Multidrug resistance (MDR) represents a serious problem in cancer treatment. One strategy to overcome this obstacle is to identify agents that are selectively lethal to MDR cells. The aim of this study was to discover novel compounds against MDR leukemia and to determine the molecular mechanisms behind collateral sens...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2017.10.008

    authors: Hamdoun S,Fleischer E,Klinger A,Efferth T

    更新日期:2017-12-15 00:00:00

  • Zardaverine as a selective inhibitor of phosphodiesterase isozymes.

    abstract::The pyridazinone derivative zardaverine has recently been introduced as a potent bronchodilator in vivo and in vitro. In addition, zardaverine exerts a positive inotropic action on heart muscle in vitro. The actions of zardaverine are thought to be mediated via inhibition of phosphodiesterase (PDE) activity. Recent da...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(91)90694-z

    authors: Schudt C,Winder S,Müller B,Ukena D

    更新日期:1991-06-21 00:00:00

  • Cucurbitacin E-induced disruption of the actin and vimentin cytoskeleton in prostate carcinoma cells.

    abstract::Cucurbitacin E has been identified by an empiric screening strategy as a sterol with potent growth inhibitory activity in vitro directed against prostate carcinoma explants (IC50 of 7-50 nM in 2- to 6-day exposures). The mechanism of cucurbitacin cytoxicity has not been elucidated previously. In the present study, we ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0006-2952(96)00557-6

    authors: Duncan KL,Duncan MD,Alley MC,Sausville EA

    更新日期:1996-11-22 00:00:00

  • Tissue distribution of captopril, reducible captopril conjugates and S-methylcaptopril in the rat.

    abstract::The tissue distribution of captopril, an antihypertensive drug possessing a free sulfhydryl group, and its sulfur-conjugated metabolites was studied in rats by gas chromatography-mass spectrometry at 15, 30 and 60 min following a single 10 mg/kg oral dose of captopril. It was found that tissue accumulation of captopri...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(83)90328-3

    authors: Drummer OH,Worland PJ,Jarrott B

    更新日期:1983-05-15 00:00:00

  • In vitro and in vivo inhibition by benserazide of clorgyline-resistant amine oxidases in rat cardiovascular tissues.

    abstract::Bernserazide (D,L-serine 2-[2,3,4-trihydroxybenzyl]-hydrazide) as been shown to inhibit the clorgyline-resistant amine oxidase (CRAO) activities which metabolize benzylamine in homogenates of rat aorta, heart and brown adipose tissue. In vitro studies showed a concentration- and time-dependent inhibition of CRAO in he...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(82)90037-5

    authors: Lyles GA,Callingham BA

    更新日期:1982-04-01 00:00:00

  • Stereoselective metabolism of 3-isopropyl-5-(1-naphthoxymethyl)oxazolidine, a prodrug of propranolol.

    abstract::This investigation suggests that the oxazolidine derivative of propranolol is a prodrug which is hydrolysed stereoselectively to propranolol by hepatic post-mitochondrial supernatant. The (S)-form of the prodrug is more stable in the biological system than its (R)-form. ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(91)90113-j

    authors: Kamal A,Rao AB,Rao MV

    更新日期:1991-05-01 00:00:00

  • Characterization of sequence-dependent synergy between ZD1839 ("Iressa") and oxaliplatin.

    abstract:UNLABELLED:ZD1839 ("Iressa"), a selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI), is currently undergoing preclinical and clinical evaluation in several solid tumors. The present study aimed to assess the effect of ZD1839 in combination with oxaliplatin in the colon cancer cell lines HT-2...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0006-2952(03)00291-0

    authors: Xu JM,Azzariti A,Severino M,Lu B,Colucci G,Paradiso A

    更新日期:2003-08-15 00:00:00

  • Specific binding of 125I SCH 23982, a selective dopamine (D1) receptor ligand to plasma membranes derived from human kidney cortex.

    abstract::Binding of the selective D-1 dopamine receptor ligand 125I SCH 23982 was studied using crude plasma membranes derived from human renal cortex. 125I SCH 23982 bound saturably to a single high affinity site (Kd = 650 pM, Bmax = 19 fmol/mg protein). Binding at 37 degrees was rapid and reversible with forward and reverse ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(89)90231-1

    authors: Hughes A,Sever P

    更新日期:1989-03-01 00:00:00

  • Suppression of cytokine production and neural cell death by the anti-inflammatory alkaloid cepharanthine: a potential agent against HIV-1 encephalopathy.

    abstract::Inflammatory cytokines and human immunodeficiency virus type 1 (HIV-1) gp120 are considered to play an important role in the pathogenesis of HIV-1-associated CNS disorders. These substances are produced predominantly by HIV-1-infected or activated macrophages and microglia in the brain and induce neural cell death. Ce...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0006-2952(01)00692-x

    authors: Okamoto M,Ono M,Baba M

    更新日期:2001-09-15 00:00:00

  • Allosteric regulation of cloned m1-m5 muscarinic receptor subtypes.

    abstract::Allosteric regulation of [3H]N-methylscopolamine [( 3H]NMS) and [3H]quinuclidinyl benzilate [( 3H]QNB) dissociation from the m1-m5 muscarinic receptor subtypes was examined in transfected CHO-K1 cells. Half-times of dissociation of [3H]NMS from cell membranes (at 23 degrees) ranged from less than 5 min for the m2 subt...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(91)90591-r

    authors: Ellis J,Huyler J,Brann MR

    更新日期:1991-10-24 00:00:00

  • Gli family transcription factors are drivers of patupilone resistance in ovarian cancer.

    abstract::Epothilones constitute a novel class of antitubulin agents that are active in patients who relapse after treatment with other chemotherapeutics. This study investigated the molecular mechanisms leading to the onset of epothilone-B (patupilone) resistance in ovarian cancer. Results demonstrated that the Gli family of t...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2012.08.019

    authors: Mozzetti S,Martinelli E,Raspaglio G,Prislei S,De Donato M,Filippetti F,Shahabi S,Scambia G,Ferlini C

    更新日期:2012-12-01 00:00:00

  • Molecular characterization of functional UDP-glucuronosyltransferases 1A and 2B in common marmosets.

    abstract::UDP-glucuronosyltransferases (UGTs) are essential drug-conjugation enzymes that metabolize a variety of endobiotic and xenobiotic substrates. The molecular characteristics of UGTs have been extensively investigated in humans, but remain to be investigated in common marmosets, a nonhuman primate species widely used in ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2019.113748

    authors: Uno Y,Uehara S,Inoue T,Kawamura S,Murayama N,Nishikawa M,Ikushiro S,Sasaki E,Yamazaki H

    更新日期:2020-02-01 00:00:00

  • Effect of early inorganic lead exposure on rat blood-brain barrier permeability to tyrosine or choline.

    abstract::The primary objective of this research was to test the hypothesis that low level lead (Pb) exposure during early life leads to disruption in blood-brain barrier (BBB) function in the young rat. Newborn rats received lead via milk from lactating dams that were drinking water containing 0.1% lead acetate Pb(Ac)2. Pups w...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(82)90491-9

    authors: Michaelson IA,Bradbury M

    更新日期:1982-05-15 00:00:00

  • Identification of glutathione S-transferase as a determinant of 4-hydroperoxycyclophosphamide resistance in human breast cancer cells.

    abstract::Aldehyde dehydrogenase (ALDH) is well known for its involvement in the resistance of tumor cells to cyclophosphamide (CPA) and its activated derivatives, such as 4-hydroperoxy-CPA (4HC). The role of other drug-metabolizing enzymes such as glutathione S-transferase (GST) in CPA resistance is, however, less certain. In ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(95)00079-f

    authors: Chen G,Waxman DJ

    更新日期:1995-05-26 00:00:00

  • Pharmacokinetics relevant to the anti-carcinogenic and anti-tumor activities of glucarate and the synergistic combination of glucarate:retinoid in the rat.

    abstract::Alone and in synergistic combination with retinoids, dietary glucarate inhibits both the chemical induction and growth of rat mammary tumors. To investigate the pharmacokinetics of glucarate, [14C]glucarate was synthesized, converted to the calcium salt, and administered to rats bearing primary mammary tumors. When gi...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(94)90544-4

    authors: Webb TE,Pham-Nguyen MH,Darby M,Hamme AT 2nd

    更新日期:1994-04-29 00:00:00