Inhibition of the release of prostaglandins, leukotrienes and lysosomal acid hydrolases from macrophages by selective inhibitors of lecithin biosynthesis.

abstract：:Adherence of Plasmodium falciparum-infected erythrocytes (IE) to the venular endothelium in brain and other organs is characteristic of cerebral malaria, an often fatal complication in infected individuals. It has been shown that cytoadherence may be mediated through interaction of IE with glycoproteins on host target...

journal_title：Biochemical pharmacology

authors： Wright PS,Cross-Doersen DE,Schroeder KK,Bowlin TL,McCann PP,Bitonti AJ

更新日期：1991-06-15 00:00:00

abstract：:In assessing the biological effects of exposure to a complex chemical mixture, it is important to determine how the behavior of one compound may be influenced by the presence of other compounds in the mixture. In this study the effect of pre-exposure to an organic extract of diesel exhaust or to selected compounds in ...

journal_title：Biochemical pharmacology

authors： Howard AJ,Mitchell CE,Dutcher JS,Henderson TR,McClellan RO

更新日期：1986-07-01 00:00:00

abstract：:Disodium cromoglycate and compounds which elevated levels of cyclic AMP in the mast cell variously inhibited cytotoxic histamine release induced by the surface active agents melittin, Tween 20 and Triton X-100. These results are inconsistent with the postulated effects of the drugs on receptor mediated calcium channel...

journal_title：Biochemical pharmacology

authors： Pearce FL,Clements J

更新日期：1982-07-01 00:00:00

abstract：:Guanidines, amidines, S-alkylisothioureas, and other compounds containing the amidine function (-C(=NH)NH2) have been described as inhibitors of the generation of nitric oxide (NO) by NO synthase (NOS). Here we report on the inhibition of the activity of NOS isoforms by compounds in which the amidine function is attac...

journal_title：Biochemical pharmacology

authors： Southan GJ,Gauld D,Lubeskie A,Zingarelli B,Cuzzocrea S,Salzman AL,Szabó C,Wolff DJ

更新日期：1997-08-01 00:00:00

abstract：:The addition of agents, such as tumor necrosis factor-alpha, to human peripheral neutrophils (HPPMN) induces priming, which enhances the receptor-mediated superoxide (O2-) generation and tyrosine phosphorylation of several HPPMN proteins. Lidocaine, a local anesthetic, inhibited both enhanced O2- generation and tyrosi...

journal_title：Biochemical pharmacology

authors： Kanbara T,Tomoda MK,Sato EF,Ueda W,Manabe M

更新日期：1993-04-22 00:00:00

abstract：:The binding affinity of ethanol for carbohydrates is unknown. Glycoconjugates are postulated to be sensitive targets of ethanol action. The glycogen content of muscle, liver, and brain is sensitive to ethanol. To explore whether carbohydrates as a class have a specific affinity to bind ethanol, we measured the binding...

journal_title：Biochemical pharmacology

authors： Channareddy S,Jose SS,Janes N

更新日期：1996-12-24 00:00:00

abstract：:Isolated liver from phenobarbital-induced male mice was perfused using infusions of cytochrome c pulses as quality control of the system. Livers spontaneously evolved 1.1 pmoles ethane g-1 liver min-1, exogenous pentane disappeared with 0.6 pmoles g-1 min-1. Infusion of 0.26 mmoles/l. FeCl2 led to immediate ethane pro...

journal_title：Biochemical pharmacology

authors： Thelen M,Wendel A

更新日期：1983-06-01 00:00:00

abstract：:In a previous study we reported that triethyllead (Et3Pb+) inhibits cell proliferation of normal human lymphocytes. To further characterize this interaction, we studied herein the effects of Et3Pb+ on the cell viability of normal and leukemic human lymphocytes and analysed the expression and dynamics of the monomer/po...

journal_title：Biochemical pharmacology

authors： Stiakaki E,Stournaras C,Dimitriou H,Kalmanti M

更新日期：1997-12-15 00:00:00

abstract：:The disturbances of the cholesterol synthesis and metabolism described in Alzheimer's disease (AD) may be both a consequence of the neurodegenerative process and a contributor to the pathogenesis. These putative relationships and their underlying mechanisms are not well understood. The aim of this study was to evaluat...

journal_title：Biochemical pharmacology

authors： Popp J,Meichsner S,Kölsch H,Lewczuk P,Maier W,Kornhuber J,Jessen F,Lütjohann D

更新日期：2013-07-01 00:00:00

abstract：:Dichlorodi[U-14C]phenyltrichloroethane ( [14C]DDT), incubated with rat hepatic microsomes and NADPH, produced reactive intermediates which covalently bound to microsomal protein and lipids. In atmospheric oxygen, DDT bound to microsomal protein; however, binding was increased up to approximately 70% by oxygen depletio...

journal_title：Biochemical pharmacology

authors： Baker MT,Van Dyke RA

更新日期：1984-01-15 00:00:00

abstract：:SR 4233 or WIN 59075 (3-amino-1,2,4-benzotriazine-1,4-dioxide) is a novel and highly selective hypoxic cell cytotoxin requiring reductive bioactivation for its impressive antitumour effects. Expression of appropriate reductases will contribute to therapeutic selectivity. Here we provide more detailed information on th...

journal_title：Biochemical pharmacology

authors： Walton MI,Wolf CR,Workman P

更新日期：1992-07-22 00:00:00

abstract：:PI3K cascade is a central signaling pathway regulating cell proliferation, growth, differentiation, and survival. Tight regulation of the PI3K signaling pathway is necessary to avoid aberrant cell proliferation and cancer development. Together with SHIP-1, the inositol phosphatases PTEN and SHIP-2 are the gatekeepers ...

journal_title：Biochemical pharmacology

authors： Condé C,Gloire G,Piette J

更新日期：2011-11-15 00:00:00

abstract：:In order to understand the relationship between the free ionized calcium concentration in the axon terminals and the transmitter release we have investigated the effect of ruthenium red (RuR) and m-chloro-carbonylcyanide phenyl hydrazon (CCCP), mitochondrial uncoupler agents on the liberation of acetylcholine from mye...

journal_title：Biochemical pharmacology

authors： Bernath S,Vizi ES

更新日期：1987-11-01 00:00:00

abstract：:In vitro treatment of human T-cell leukemia cells with 7-hydroxymethotrexate, the major metabolite of methotrexate resulted in acquired resistance as a result of the complete loss of folypolyglutamate synthetase (FPGS) activity. This was in contradistinction to the major modality of antifolate resistance of impaired d...

journal_title：Biochemical pharmacology

authors： Fotoohi AK,Assaraf YG,Moshfegh A,Hashemi J,Jansen G,Peters GJ,Larsson C,Albertioni F

更新日期：2009-04-15 00:00:00

abstract：:trans-Resveratrol is a dietary polyphenolic compound present in grapes, which has been shown to exhibit strong anti-inflammatory, antioxidant, and chemopreventive activities. In this study we have compared the in vitro and in vivo effects of resveratrol on the development of various cell-mediated immune responses, inc...

journal_title：Biochemical pharmacology

authors： Gao X,Deeb D,Media J,Divine G,Jiang H,Chapman RA,Gautam SC

更新日期：2003-12-15 00:00:00

abstract：:The hypolipidemic drug ethyl chlorophenoxyisobutyrate (clofibrate) is known to induce peroxisome proliferation and to be carcinogenic after long term administration to rats and mice. We examined the effects of treatment with this drug for periods of up to 18 months on cytosolic ATP-stimulated and ADP-inhibited acetyl-...

journal_title：Biochemical pharmacology

authors： Nakanishi Y,Okamoto K,Isohashi F

更新日期：1993-04-06 00:00:00

abstract：:We have studied the effects of thimerosal, a mercurial compound extensively used as a preservative, as well as other sulfhydryl reagents (e.g. p-hydroxymercurybenzoate, hydrogen peroxide, bromophenacyl bromide, and mercuric chloride) on Ca2+ homeostasis and the redox status of sulfhydryl groups in thymus lymphocytes. ...

journal_title：Biochemical pharmacology

authors： Pintado E,Baquero-Leonis D,Conde M,Sobrino F

更新日期：1995-01-18 00:00:00

abstract：:The inhibitory effects of anion channel blockers were evaluated on aggregation, intracellular Ca2+ rises, and the production of arachidonic acid metabolites in human platelets. Inhibitors included five anion channel blockers: phloretin, probenecid, pyridoxal phosphate, 4,4'-diisothiocyano-2,2'-disulfonic acid stilbene...

journal_title：Biochemical pharmacology

authors： Ozaki Y,Matsumoto Y,Yatomi Y,Higashihara M,Kariya T,Shoji K

更新日期：1989-07-01 00:00:00

abstract：:OSI-7836 (4'-thio-araC, T-araC) is a nucleoside analogue that shows efficacy against solid tumor xenograft models. We examined how the triphosphates of OSI-7836 (T-araCTP), cytarabine (araCTP), and gemcitabine (dFdCTP) affected the initiation of new DNA strands by the pol alpha primase complex. Whereas dFdCTP very wea...

journal_title：Biochemical pharmacology

authors： Richardson KA,Vega TP,Richardson FC,Moore CL,Rohloff JC,Tomkinson B,Bendele RA,Kuchta RD

更新日期：2004-12-15 00:00:00

abstract：:The capacity of G protein-coupled receptors to modulate mechanistic target of rapamycin (mTOR) activity is a newly emerging paradigm with the potential to link cell surface receptors with cell survival. Cardiomyocyte viability is linked to signalling pathways involving Akt and mTOR, as well as increased glucose uptake...

journal_title：Biochemical pharmacology

authors： Sato M,Evans BA,Sandström AL,Chia LY,Mukaida S,Thai BS,Nguyen A,Lim L,Tan CYR,Baltos JA,White PJ,May LT,Hutchinson DS,Summers RJ,Bengtsson T

更新日期：2018-02-01 00:00:00

abstract：:[3H]Morphine, PL-017[prolyl-3,4-3H,D-prolyl,3,4-3H] ([3H]PL-017) and enkephalin-(2-D-penicillamine,5-D-penicillamine)[tyrosyl-2,6-3H] ([3H]DPDPE) were directly cross-linked to mouse brain opiate receptors by an ultraviolet (254 nm) irradiation procedure. [3H]Morphine preferentially and specifically labeled a 58 kDa pr...

journal_title：Biochemical pharmacology

authors： Nagamatsu K,Tagawa Y,Uchida S,Hasegawa A

更新日期：1993-10-05 00:00:00

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

authors： Chong LK,Tattersall MH

更新日期：1995-03-15 00:00:00

abstract：:The kinetics of methotrexate inhibition of dihydrofolate reductase from Neisseria gonorrhoeae have been investigated. Methotrexate was shown to be a tight-binding inhibitor (Kt = 13 pM) competitive with dihydrofolate. However, "stoichiometric" or "pseudoirreversible" inhibition could not be demonstrated. Progress curv...

journal_title：Biochemical pharmacology

authors： Baccanari DP,Tansik RL

更新日期：1984-07-01 00:00:00

abstract：:Previous work has shown that 5-hydroxytryptamine (5-HT)2A receptors can be radiolabelled with various radioligands, including partial agonists, such as [125I]-DOI and [3H]-DOB, and antagonists, such as [3H]-ketanserin and [3H]-spiperone. Because 5-HT has high affinity for the 5-HT2A receptor when displacing [3H]-DOB, ...

journal_title：Biochemical pharmacology

authors： Sleight AJ,Stam NJ,Mutel V,Vanderheyden PM

更新日期：1996-01-12 00:00:00

abstract：:Microsomal and cytosolic epoxide hydrolase (mEH and cEH respectively) and glutathione S-transferase (GST) activities were measured in the liver, kidney, and gills of rainbow trout. Assays were optimized for time, pH, and temperature, using trans-stilbene oxide (TSO) and cis-stilbene oxide (CSO) as substrates for cEH a...

journal_title：Biochemical pharmacology

authors： Laurén DJ,Halarnkar PP,Hammcock BD,Hinton DE

更新日期：1989-03-15 00:00:00

abstract：:Aequorin-based assays for stable fly, Stomoxys calcitrans, (STKR) and human (neurokinin receptor 1 (NK1), neurokinin receptor 2 (NK2)) neurokinin-like receptors were employed to investigate the impact of a C-terminal amino acid exchange in synthetic vertebrate ('FXGLMa') and invertebrate ('FX1GX2Ra') tachykinin-like p...

journal_title：Biochemical pharmacology

authors： Torfs H,Detheux M,Oonk HB,Akerman KE,Poels J,Van Loy T,De Loof A,Vassart G,Parmentier M,Vanden Broeck J

更新日期：2002-05-01 00:00:00

abstract：:The mechanism for formation of high-affinity binding of 1-(2,6-dichlorobenzylidene-amino)-3-hydroxyguanidine (guanoxabenz) to alpha2-adrenoceptors was studied in particulate fractions from the rat spleen. The proportion of apparent high versus low-affinity alpha2-adrenoceptor binding sites increased with increasing in...

journal_title：Biochemical pharmacology

authors： Uhlén S,Dambrova M,Tiger G,Oliver DW,Wikberg JE

更新日期：1998-11-01 00:00:00

abstract：:Although there are a number of well-characterised animal models available for testing and comparing the efficacy of iron chelators, most are expensive to operate and are not capable of providing rapid and reproducible results. The method described herein is based on the labelling of rat liver with 59Fe using rat 59Fe-...

journal_title：Biochemical pharmacology

authors： Liu ZD,Lu SL,Hider RC

更新日期：1999-03-01 00:00:00

abstract：:When HL-60 cells were stimulated with histamine, a significant differentiation of the cells toward neutrophils was elicited. Histamine increased phagocytic activity, but it reduced myeloperoxidase activity of HL-60 cells. Histamine-induced differentiation in HL-60 cells was inhibited not only by H2 antagonists, such a...

journal_title：Biochemical pharmacology

authors： Nonaka T,Mio M,Doi M,Tasaka K

更新日期：1992-09-25 00:00:00

abstract：:Accumulation of radioactive iron (59Fe) into isolated fragments of rat small intestine in the presence of two hydroxypyrones, maltol and ethyl maltol, was compared with that in the presence of another chelator of iron(III), nitrilotriacetic acid (NTA). The characteristics of uptake were similar with all three ligands....

journal_title：Biochemical pharmacology

authors： Levey JA,Barrand MA,Callingham BA,Hider RC

更新日期：1988-05-15 00:00:00