Effects of Polybrominated Diphenyl Ethers on Rat and Human 11β-Hydroxysteroid Dehydrogenase 1 and 2 Activities.

Abstract:

:Polybrominated diphenyl ethers (PBDEs) are a class of brominated flame retardants. PBDEs have been widely used in textiles, flexible polyurethane foams, electronic components, electrical components, and plastics. 11β-Hydroxysteroid dehydrogenases, isoform 1 (HSD11B1) and isoform 2 (HSD11B2), have been demonstrated to be the regulators of local glucocorticoid levels. In this study, the potencies of 4 different PBDEs (BDE-3, BDE-47, BDE-100, and BDE-153) with 1-6 bromine atoms attached in inhibition of rat and human HSD11B1 and HSD11B2 activities were compared to 4-bromobiphenyl (BBP), a structurally similar compound. All 4 PBDEs and BBP did not inhibit rat and human HSD11B1. BDE-3 and BDE-47 potently inhibited rat HSD11B2, and BDE-47 and BDE-153 potently inhibited human HSD11B2, with the half maximal inhibitory concentration values of 12.42, 5.95, 11.97, and 4.41 µmol/l, respectively. All PBDEs noncompetitively inhibited HSD11B2 when a steroid substrate was used. However, PBDEs exerted uncompetitive inhibition when the cofactor NAD+ was used. In conclusion, some PBDEs are selective inhibitors of HSD11B2, possibly causing excessive glucocorticoid action in local tissues.

journal_name

Pharmacology

journal_title

Pharmacology

authors

Chen X,Dong Y,Cao S,Li X,Wang Z,Chen R,Ge RS

doi

10.1159/000445213

subject

Has Abstract

pub_date

2016-01-01 00:00:00

pages

115-23

issue

3-4

eissn

0031-7012

issn

1423-0313

pii

000445213

journal_volume

98

pub_type

杂志文章
  • Aspirin, indomethacin, and tartrazine increase carotid-sinus-nerve activity and arterial blood pressure in guinea pigs.

    abstract::Acetylsalicylic acid (ASA; 0.1-10 mg/kg), indomethacin (IND; 0.1-1.0 mg/kg), and tartrazine (TZ; 0.1-2.0 mg/kg), given intravenously induced dose-dependent increases in carotid-sinus nerve (CSN) activity, accompanied by increases in mean arterial blood pressure (MABP), but only the IND-induced MABP increases were dose...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000138258

    authors: D'Souza SJ,Biggs DF

    更新日期:1987-01-01 00:00:00

  • Therapeutic drug monitoring of the HIV/AIDS drugs abacavir, zidovudine, efavirenz, nevirapine, indinavir, lopinavir, and nelfinavir.

    abstract::Combination therapy with antiretroviral drugs is used for the treatment of patients infected with the human immunodeficiency virus. To achieve optimal drug concentrations for viral suppression and avoidance of drug toxicity, monitoring of drug levels has been considered essential. We set up an analytical procedure for...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000073664

    authors: Donnerer J,Kronawetter M,Kapper A,Haas I,Kessler HH

    更新日期:2003-12-01 00:00:00

  • Irreversible inhibition of [3H]glycine transport into channel catfish erythrocytes by thiol group modifiers.

    abstract::Erythrocytes can take up amino acids from the blood by using a variety of transport systems. GLYT is a key transport protein in the plasma membrane responsible for the Na(2+)-dependent uptake of glycine needed for glutathione biosynthesis. Certain cysteine-specific compounds, particularly mercuric chloride and 5,5'-di...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000074973

    authors: McCormick SJ,Tunnicliff G

    更新日期:2004-03-01 00:00:00

  • Lithium absorption, distribution and clearance and body temperature in rats given lithium plus haloperidol.

    abstract::Renal lithium clearance, tissue lithium levels, serum lithium concentration, and body temperature were determined in rats given lithium alone or combined with haloperidol (0.5-1 mg/kg). A slight increase in serum lithium concentration occurred in one of the three groups given lithium plus haloperidol. Haloperidol fail...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000136708

    authors: Smith DF,Shimizu M,Schou M

    更新日期:1977-01-01 00:00:00

  • A bioequivalence study of two oral desmopressin tablet formulations.

    abstract::The present study was carried out to test bioequivalence between two different oral desmopressin formulations. Sixty healthy volunteers were enrolled in the study and were randomly assigned to receive the test (T) and reference (R) drug in a two-period two-sequence, crossover, analyst-blinded study design. Subjects re...

    journal_title:Pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1159/000092625

    authors: Kaehler ST,Steiner IM,Sauermann R,Scheidl H,Mueller M,Joukhadar C

    更新日期:2006-01-01 00:00:00

  • On the heterogeneity of mast cells.

    abstract::Mast cells from different locations are shown to vary in their histochemical, ultrastructural, cytochemical and functional properties. The clinical consequences of this heterogeneity and possible reasons for its origin are discussed. ...

    journal_title:Pharmacology

    pub_type: 杂志文章,评审

    doi:10.1159/000138153

    authors: Pearce FL

    更新日期:1986-01-01 00:00:00

  • Lisuride acts at multiple sites to induce ocular hypotension and mydriasis.

    abstract::Topically unilaterally applied lisuride caused dose-related lowering of intraocular pressure in ipsilateral (treated) but not in contralateral eyes of normal rabbits. The ocular hypotensive response induced by lisuride was antagonized by pretreatment with metoclopramide, a dopamine receptor antagonist, and was partial...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000028249

    authors: Potter DE,Ogidigben MJ,Chu TC

    更新日期:1998-11-01 00:00:00

  • Time course of the distribution of morphine in brain regions, spinal cord and serum following intravenous injection to rats of differing ages.

    abstract::Previously it was demonstrated that intravenously administered morphine produced greater analgesic but lower hyperthermic responses to morphine in 24-week-old rats in comparison to 8-week-old rats. The differential pharmacological responses to morphine could not solely be attributed to the pharmacokinetic parameters, ...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000139073

    authors: Bhargava HN,Villar VM,Rahmani NH,Larsen AK

    更新日期:1993-07-01 00:00:00

  • The Efficacy of Rituximab Combined with 131I for Ophthalmic Outcomes of Graves' Ophthalmopathy Patients.

    abstract:PURPOSE:The purpose of this study is to examine the effectiveness of introducing both rituximab (RTX) and 131I for active Graves' ophthalmopathy (GO) with hyperthyroidism. METHODS:In total, 217 patients suffering from active GO with hyperthyroidism were included in this research. All subjects were randomly assigned to...

    journal_title:Pharmacology

    pub_type: 杂志文章,随机对照试验

    doi:10.1159/000453618

    authors: Li J,Xiao Z,Hu X,Li Y,Zhang X,Zhang S,Gong W,Zhao J,Ye X

    更新日期:2017-01-01 00:00:00

  • Control of 2,3,7,8-tetrachlorodibenzo-p-dioxin binding protein(s) in the hamster kidney.

    abstract::Hamster renal cytosol binds [3H]-2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) with high specificity. Sucrose density gradient centrifugation revealed two binding entities- one with a low sedimentation coefficient of 4-5 S which was displaced by neither TCDD nor other polycyclic aromatic hydrocarbons (PAHs) and another w...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000138074

    authors: Kurl RN,Loring JM,Villee CA

    更新日期:1985-01-01 00:00:00

  • The structure-action relationship and kinetics of some naloxone and naltrexone derivatives.

    abstract::The isolated longitudinal muscle preparation (with attached Auerbach plexus) of the guinea pig ileum was used to investigate the structure activity relationship and kinetics of some naloxone and naltrexone derivatives and that of cyclazocine. The agonist used for the investigation of the antagonistic effect of these c...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000136582

    authors: Vizi ES,Foldes FF,Rich J,Knoll J

    更新日期:1976-01-01 00:00:00

  • Effects of cyclic adenosine monophosphate-dependent protein kinase and calcium-dependent protein kinase modulators on stimulated gastric acid secretion in the perfused rat stomach.

    abstract::The effects of cyclic adenosine monophosphate-dependent protein kinase (PKA) and calcium-dependent protein kinase (PKC) modulators on secretagogue-stimulated gastric acid secretion were studied in the continuously perfused stomach of the anesthetized rat. Intravenous histamine (0.25 mg/kg/h) and pentagastrin (2 microg...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000139368

    authors: Rotker JD,Strapko A,Nandi J,Bosche MC,Levine RA

    更新日期:1995-10-01 00:00:00

  • Effects of peptides and amines on isolated guinea pig tracheae as influenced by inhibitors of the metabolism of arachidonic acid.

    abstract::Stimulants (histamine, acetylcholine and substance P) and relaxants (isoprenaline and bradykinin) of the guinea pig trachea were tested in the absence and presence of mepacrine, eicosatetraynoic acid, BW 755C and indomethacin in order to evaluate the involvement of prostaglandins and congeners in the effects of amines...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000137758

    authors: Mizrahi J,D'Orléans-Juste P,Caranikas S,Regoli D

    更新日期:1982-01-01 00:00:00

  • Reversible, narcotic-associated mental status impairment in patients with metastatic cancer.

    abstract::Pain and mental status were assessed in a series of 35 consecutive hospitalized patients with metastatic cancer receiving narcotics for pain that was difficult to control. Forty-five episodes of mental status impairment were detected in 27 of these patients. Fifteen patients had dose-related oversedation or organic br...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000138294

    authors: Leipzig RM,Goodman H,Gray G,Erle H,Reidenberg MM

    更新日期:1987-01-01 00:00:00

  • Periplaneta Americana Extract May Attenuate Renal Fibrosis through Inhibiting Janus Tyrosine Kinase 2/Signal Transducer and Activator of Transcription 3 Pathway.

    abstract:BACKGROUND:Periplaneta americana is one of the ancient insect groups with the strongest vitality. Periplaneta americana extract (PAE) has been explored as an alternative remedy for many diseases. Although much progress has been made in the study about PAE, the role of the drug in renal disease is rarely reported, espec...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000488535

    authors: Liu J,Zhou L,He L,Zhong Y,Zhang X,Xiao B,Liu G

    更新日期:2018-01-01 00:00:00

  • Effect of carvedilol on renal hemodynamics and renal excretory function in spontaneously hypertensive rats.

    abstract::The effects of the novel antihypertensive agent, carvedilol, on renal hemodynamics and excretory function have been investigated and compared with the effects of labetalol in conscious, spontaneously hypertensive rats. Sustained intravenous infusion of carvedilol or labetalol at a rate of 10 micrograms/kg/min resulted...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000138719

    authors: Gellai M,DeWolf R,Ruffolo RR Jr

    更新日期:1990-01-01 00:00:00

  • Effect of ketotifen on the production of reactive oxygen species from human eosinophils primed by eotaxin.

    abstract::Ketotifen is an antiallergic drug and may have direct inhibitory effects on eosinophils. To investigate the anti-eosinophilic effect of ketotifen, we examined the effect of ketotifen on the production of reactive oxygen species (ROS) from eotaxin-primed human eosinophils. Ketotifen at 10(-10)-10(-6) mol/l significantl...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000072666

    authors: Yamada Y,Sannohe S,Saito N,Cui CH,Ueki S,Oyamada H,Kanda A,Yamaguchi K,Hamada K,Adachi T,Kayaba H,Chihara J

    更新日期:2003-11-01 00:00:00

  • Effects of spasmogens on relaxant dose-response curves to full or partial agonists at beta-adrenoceptors of guinea pig isolated trachea.

    abstract::When guinea pig isolated trachea is contracted with either carbachol or methacholine, relaxant concentration-response curves to isoprenaline, salmefamol and fenoterol were shifted to the right, compared with curves obtained with either spontaneous or histamine-induced tone. Carbachol and methacholine also reduced the ...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000138256

    authors: Hutson PA,Carpenter JR

    更新日期:1987-01-01 00:00:00

  • Effects of different cyclooxygenase inhibitors on the segmental distribution of pulmonary vascular resistance in the dog.

    abstract::An increase in pulmonary vascular resistance (PVR) after cyclooxygenase inhibition (COI) is well documented in the dog, but the site of vasoconstriction to chemically distinct cyclooxygenase inhibitors is largely unknown. The purpose of the present study was to examine and compare equimolar concentrations of three che...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000138935

    authors: Endrédi J,el-Kashef HA,Hofman WF,Ehrhart IC

    更新日期:1992-01-01 00:00:00

  • Effect of nabumetone treatment on vascular responses of the thoracic aorta in rat experimental arthritis.

    abstract::Nabumetone is a nonsteroidal anti-inflammatory (NSAI) drug which is known to cause less gastrointestinal damage than other NSAI drugs. This study was performed to evaluate whether nabumetone treatment might alter the vascular aberrations related to inflammation in a rat model of adjuvant-induced arthritis. Nabumetone ...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000028358

    authors: Ulker S,Onal A,Hatip FB,Sürücü A,Alkanat M,Koşay S,Evinç A

    更新日期:2000-04-01 00:00:00

  • Unexpected insensitivity of the cholinergic motor responses to morphine in the human small intestine.

    abstract:BACKGROUND/AIMS:morphine is known to inhibit cholinergic contractions of the guinea pig small intestine. This has been compared to the human small intestinal innervated longitudinal muscle in the current study. METHODS:cholinergic primary contractions of human small intestinal longitudinal strips were evoked by electr...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000316637

    authors: Benko R,Molnár Z,Nemes D,Dékány A,Kelemen D,Illényi L,Cseke L,Papp A,Varga G,Bartho L

    更新日期:2010-01-01 00:00:00

  • Effect of vasoactive intestinal peptide and naloxone combination on urinary N-acetyl-beta-D-glucosaminidase level and kidney histology of rats exposed to severe hemorrhage.

    abstract::Renal hypoperfusion which occurs in hemorrhagic shock creates an environment in which cellular injury and organ dysfunction can occur during the episode of shock as well as reoxygenation and reperfusion. At the same time, mast cell degranulation which is observed during hemorrhage may have an additional deleterious ef...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000139097

    authors: Akin MZ,Tunçel N,Gürer F,Kural N,Uslu S

    更新日期:1993-09-01 00:00:00

  • Lidocaine Reversible Inactivation of the Central Nucleus of Amygdala Impairs Acquisition, Consolidation, and Retrieval of Morphine State-Dependent Learning in Rat.

    abstract:BACKGROUND/AIMS:Morphine causes state-dependent learning that its mechanism and brain-related structures are not fully understood. This study aimed to determine whether lidocaine reversible inactivation of the central nucleus of the amygdala (CeA) could affect acquisition, consolidation, and retrieval of morphine state...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000503726

    authors: Noorbakhshnia M,Rahmani-Samani P,Eivani M

    更新日期:2020-01-01 00:00:00

  • Effects induced by Tityus serrulatus scorpion venom and its toxins TsTX-I and TsTX-V on the rat isolated retractor penis muscle.

    abstract::The aims of the present study were to investigate the pharmacological effects induced by Tityus serrulatus venom (TsV) and its fractions and to compare with the effects induced by pure alpha (TsTX-V) and beta (TsTX-I) toxins isolated from TsV on rat retractor penis muscle (RPM). TsV, fractions X, XI, XIIa, XIIb (0.01-...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000082804

    authors: Bomfim JH,de Godoy MA,Giglio JR,de Oliveira AM,Arantes EC

    更新日期:2005-03-01 00:00:00

  • Comparison of suprofen and ibuprofen in the treatment of pain secondary to osteoarthritis.

    abstract::43 patients with osteoarthritis of the knee and/or hip(s) were treated with suprofen 800 mg/day or ibuprofen 1,600 mg/day for 14 days. Both drugs produced an improvement in subjective symptoms by day 7, although the most rapid analgesic effect was obtained with suprofen. Patients receiving suprofen experienced a signi...

    journal_title:Pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1159/000137898

    authors: Schuermans Y

    更新日期:1983-01-01 00:00:00

  • Availability of learned helplessness test as a model of depression compared to a forced swimming test in rats.

    abstract::This study was designed to evaluate the antidepressant activity of various antidepressants using the learned helplessness test (LH) or the forced swimming test (FS) in rats. Repeated treatment of the tricyclic antidepressants imipramine (10 mg/kg, p.o.), clomipramine (0.625 mg/kg, p.o.), amitriptyline (10 mg/kg, p.o.)...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000056126

    authors: Takamori K,Yoshida S,Okuyama S

    更新日期:2001-01-01 00:00:00

  • Effects of fructose-1,6-diphosphate on the activity of rat liver nitric oxide synthase in vitro.

    abstract::Fructose-1,6-diphosphate (FDP) was found to cause significant stimulation of nitric oxide synthase (NOS) in rat liver homogenates in vitro. This effect was more pronounced for the inducible isoform than its constitutive counterpart. Furthermore, FDP restored rat liver inducible NOS levels following their depletion by ...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000139468

    authors: Mihas AA,Maliakkal RJ,Mihas TA,Kanji VK,Markov AK

    更新日期:1997-01-01 00:00:00

  • Nitric oxide reduces myocardial contractility in isoproterenol-stimulated rat hearts by a mechanism independent of cyclic GMP or cyclic AMP.

    abstract::Nitric oxide has been shown to decrease myocardial contractility and O2 consumption. This study was designed to evaluate the hypothesis that nitric oxide-mediated increases in cyclic GMP require elevated cyclic AMP to produce cardiac depression. Using isolated, Langendorff-perfused rat hearts, we determined the effect...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000139529

    authors: Weiss HR,Sadoff JD,Scholz PM,Klabunde RE

    更新日期:1997-10-01 00:00:00

  • Efficacy and safety of prolonged-release trazodone in major depressive disorder: a multicenter, randomized, double-blind, flexible-dose trial.

    abstract:OBJECTIVE:To investigate the efficacy, safety, and clinical benefit of prolonged-release trazodone (Trittico) in the treatment of major depressive disorder (MDD). METHODS:In this study, 363 Chinese patients with MDD were randomized 1:1 to receive either prolonged-release trazodone (150-450 mg) or placebo treatment for...

    journal_title:Pharmacology

    pub_type: 杂志文章,多中心研究,随机对照试验

    doi:10.1159/000368559

    authors: Zhang L,Xie WW,Li LH,Zhang HG,Wang G,Chen DC,Cao Y,Cui LJ,Zhang KR,Shi JG,Tan QR,Zheng HB,Xu XF,Cheng ZH,Zhao JP

    更新日期:2014-01-01 00:00:00

  • Regional cerebral glucose utilization during vasopressin-induced barrel rotations or bicuculline-induced seizures in rats.

    abstract::Regional cerebral metabolic rates of glucose (rCMRglu) were measured in conscious rats grouped according to three treatments: control, bicuculline (5.5 mg/kg s.c.), and intracerebroventricular arginine vasopressin (0.5 micrograms/5 microliter). Rats in the latter group were pre-exposed to the peptide 48 h earlier to r...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000138340

    authors: Wurpel JN,Dundore RL,Bryan RM Jr,Keil LC,Severs WB

    更新日期:1988-01-01 00:00:00