Lidocaine inhibits priming and protein tyrosine phosphorylation of human peripheral neutrophils.

abstract：:The stereoselective sulfoxidation of the pharmacologically active metabolite of sulindac, sulindac sulfide, was characterized in human liver, kidney, and cDNA-expressed enzymes. Kinetic parameter estimates (pH = 7.4) for sulindac sulfoxide formation in human liver microsomes (N = 4) for R- and S-sulindac sulfoxide wer...

journal_title：Biochemical pharmacology

authors： Hamman MA,Haehner-Daniels BD,Wrighton SA,Rettie AE,Hall SD

更新日期：2000-07-01 00:00:00

abstract：:Previous studies of platinum(II) compounds with bidentate leaving ligands have emphasized the contrast between the stability of the bidentate leaving ligand in vitro (T1/2 greater than 11 days in water) and the apparent reactivity of these bidentate platinum compounds in vivo. However, none of these studies actually m...

journal_title：Biochemical pharmacology

authors： Mauldin SK,Plescia M,Richard FA,Wyrick SD,Voyksner RD,Chaney SG

更新日期：1988-09-01 00:00:00

abstract：:Glutamatergic hypofunction and elevated levels of kynurenic acid (KYNA) in the brain are common features of patients with schizophrenia. In vivo studies indicate that in the hippocampus KYNA decreases glutamate levels, presumably via inhibition of α7 nicotinic receptors (nAChRs). Here we tested the hypothesis that bas...

journal_title：Biochemical pharmacology

authors： Banerjee J,Alkondon M,Albuquerque EX

更新日期：2012-10-15 00:00:00

abstract：:Cobalt protoporphyrin generated from 5-amino[4-14C]laevulinate by homogenates or primary cultures of chick embryo liver exposed to CoCl2 was found to be radioactivity unextractable by acid/acetone, when extra protein was added. The activity of ferrochelatase was required for formation of cobalt protoporphyrin since in...

journal_title：Biochemical pharmacology

authors： Sinclair PR,Sinclair JF,Bonkowsky HL,Gibbs AH,De Matteis F

更新日期：1982-03-15 00:00:00

abstract：:A newly synthesized compound, 2-[N-(2-aminoethyl)-N-(5-isoquinolinesulfonyl)]amino-N-(4-chlorocinnamyl )-N-methylbenzylamine (CKA-1306), was found to inhibit cyclic AMP-dependent protein kinase (PKA) and Ca2+/calmodulin-dependent protein kinase I (CaMK I) with IC50 values of 1.6+/-0.14 and 2.5+/-0.16 microM, respectiv...

journal_title：Biochemical pharmacology

authors： Sakaguchi H,Yokokura H,Terada O,Naito Y,Nimura Y,Hidaka H

更新日期：1998-08-01 00:00:00

abstract：:Common marmosets (Callithrix jacchus) are potentially useful nonhuman primate models for preclinical studies. An anti-inflammatory drug, diclofenac is reportedly metabolized mainly by human cytochrome P450 (P450) 2C9 to 4'-hydroxydiclofenac and minorly by P450 3A4 to 5-hydroxydiclofenac that leads to reactive intermed...

journal_title：Biochemical pharmacology

authors： Nakanishi K,Uehara S,Kusama T,Inoue T,Shimura K,Kamiya Y,Murayama N,Shimizu M,Uno Y,Sasaki E,Yamazaki H

更新日期：2018-06-01 00:00:00

abstract：:The ex vivo sensitivity of murine pluripotent hematopoietic stem cells (CFU-S) and myeloid progenitor cells (CFU-GM) to 4-hydroperoxycyclophosphamide, ASTA Z 7557, phosphoramide mustard, acrolein, melphalan, and cis-platinum was determined in the absence and presence of known (disulfiram, diethyldithiocarbamate, cyana...

journal_title：Biochemical pharmacology

authors： Kohn FR,Sladek NE

更新日期：1985-10-01 00:00:00

abstract：:Incubation of human carcinoma cells with mitoxantrone resulted in an intracellular distribution of the drug into cytoplasmic, nuclear and cytoskeletal compartments occurring within 1 min of drug treatment. Incubation of the cells in drug-free medium resulted in an efflux of the drug such that 80% of the intracellular ...

journal_title：Biochemical pharmacology

authors： Roberts RA,Cress AE,Dalton WS

更新日期：1989-12-01 00:00:00

abstract：:Polychlorinated biphenyls (PCBs) induce drug metabolism that may lead to the bioactivation of PCBs themselves or alternatively may lead to oxidative events within the cell. The goal of the present study was to determine the influence of congeneric PCBs, selected as substrates for or inducers of drug metabolism, upon h...

journal_title：Biochemical pharmacology

authors： Twaroski TP,O'Brien ML,Robertson LW

更新日期：2001-08-01 00:00:00

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

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

更新日期：1990-01-15 00:00:00

abstract：:Tenofovir alafenamide (TAF) can be considered a new prodrug of tenofovir (TFV), as successor of tenofovir disoproxil fumarate (TDF). It is in vivo as potent against human immunodeficiency virus (HIV) at a 30-fold lower dose (10mg) than TDF (300mg). TAF has been approved in November 2015 (in the US and EU), as a single...

journal_title：Biochemical pharmacology

authors： De Clercq E

更新日期：2016-11-01 00:00:00

abstract：:ICRF-193 [meso-2,3-bis(3,5-dioxopiperazine-1-yl)butane], a bisdioxopiperazine compound, has been shown to be a catalytic inhibitor of DNA topoisomerase II by stabilizing the enzyme in the form of a closed "protein clamp," an intermediate form in the catalytic cycle (Roca et al., Proc Natl Acad Sci USA 91: 1781-1785, 1...

journal_title：Biochemical pharmacology

authors： Sato M,Ishida R,Narita T,Kato J,Ikeda H,Fukazawa H,Andoh T

更新日期：1997-09-01 00:00:00

abstract：:Angiogenesis, the development of neovessels from pre-existing vessels, is obligatory for solid tumors survival, growth, invasion, and metastasis. Many anti-angiogenic agents are small molecules originated from natural sources. Recently, angiosuppressive effects of indirubin and its derivatives, the active components i...

journal_title：Biochemical pharmacology

authors： Chan YK,Kwok HH,Chan LS,Leung KS,Shi J,Mak NK,Wong RN,Yue PY

更新日期：2012-03-01 00:00:00

abstract：:AM404 is a synthetic TRPV1/CB(1) hybrid ligand with inhibitory activity on the anandamide transporter and is used for the pharmacological manipulation of the endocannabinoid system. It has been recently described that acetaminophen is metabolised in the brain to form the bioactive N-acylphenolamine AM404 and therefore...

journal_title：Biochemical pharmacology

authors： Caballero FJ,Navarrete CM,Hess S,Fiebich BL,Appendino G,Macho A,Muñoz E,Sancho R

更新日期：2007-04-01 00:00:00

abstract：:The mitomycin C (MC) analog BMS-181174 (previously designated as BMY25067) has been shown to be active against a variety of solid tumors in mice. The activity of this compound against tumor cell lines resistant to MC and the different toxicity profiles of BMS-181174 and MC suggested that there may be significant diffe...

journal_title：Biochemical pharmacology

authors： Rockwell S,Kemple B,Kelley M

更新日期：1995-10-12 00:00:00

abstract：:Sodium nitroprusside (SNP) stimulates cGMP formation to a greater extent in 20,000 g supernatant fractions of the human neuroblastoma clones NB1-G and SH-SY5Y than in the human astrocytoma clone D384. This suggests that these cell lines contain the soluble form of guanylate cyclase. Arachidonic, 8,11,14- and 11,14,17-...

journal_title：Biochemical pharmacology

authors： Vaughan PF,Ball SG

更新日期：1990-02-01 00:00:00

abstract：:The inhibition of formyl-methionyl-leucyl-phenylalanine (fMLP)-induced superoxide anion (O2(.-)) generation by 2-benzyloxybenzaldehyde (CCY1a) was investigated in rat neutrophils, and the underlying mechanism of this inhibition was assessed. CCY1a concentration-dependently inhibited O2(.-) generation (IC(50)=18.5+/-4....

journal_title：Biochemical pharmacology

authors： Wang JP,Chang LC,Lin YL,Hsu MF,Chang CY,Huang LJ,Kuo SC

更新日期：2003-04-01 00:00:00

abstract：:Glucose metabolism and hemoglobin reactivity in intact human erythrocytes were assessed in the presence of the tryptophan metabolites, 3-hydroxyanthranilate (3-HAT), quinolinate and picolinate. Of these compounds, only 3-HAT altered red cell oxidative status by inducing, in a dose-dependent manner, formation of methem...

journal_title：Biochemical pharmacology

authors： Dykens JA,Sullivan SG,Stern A

更新日期：1989-05-15 00:00:00

abstract：:During a cellular screening of thiocolchicine analogs, thiocolchicine dimers resulted particularly active in cisplatin-resistant A2780-CIS cells. In order to discover by which mechanism(s) thiocolchicine dimers overcame cisplatin resistance, p53, p21waf1 and MLH1 were assessed by Western blot. Results pointed out that...

journal_title：Biochemical pharmacology

authors： Raspaglio G,Ferlini C,Mozzetti S,Prislei S,Gallo D,Das N,Scambia G

更新日期：2005-01-01 00:00:00

abstract：:A series of nitrogen mustard derivatives was tested for neurotoxic effects on cholinergic and GABAergic markers at three rat brain regions: hippocampus, striatum and cortex. All compounds were administered intracerebroventricularly, and the enzymatic activities were measured 7 days after treatment. The effects of synt...

journal_title：Biochemical pharmacology

authors： Maysinger D,Tagari PC,Cuello C

更新日期：1986-10-15 00:00:00

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

authors： Singh AK

更新日期：1993-03-09 00:00:00

abstract：:Previous studies from this lab and others have demonstrated that nitric oxide (NO) in a concentration dependent manner, modulated neutrophil and leukemic cell survival. Subsequent studies delineated importance of iNOS in neutrophil differentiation and leukemic cell death. On the contrary, role of nNOS in survival of t...

journal_title：Biochemical pharmacology

authors： Sadaf S,Awasthi D,Singh AK,Nagarkoti S,Kumar S,Barthwal MK,Dikshit M

更新日期：2020-06-01 00:00:00

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

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

abstract：:Continuous in vitro cultivation of human lymphoid H9 cells in the presence of 0.5microM arabinosyl-cytosine (araC) resulted in cell variant, H9-araC cells, that was >600-fold resistant to the drug and cross resistant to its analogs and other unrelated nucleosides, e.g. dideoxycytidine (5-fold), thiacytidine (2-fold), ...

journal_title：Biochemical pharmacology

authors： Sarkar M,Han T,Damaraju V,Carpenter P,Cass CE,Agarwal RP

更新日期：2005-08-01 00:00:00

abstract：:Inorganic polyphosphate (polyP) is a physiological polymer composed of tens to hundreds of phosphate units linked together via phosphoanhydride bonds. Here we compared the biological activity of polyP (chain length of 40 phosphate units), complexed with Gd(3+) (polyP·Gd), with the one caused by polyP (as calcium salt)...

journal_title：Biochemical pharmacology

authors： Wang X,Huang J,Wang K,Neufurth M,Schröder HC,Wang S,Müller WEG

更新日期：2016-02-15 00:00:00

abstract：:Dexamethasone and etoposide both induce apoptosis in immature rat thymocytes. We investigated the dependence of apoptosis on the phase of the cell cycle after incubation with these drugs. Cell cycle progression was followed by a combination of pulse labelling with 5-bromo-2'-deoxyuridine (BrdU), labelling fixed cells ...

journal_title：Biochemical pharmacology

authors： Fearnhead HO,Chwalinski M,Snowden RT,Ormerod MG,Cohen GM

更新日期：1994-09-15 00:00:00

abstract：:Reduction of exogenous lipoic acid to dihydrolipoate is known to occur in several mammalian cells and tissues. Dihydrolipoate is a potent radical scavenger, and may provide significant antioxidant protection. Because lipoic acid appears in the bloodstream after oral administration, we have examined the reduction of ex...

journal_title：Biochemical pharmacology

authors： Constantinescu A,Pick U,Handelman GJ,Haramaki N,Han D,Podda M,Tritschler HJ,Packer L

更新日期：1995-07-17 00:00:00

abstract：:The carrier protein for methotrexate and tetrahydrofolate cofactors (GP-MTX) in CCRF-CEM human lymphoblastic leukemia cells in a 117 kDa glycoprotein containing both N- and O-linked oligosaccharides (Matherly et al., J Biol Chem 267: 23253-23260, 1992). Tunicamycin, an inhibitor of N-glycosylation, was used to investi...

journal_title：Biochemical pharmacology

authors： Matherly LH,Angeles SM

更新日期：1994-03-15 00:00:00

abstract：:SAD-128 was found to be an effective protector of acetylcholinesterase against inhibition by soman, due to its ability to function as a reversible inhibitor and allosteric modifier of the AChE active site. It also attenuated aging of the soman-inhibited enzyme. In order to study the connection between some of these ef...

journal_title：Biochemical pharmacology

authors： Stalc A,Sentjurc M

更新日期：1990-12-01 00:00:00

abstract：:Recently, accumulated statistical data indicate the protective effect of caffeine consumption against several types of cancer diseases. There are also reports about protective effect of caffeine and other xanthines against tumors induced by polycyclic aromatic hydrocarbons. One of the explanations is based on biologic...

journal_title：Biochemical pharmacology

authors： Kapuscinski J,Ardelt B,Piosik J,Zdunek M,Darzynkiewicz Z

更新日期：2002-02-15 00:00:00