当前位置： SCI文献检索 > BIOCHEMICAL PHARMACOLOGY期刊下所有文献 > Pharmacological characterization of novel adenosine ligands in recombinant and native human A2B receptors.

Pharmacological characterization of novel adenosine ligands in recombinant and native human A2B receptors.

Abstract：

:The present study was designed to evaluate the effects of novel and recognised compounds at human recombinant A(2B) adenosine receptors expressed in Chinese hamster ovary (hA(2B)CHO), in human embryonic kidney 293 (hA(2B)HEK-293) and at endogenous A(2B) receptors in human mast cells (HMC-1). Saturation binding experiments performed using the new high affinity A(2B) adenosine radioligand [(3)H]-N-benzo[1,3]dioxol-5-yl-2-[5-(2,6-dioxo-1,3-dipropyl-2,3,6,7-tetra hydro-1H-purin-8-yl)-1-methyl-1H-pyrazol-3-yloxy]-acetamide ([(3)H]-MRE 2029F20) revealed a single class of binding sites in hA(2B)CHO, hA(2B)HEK-293 and HMC-1 cells with K(D) (nM) of 1.65+/-0.18, 2.83+/-0.34, 2.62+/-0.27 and B(max) (fmol/mg protein) of 36+/-4, 475+/-50 and 128+/-15, respectively. The pharmacological profile of new compounds, determined in inhibition binding experiments in hA(2B)HEK-293 cells using [(3)H]-MRE 2029F20, showed a rank order of potency typical of the A(2B) receptors with K(i) values in the range 3.2-28nM. In functional assays, recognised agonists and antagonists were studied by evaluating their capability to modulate the cAMP production in hA(2B)CHO and in HMC-1 cells. Novel compounds were able to decrease NECA-stimulated cAMP production in hA(2B)CHO and in HMC-1 cells showing a high potency. New compounds were also able to inhibit cAMP levels in the absence of NECA and in the presence of forskolin stimulation in hA(2B)CHO and in HMC-1 cells. In HEK-293 cells MRE 2029F20 reduced cAMP basal levels with an IC(50) value of 2.9+/-0.3nM. These results suggest that novel compounds are antagonists with an inverse agonist activity in recombinant and native human A(2B) receptors.

journal_name

Biochem Pharmacol

journal_title

Biochemical pharmacology

authors

Varani K,Gessi S,Merighi S,Vincenzi F,Cattabriga E,Benini A,Klotz KN,Baraldi PG,Tabrizi MA,Lennan SM,Leung E,Borea PA

doi

10.1016/j.bcp.2005.08.018

subject

Has Abstract

pub_date

2005-11-25 00:00:00

pages

1601-12

issue

11

eissn

0006-2952

issn

1873-2968

pii

S0006-2952(05)00567-8

journal_volume

70

pub_type

杂志文章

相关文献

BIOCHEMICAL PHARMACOLOGY文献大全
  • Metabolism and RNA incorporation of cyclopentenyl cytosine in human colorectal cancer cells.

    abstract：:We studied the cytotoxicity and metabolism of the investigational cytidine analogue cyclopentenyl cytosine (CPE-C) in three human colorectal cancer cell lines: HCT 116, SNU-C4, and NCI-H630. CPE-C potently inhibited cell growth and decreased clonogenic capacity at concentrations achieved in murine and primate pharmaco...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(92)90218-8

    authors： Yee LK,Allegra CJ,Trepel JB,Grem JL

    更新日期：1992-04-01 00:00:00

  • Inhibition of topoisomerase II by 8-chloro-adenosine triphosphate induces DNA double-stranded breaks in 8-chloro-adenosine-exposed human myelocytic leukemia K562 cells.

    abstract：:8-Chloro-cAMP and 8-chloro-adenosine (8-Cl-Ado) are known to inhibit proliferation of cancer cells by converting 8-Cl-Ado into an ATP analog, 8-chloro-ATP (8-Cl-ATP). Because type II topoisomerases (Topo II) are ATP-dependent, we infer that 8-Cl-Ado exposure might interfere with Topo II activities and DNA metabolism i...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2008.10.022

    authors： Yang SY,Jia XZ,Feng LY,Li SY,An GS,Ni JH,Jia HT

    更新日期：2009-02-01 00:00:00

  • On the specificity of verapamil as a calcium channel-blocker.

    abstract：:The stimulated uptake of 45Ca2+ into incubated cerebrocortical synaptosomes caused by veratrine (75 microM) was blocked by low concentrations of verapamil (0.5-30 microM) which did not prevent or reduce depolarization as judged by efflux of potassium (K+). However, verapamil did not prevent amino acid neutrotransmitte...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(85)90314-4

    authors： Norris DK,Bradford HF

    更新日期：1985-06-01 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

  • N-butyldeoxygalactonojirimycin: a more selective inhibitor of glycosphingolipid biosynthesis than N-butyldeoxynojirimycin, in vitro and in vivo.

    abstract：:N-Butyldeoxynojirimycin (NB-DNJ) inhibits the ceramide glucosyltransferase which catalyses the first step in glycosphingolipid (GSL) biosynthesis. It has the potential to be used for the treatment of the GSL lysosomal storage diseases and is currently in clinical trials for the treatment of type 1 Gaucher's disease. H...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(99)00384-6

    authors： Andersson U,Butters TD,Dwek RA,Platt FM

    更新日期：2000-04-01 00:00:00

  • Immunocytochemical localization of cytochrome P-450 in hepatic and extra-hepatic tissues of the rat with a monoclonal antibody against cytochrome P-450 c.

    abstract：:The cellular distribution of cytochrome P-450 has been studied in the liver and a number of extrahepatic tissues in the rat by immunocytochemistry, using an antibody raised against cytochrome P-450 form c. Immunoreactive cytochrome P-450, most probably form c, was found in the proximal tubules of the kidney, in the Cl...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(86)90777-x

    authors： Foster JR,Elcombe CR,Boobis AR,Davies DS,Sesardic D,McQuade J,Robson RT,Hayward C,Lock EA

    更新日期：1986-12-15 00:00:00

  • Binding of colchiceine to tubulin. Mechanisms of ligand association with tubulin.

    abstract：:Colchiceine, a closely related structural analog of colchicine possessing a C-ring tropolone, has been shown to be a potent inhibitor of microtubule assembly in vitro (I50 = 20 microM). The mechanism of inhibition is mediated through binding to tubulin (KA = 1.2 +/- 0.7 x 10(4) M-1), although potentially not through t...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(90)90002-3

    authors： Hastie SB,Macdonald TL

    更新日期：1990-04-15 00:00:00

  • New tanshinone I derivatives S222 and S439 similarly inhibit topoisomerase I/II but reveal different p53-dependency in inducing G2/M arrest and apoptosis.

    abstract：:Tanshinone I (Tanshinone-1), a major active principle of the traditional Chinese medicine Salvia miltiorrhiza, possesses excellent anticancer properties, including inhibiting proliferation, angiogenesis and metastasis and overcoming multidrug resistance (MDR). However, its direct anticancer molecular target(s) remain ...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2018.05.006

    authors： Tian QT,Ding CY,Song SS,Wang YQ,Zhang A,Miao ZH

    更新日期：2018-08-01 00:00:00

  • Butyrylcholinesterase, a stereospecific in vivo bioscavenger against nerve agent intoxication.

    abstract：:Human butyrylcholinesterase (E.C. 3.1.1.8) purified from blood plasma has previously been shown to provide protection against up to five and a half times the median lethal dose of an organophosphorus nerve agent in several animal models. In this study the stoichiometric nature of the protection afforded by human butyr...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2019.113670

    authors： Cerasoli DM,Armstrong SJ,Reeves TE,Hodgins SM,Kasten SA,Lee-Stubbs RB,Cadieux CL,Otto TC,Capacio BR,Lenz DE

    更新日期：2020-01-01 00:00:00

  • A novel approach for stress-induced gastritis based on paradoxical anti-oxidative and anti-inflammatory action of exogenous 8-hydroxydeoxyguanosine.

    abstract：:Reactive oxygen species (ROS) attack guanine bases in DNA and form 8-hydroxydeoxyguanosine (8-OHdG), which has been regarded simply as an oxidative mutagenic by-product. On the other hand, our previous report showed paradoxically ROS attenuating action of generated 8-OHdG. In the current study, both in vitro and in vi...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2010.08.023

    authors： Ock CY,Hong KS,Choi KS,Chung MH,Kim Ys,Kim JH,Hahm KB

    更新日期：2011-01-01 00:00:00

  • Jingzhaotoxin-II, a novel tarantula toxin preferentially targets rat cardiac sodium channel.

    abstract：:Naturally occurring toxins are invaluable tools for exploration of the structure and function relationships of voltage-gated sodium channels (VGSCs). In this study, we isolated and characterized a novel VGSC toxin named jingzhaotoxin-II (JZTX-II) from the tarantula Chilobrachys jingzhao venom. JZTX-II consists of 32 a...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2008.09.008

    authors： Wang M,Liu Q,Luo H,Li J,Tang J,Xiao Y,Liang S

    更新日期：2008-12-15 00:00:00

  • Cross-talk between minimally primed HL-60 cells and resting HUVEC reveals a crucial role for adhesion over extracellularly released oxidants.

    abstract：:This study demonstrates that a long-lasting co-culture of neutrophil surrogates (HL-60 cells), minimally primed by platelet activating factor (PAF), and resting endothelial cells (EC) results in the elaboration of an hyper-adhesive endothelial surface, as measured by the increase in the expression of endothelial adhes...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2010.10.018

    authors： Allegra M,D'Acquisto F,Tesoriere L,Livrea MA,Perretti M

    更新日期：2011-02-01 00:00:00

  • Tobacco and alcohol use during adolescence: Interactive mechanisms in animal models.

    abstract：:There is a strong association between tobacco smoking and the consumption of alcoholic beverages. When compared to the effects of either drug on its own, the combined use may lead to worsened outcomes, such as less successful quitting attempts and increased likelihood of developing mood disorders. Co-consumption most ...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章,评审

    doi：10.1016/j.bcp.2017.06.113

    authors： Abreu-Villaça Y,Manhães AC,Krahe TE,Filgueiras CC,Ribeiro-Carvalho A

    更新日期：2017-11-15 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

  • Differentiation of human hepatoma cells during confluence as revealed by gene expression profiling.

    abstract：:Certain human hepatocarcinoma cells undergo differentiation when grown at confluence. In order to understand the basis for this differentiation, we investigated the phenotypic changes occurring during confluent growth of the human hepatoma B16A2 cell line. The global gene expression profile of B16A2 cells grown during...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2003.10.033

    authors： Butura A,Johansson I,Nilsson K,Wärngård L,Ingelman-Sundberg M,Schuppe-Koistinen I

    更新日期：2004-04-01 00:00:00

  • Oxidative stress and nuclear factor-kappaB activation: a reassessment of the evidence in the light of recent discoveries.

    abstract：:Nuclear factor-kappaB (NFKB) is a transcription factor with a pivotal role in inducing genes involved in physiological processes as well as in the response to injury and infection. A model has been proposed whereby the diverse agents that activate NFkappaB do so by increasing oxidative stress within the cell. Activati...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章,评审

    doi：10.1016/s0006-2952(99)00296-8

    authors： Bowie A,O'Neill LA

    更新日期：2000-01-01 00:00:00

  • Effect of fluoxetine on rat liver mitochondria.

    abstract：:The in vitro and in vivo effects of fluoxetine (and its active metabolite norfluoxetine) on mitochondrial respiration and F0F1-ATPase were studied, respectively, in mitochondria and submitochondrial particles isolated from rat liver. Fluoxetine in vitro inhibited state 3 mitochondrial respiration for alpha-ketoglutara...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(94)90283-6

    authors： Souza ME,Polizello AC,Uyemura SA,Castro-Silva O,Curti C

    更新日期：1994-08-03 00:00:00

  • Reduced hepatic expression of CYP7A1 and CYP2C13 in rats with spontaneous hyperlipidaemia.

    abstract：:A strain of hyperlipidaemic Sprague-Dawley (HSD) rat was compared with normal Sprague-Dawley (SD) rats for expression of cholesterol 7alpha-hydroxylase activity (CYP7A1) and other cytochrome P450 (P450) enzymes in liver. Hepatic microsomal CYP7A1 activity in male HSD rats was 2-3-fold lower than in male SD rats with C...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(98)00015-x

    authors： Brassil PJ,Debri K,Nakura H,Kobayashi S,Davies DS,Edwards RJ

    更新日期：1998-07-15 00:00:00

  • Regulatory roles of adenylate cyclase and cyclic nucleotide phosphodiesterases 1 and 4 in interleukin-13 production by activated human T cells.

    abstract：:We studied the activities of 3',5'-adenosine-cyclic monophosphate (cAMP)- synthesizing adenylate cyclase (AC) and cAMP-hydrolyzing cyclic nucleotide phosphodiesterase (PDE) in phytohemagglutinin (PHA)- or anti-CD3 plus anti-CD28-stimulated human T cells, and examined their roles in interleukin-13 (IL-13) production. T...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(01)00688-8

    authors： Kanda N,Watanabe S

    更新日期：2001-08-15 00:00:00

  • Depletion of cardiac norepinephrine in rats and mice by 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP).

    abstract：:1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) is a commercially available chemical reagent. Although little has been known about its biological effects, recently MPTP has been reported to cause irreversible Parkinson's disease-like symptoms in humans and in monkeys. We describe here another pharmacologic effect ...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(84)90593-8

    authors： Fuller RW,Hahn RA,Snoddy HD,Wikel JH

    更新日期：1984-10-01 00:00:00

  • The multikinase inhibitor axitinib is a potent inhibitor of human CYP1A2.

    abstract：:The tyrosine kinase inhibitors (TKIs) and multikinase inhibitors (MKIs) are oncology drugs of increasing importance that have improved the treatment of multiple tumors types. In some patients these agents produce adverse effects, including pharmacokinetic drug-drug interactions, due to cytochrome P450 (CYP) inhibition...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2014.01.016

    authors： Gu R,Hibbs DE,Ong JA,Edwards RJ,Murray M

    更新日期：2014-03-15 00:00:00

  • Denitrosation of 1,3-dimethyl-2-cyano-1-nitrosoguanidine in rat primary hepatocyte cultures.

    abstract：:N-Nitrosoguanidines are potential carcinogens. However, the toxicity of these agents is attenuated significantly in laboratory rodents by processes that remove the nitroso group to generate the relatively innocuous parent guanidinium compound. The denitrosation of 1,3-dimethyl-2-cyano-1-nitrosoguanidine (CyanoDMNG) me...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(96)00861-1

    authors： Jensen DE,Belka GK,Dworkin C

    更新日期：1997-05-09 00:00:00

  • Modelling and molecular dynamics of the interaction between the E3 ubiquitin ligase Itch and the E2 UbcH7.

    abstract：:Itch, a member of the E6AP carboxy terminus (HECT) domain-containing family of ubiquitin E3 ligases, acts in concert with the ubiquitin activating enzyme (E1) and the ubiquitin conjugating enzyme (E2) to catalyze ubiquitylation of protein targets. This sub-family of E3s shares a 350 residue C-terminal HECT domain havi...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2008.08.026

    authors： Raimondo D,Giorgetti A,Bernassola F,Melino G,Tramontano A

    更新日期：2008-12-01 00:00:00

  • Selective inhibition of cyclic AMP and cyclic GMP phosphodiesterases of cardiac nuclear fraction.

    abstract：:Approximately 60% of the total particulate phosphodiesterase activity occurring in cardiac tissue was associated with the nuclear fraction. Cyclic GMP phosphodiesterase activity of the purified cardiac nuclear fraction was selectively inhibited by trifluoperazine (I50 = 19 microM) with negligible inhibition (less than...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(82)90447-6

    authors： Ahluwalia GS,Rhoads AR

    更新日期：1982-03-01 00:00:00

  • Synergistic effects of neurotensin and beta-adrenergic agonist on 3,5-cyclic adenosine monophosphate accumulation and DNA synthesis in prostate cancer PC3 cells.

    abstract：:Since neurotensin is often co-stored with catecholamines and since it can excite the release of dopamine and norepinephrine, responses to this peptide might depend upon the activity of catecholaminergic systems. In this study, we used prostate cancer PC3 cells, which express neurotensin receptors and 12-adrenergic rec...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(99)00064-7

    authors： Mitra SP,Carraway RE

    更新日期：1999-06-15 00:00:00

  • Inhibition of microsomal biotransformation by a series of nitrogen and oxygen heterocyclic histamine H2-antagonists.

    abstract：:A homologous series of potent, long-lasting thiazolo-pyrimidone-pyridine histamine H2-antagonists were examined for their inhibitory effects on rat hepatic ethylmorphine N-demethylation. Inhibitory potency increased in the order: 2-pyridinyl less than 3-pyridinyl less than 4-pyridinyl histamine H2-antagonist. Substitu...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(87)90052-9

    authors： Lindstrom TD,Whitaker GW,Pioch RP

    更新日期：1987-05-15 00:00:00

  • Redox modulation of the DNA damage response.

    abstract：:Lesions to DNA trigger the DNA-damage response (DDR), a complex, multi-branched cell-intrinsic process targeted to DNA repair, or elimination of the damaged cells by apoptosis. DDR aims at reducing permanence of mutated cells, decreasing the risk of tumor development: the more stringent the response, the lower the lik...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章,评审

    doi：10.1016/j.bcp.2012.07.022

    authors： Caputo F,Vegliante R,Ghibelli L

    更新日期：2012-11-15 00:00:00

  • Regulation of expression and function of m2 and m4 muscarinic receptors in cultured embryonic chick heart cells by transforming growth factor-beta 1.

    abstract：:Incubation of cultured embryonic chicken heart cells with transforming growth factor beta 1 (TGF-beta 1) resulted in a concentration- and time-dependent decrease in the number of muscarinic acetylcholine receptors (mAChR), which reached a maximum by 24 hr. Twenty-four hours following TGF-beta 1 treatment, cm2 and cm4 ...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(97)00219-0

    authors： Jackson DA,Nathanson NM

    更新日期：1997-08-15 00:00:00

  • Studies on the action of nystatin on cultured rat myocardial cells and cell membranes, isolated rat hearts, and intact rats.

    abstract：:The action of nystatin, a polyene antibiotic, was studied in rat myocardial cells, isolated rat hearts, and intact rats. Myocardial cells responded to 10 and 25 micrograms nystatin/ml with arrhythmias that could be minimized by elevated concentrations of K+ and Mg2+ or reversed by washing the cells. Similarly, the iso...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(84)90040-6

    authors： Aszalos A,Bradlaw JA,Reynaldo EF,Yang GC,El-Hage AN

    更新日期：1984-12-01 00:00:00

  • Evidence for distinct regulation processes in the aclacinomycin- and doxorubicin-mediated differentiation of human erythroleukemic cells.

    abstract：:Human erythroleukemic K 562 cells were induced to were induced to differentiate along the erythroid lineage by anthracycline antitumor drugs, such as aclacinomycin (ACLA) and doxorubicin (DOX). Subsequent stimulation of heme and globin synthesis led to a differential quantitative expression of hemoglobins. Gower 1 (ep...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(95)02240-6

    authors： Morceau F,Aries A,Lahlil R,Devy L,Jardillier JC,Jeannesson P,Trentesaux C

    更新日期：1996-03-22 00:00:00