Effect of diethyl maleate on the biliary excretion rate of infused sulfobromophthalein-glutathione.

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

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

更新日期：1996-11-22 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：:Antitubulin activities of ansamitocins, maytansine and four maytansinoids which are structurally related to ansamitocins were studied using three reaction systems; inhibition of polymerization of bovine brain tubulin, depolymerization of the once polymerized tubulin, and immunofluorescent staining of cytoplasmic micro...

journal_title：Biochemical pharmacology

authors： Ikeyama S,Takeuchi M

更新日期：1981-09-01 00:00:00

abstract：:Resveratrol decreases basal and induced CYP1A1 mRNA/protein levels in both in vitro and in vivo models, and some studies suggest that resveratrol acts as an aryl hydrocarbon receptor (AhR) antagonist. Treatment of T47D or MCF-7 cells with 10 microM resveratrol inhibited induction of CYP1A1 mRNA and CYP1A1-dependent ac...

journal_title：Biochemical pharmacology

authors： Lee JE,Safe S

更新日期：2001-10-15 00:00:00

abstract：:The effects of propranolol or phentolamine on the metabolism of phospholipids, diacylglycerol, and triacylglycerol were studied in the bovine retina in vitro. Lipid labeling was followed during short-term incubation of intact bovine retinas with [U-14C]glycerol and [1-14C]palmitic acid. Each of these precursors was re...

journal_title：Biochemical pharmacology

authors： de Boschero MG,Bazan NG

更新日期：1982-03-15 00:00:00

abstract：:Knowledge of the nature of the interaction between the stimulatory G protein (Gs) and the adenylyl cyclase catalytic unit (C) is essential for interpreting the effects of Gs mutations and expression levels on cellular response to a wide variety of hormones, drugs, and neurotransmitters. It has been proposed that beta-...

journal_title：Biochemical pharmacology

authors： Krumins AM,Lapeyre JN,Clark RB,Barber R

更新日期：1997-07-01 00:00:00

abstract：:The role of Na(+) and Na(+) exchangers in intracellular Ca(2+) elevation and leukotriene B(4) (LTBs) formation was investigated in granulocyte macrophage colony-stimulating factor (GM-CSF)-primed, fMLP-stimulated human neutrophils. Isotonic substitution of extracellular Na(+) with N-methyl-D-glucamine(+) (NMDG(+)) res...

journal_title：Biochemical pharmacology

authors： Tedeschi A,Ciceri P,Zarini S,Lorini M,Di Donato M,Nicosia S,Miadonna A,Sala A

更新日期：2004-01-15 00:00:00

abstract：:Administration of pentylenetetrazol (PTZ) (60 mg/kg, s.c.) to normal or carbaryl (200 mg/kg, p.o.) treated adult male albino rats produced characteristic changes in the steady-state levels of striatal dopamine (DA), noradrenaline (NA) and homovanillic acid (HVA) at different time intervals (0.5, 1.0 and 2.0 hr). The e...

journal_title：Biochemical pharmacology

authors： Ray SK,Poddar MK

更新日期：1985-02-15 00:00:00

abstract：:The present study aimed to investigate endothelin-1 (ET-1) receptors in human and swine cardiomyocytes with binding studies using ET(A) and ET(B) selective receptor antagonists (BMS-182874 and BQ-788, respectively). Cell distribution of mRNA expression for ET(A) and ET(B) subtypes was investigated by in situ hybridiza...

journal_title：Biochemical pharmacology

authors： Modesti PA,Vanni S,Paniccia R,Perna A,Maccherini M,Lisi G,Sani G,Neri Serneri GG

更新日期：1999-07-15 00:00:00

abstract：:The interaction of dicumarol derivatives and protriptyline with respect to the binding to alpha 1-acid glycoprotein (AGP) has been investigated by circular dichroism (CD), equilibrium dialysis and ultrafiltration. Investigation of the induced CD spectra of dicumarol derivatives bound to AGP indicated that the conforma...

journal_title：Biochemical pharmacology

authors： Miyoshi T,Yamamichi R,Maruyama T,Takadate A,Otagiri M

更新日期：1992-05-28 00:00:00

abstract：:Guinea pig gallbladder muscle strips were used to investigate the contribution of different sources of diacylglicerol (DAG) in the cholecystokinin (CCK)-induced contraction. The involvement of arachidonic acid (AA) in this response was also investigated. Three distinct pathways for DAG production were investigated wit...

journal_title：Biochemical pharmacology

authors： Alcón S,Morales S,Camello PJ,Pozo MJ

更新日期：2002-10-01 00:00:00

abstract：:Intact brain cell aggregates were dissociated from adult rat brains, by a simple sieving technique, and were used to study the binding characteristics of [3H]N-methylscopolamine to muscarinic acetylcholine receptors. The magnitude of binding of this ligand was related linearly to the amount of cell protein in the bind...

journal_title：Biochemical pharmacology

authors： Lee JH,el-Fakahany EE

更新日期：1985-12-15 00:00:00

abstract：:Radioligand binding techniques are commonly used in the characterization of beta-adrenergic receptors on human peripheral leukocytes. Accurate interpretation of receptor binding parameters necessitates appropriate radioligand selection. In addition, cell isolation techniques should have minimal effect on the binding p...

journal_title：Biochemical pharmacology

authors： Szefler SJ,Edwards CK 3rd,Haslett C,Zahniser NR,Miller JA,Henson PM

更新日期：1987-05-15 00:00:00

abstract：:Despite the steadily increased numbers of formyl peptide receptor (FPR) ligands identified over the years, few have been characterized in studies using animal disease models and even less have entered clinical trials in human subjects. A small-molecule compound, Act-389949, was however recently tested in a phase I cli...

journal_title：Biochemical pharmacology

authors： Lind S,Sundqvist M,Holmdahl R,Dahlgren C,Forsman H,Olofsson P

更新日期：2019-08-01 00:00:00

abstract：:Exogenous phosphatidic acid (PA) was observed to produce a concentration-dependent increase in [Ca(2+)](i) in cultured A10 vascular smooth muscle cells. Preincubation of cells with sarcoplasmic reticulum Ca(2+)-ATPase inhibitors (cyclopiazonic acid and thapsigargin), a phospholipase C inhibitor (2-nitro-4-carboxypheny...

journal_title：Biochemical pharmacology

authors： Bhugra P,Xu YJ,Rathi S,Dhalla NS

更新日期：2003-06-15 00:00:00

abstract：:The effect of methotrexate (MTX) on 6-mercaptopurine (6-MP) metabolism was studied in four human leukemic cell lines in vitro. CCRF-CEM, WI-L2, TBJ, and HL-60 all expressed thiopurine methyltransferase (TPMT) activity. The cells were grown in horse serum-supplemented RPMI 1640 medium to which was added 4 microM of 6-M...

journal_title：Biochemical pharmacology

authors： Giverhaug T,Loennechen T,Aarbakke J

更新日期：1998-05-15 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：:Multidrug resistance-associated protein 2 (Mrp2) is an ATP-dependent export pump that mediates the formation of bile-salt-independent bile flow. Disruption of the canalicular localization of Mrp2, without changes in its expression, is observed in chronic liver failure and is accompanied by oxidative stress. We reporte...

journal_title：Biochemical pharmacology

authors： Saeki J,Sekine S,Horie T

更新日期：2011-01-01 00:00:00

abstract：:Aspirin (ASA) and other nonsteroidal anti-inflammatory drugs (NSAIDs) inhibit colorectal tumorigenesis. Apoptosis is a critical determinant of tissue mass homeostasis and may play a role in carcinogenesis. We studied the effect of ASA on the survival of a human colon cancer cell line using more sensitive methods than ...

journal_title：Biochemical pharmacology

authors： Qiao L,Hanif R,Sphicas E,Shiff SJ,Rigas B

更新日期：1998-01-01 00:00:00

abstract：:Pancreatic stellate cells (PSCs) play a key role in pancreatic fibrosis, a constant feature of chronic pancreatitis. PSC activation occurs in response to profibrogenic mediators such as cytokines and involves proliferation, transition towards a myofibroblastic phenotype and enhanced production of extracellular matrix ...

journal_title：Biochemical pharmacology

authors： Jaster R,Brock P,Sparmann G,Emmrich J,Liebe S

更新日期：2003-04-15 00:00:00

abstract：:The nicotinic acetylcholine receptors (nAChR) assembled from alpha4 and beta2 subunits are the most densely expressed subtype in the brain. Concentration-effect curves for agonist activation of alpha4beta2*-nAChR are biphasic. This biphasic agonist sensitivity is ascribed to differences in subunit stoichiometry. The s...

journal_title：Biochemical pharmacology

authors： Marks MJ,Meinerz NM,Brown RW,Collins AC

更新日期：2010-10-15 00:00:00

abstract：:Neuronal nicotinic acetylcholine receptors (nAChR), recognized targets for drug development in cognitive and neuro-degenerative disorders, are allosteric proteins with dynamic interconversions between multiple functional states. Activation of the nAChR ion channel is primarily controlled by the binding of ligands (ago...

journal_title：Biochemical pharmacology

authors： Williams DK,Wang J,Papke RL

更新日期：2011-10-15 00:00:00

abstract：:Glutathione transferases are believed to play an important protective role in the various tissues of animals and man by catalysing the glutathione conjugation of electrophilic drugs and electrophilic drug metabolites. Many of these compounds have the potential to react with vital cellular macromolecules in the absence...

journal_title：Biochemical pharmacology

authors： Ahokas JT,Davies C,Ravenscroft PJ,Emmerson BT

更新日期：1984-06-15 00:00:00

abstract：:Antioxidant and anti-inflammatory therapy approaches have been in the focus of attention in the treatment of neurodegenerative Parkinson's and Alzheimer's diseases where oxidative stress has been implicated. Tea extracts have been previously reported to possess radical scavenger, iron chelating and anti-inflammatory p...

journal_title：Biochemical pharmacology

authors： Levites Y,Youdim MB,Maor G,Mandel S

更新日期：2002-01-01 00:00:00

abstract：:Platelet derived growth factor (PDGF) is a key factor in the induction and progression of fibrotic diseases with the activated fibroblast as its target cell. Drug targeting to the PDGF-receptor is explored as a new approach to treat this disease. Therefore, we constructed a macromolecule with affinity for the PDGF-bet...

journal_title：Biochemical pharmacology

authors： Beljaars L,Weert B,Geerts A,Meijer DK,Poelstra K

更新日期：2003-10-01 00:00:00

abstract：:Neurofibromatosis type 1 (NF1) is the most common cancer predisposition syndrome. NF1 patients present with a constellation of clinical manifestations and have an increased risk of developing certain benign and malignant tumors. This disease results from mutation within the gene encoding neurofibromin, a GTPase activa...

journal_title：Biochemical pharmacology

authors： Dilworth JT,Kraniak JM,Wojtkowiak JW,Gibbs RA,Borch RF,Tainsky MA,Reiners JJ Jr,Mattingly RR

更新日期：2006-11-30 00:00:00

abstract：:The inhibition of semicarbazide-sensitive amine oxidase (SSAO) in rat aorta homogenates by some 2-phenyl-3-haloallylamines has been studied. Derivatives containing a fluorine atom were approximately three times more potent than the corresponding 3-chloroallylamines. These halogen-containing compounds were irreversible...

journal_title：Biochemical pharmacology

authors： Lyles GA,Marshall CM,McDonald IA,Bey P,Palfreyman MG

更新日期：1987-09-01 00:00:00

abstract：:Curcumin (diferuloylmethane) is a well-known agent with anti-inflammatory, antioxidant, and anticarcinogenic properties. In this study, we observed that curcumin inhibited the kinase activity of v-Src, which led to a decrease in tyrosyl substrate phosphorylation of Shc, cortactin, and FAK. Our in vitro kinase experime...

journal_title：Biochemical pharmacology

authors： Leu TH,Su SL,Chuang YC,Maa MC

更新日期：2003-12-15 00:00:00

abstract：:Atopic diseases (atopic dermatitis, asthma and allergic rhinitis) affects a huge number of people around the world and their incidence rate is on rise. Atopic dermatitis (AD) is more prevalent in paediatric population which sensitizes an individual to develop allergic rhinitis and asthma later in life. The complex pat...

journal_title：Biochemical pharmacology

authors： Sharma S,Naura AS

更新日期：2020-03-01 00:00:00

abstract：:Class B peptide hormone GPCRs are targets for the treatment of major chronic disease. Peptide ligands of these receptors display biased agonism and this may provide future therapeutic advantage. Recent active structures of the calcitonin (CT) and glucagon-like peptide-1 (GLP-1) receptors reveal distinct engagement of ...

journal_title：Biochemical pharmacology

authors： Dal Maso E,Zhu Y,Pham V,Reynolds CA,Deganutti G,Hick CA,Yang D,Christopoulos A,Hay DL,Wang MW,Sexton PM,Furness SGB,Wootten D

更新日期：2018-04-01 00:00:00