Characterization of sequence-dependent synergy between ZD1839 ("Iressa") and oxaliplatin.

abstract：:Certain anticonvulsant drugs require N-acetylation as a major route of metabolic clearance. Single point mutations of the polymorphic N-acetyltransferase gene (pNAT) are the primary cause for impaired drug acetylation. Pharmacokinetic parameters are altered in slow acetylator phenotypes and this may compromise drug sa...

journal_title：Biochemical pharmacology

authors： Borlak JT,Harsany V,Schneble H,Haegele KD

更新日期：1994-11-01 00:00:00

abstract：:Bufuralol hydroxylation activities of liver microsomal cytochrome P450 (P450) enzymes were studied in the rat; the reaction has been used widely in determining levels of liver microsomal P450 2D6, which shows debrisoquine-type genetic polymorphism in humans. Liver microsomes catalyzed the conversion of bufuralol to 1'...

journal_title：Biochemical pharmacology

authors： Mimura M,Yamazaki H,Sugahara C,Hiroi T,Funae Y,Shimada T

更新日期：1994-06-01 00:00:00

abstract：:Chronic ethanol use can lead to folic acid deficiency in humans. In rats, acute doses of ethanol produce a marked increase in the urinary excretion of folate which is followed by a decrease in plasma folate levels. To assess the respective roles of ethanol and its metabolism in these effects, five groups of male Sprag...

journal_title：Biochemical pharmacology

authors： McMartin KE,Collins TD

更新日期：1983-09-01 00:00:00

abstract：:The partition coefficients (Kp) of three prototype Ca2+ antagonists, nitrendipine, (-)-desmethoxyverapamil and flunarizine were determined in native synaptic plasma membranes (SPM) isolated from sheep brain cortex and in liposomes prepared with the total lipids extracted from the membranes. We found that at 25 degrees...

journal_title：Biochemical pharmacology

authors： Carvalho CM,Oliveira CR,Lima MP,Leysen JE,Carvalho AP

更新日期：1989-07-01 00:00:00

abstract：:To uncover the full spectrum of its pharmacological activities, the selective COX-2 inhibitor celecoxib is routinely being used at concentrations of up to 100 microM in cell culture. At these elevated concentrations, several COX-2-independent effects were identified, although many details of these events have remained...

journal_title：Biochemical pharmacology

authors： Pyrko P,Kardosh A,Schönthal AH

更新日期：2008-01-15 00:00:00

abstract：:Diethyl maleate (DEM) was given intraperitoneally to rats in a dose (4.3 mmoles/kg) known to markedly decrease glutathione levels in liver. DEM induced a choleresis previously shown to be due to the osmotic activity of DEM conjugates (DEM-glutathione and subsequent metabolic products) excreted into bile. Coincident wi...

journal_title：Biochemical pharmacology

authors： Combes B,Backof B

更新日期：1982-08-15 00:00:00

abstract：:Low molecular weight cadmium-binding proteins were studed in lung tissue from rabbits exposed to aerosols of CdCl2. Lungs obtained from animals exposed by inhalation to aerosols of 800 or 1600 micrograms/m3 CdCl2 for 2-hr periods/day, every other day for a 5-day period, were found to contain at least three low molecul...

journal_title：Biochemical pharmacology

authors： Post CT,Squibb KS,Fowler BA,Gardner DE,Illing J,Hook GE

更新日期：1982-09-15 00:00:00

abstract：:Tetranitromethane (TNM) is a reagent which reacts with the tyrosine and cysteine residues of proteins. Chemical modification of partially purified human platelet alpha 2-adrenoceptors with TNM resulted in an irreversible loss of binding activity. Typically, an 80-90% decrease in binding activity occurred with a 60-min...

journal_title：Biochemical pharmacology

authors： Nakata H,Regan JW,Lefkowitz RJ

更新日期：1986-11-15 00:00:00

abstract：:The anti-anginal agent bepridil blocks slow Ca2+ channels in a variety of tissues. Since bepridil accumulates inside cells, the possibility exists that bepridil acts, at least partially, from inside the cell. To test this possibility, we examined the effects of a quaternary ammonium analog of bepridil, methylated bepr...

journal_title：Biochemical pharmacology

authors： Wahler GM,Doane JD,Ousterhout JM,Sperelakis N,Lamar JC,Busch N,Biswas JC,Rogers TB

更新日期：1986-07-15 00:00:00

abstract：:Ethyl 2[5(4-chlorophenyl)pentyl]oxirane-2-carboxylate (POCA) is strongly hypoglycaemic in fasted normal and diabetic rats [H. P. O. Wolf, K. Eistetter and G. Ludwig, Diabetologia 22, 456 (1982)]. POCA was fed for 12 weeks to rats on a standard low-fat (3%) diet at levels of 0.05% and 0.2% to give daily intakes of abou...

journal_title：Biochemical pharmacology

authors： Koundakjian PP,Turnbull DM,Bone AJ,Rogers MP,Younan SI,Sherratt HS

更新日期：1984-02-01 00:00:00

abstract：:The seminal vesicle protein No. 4 (SV-IV) secreted from the rat seminal vesicle epithelium, possesses immunosuppressive and anti-inflammatory properties and it is a potent inhibitor of platelet aggregation both in vivo and in vitro. This research aimed to investigate the possible effect of SV-IV on the process of huma...

journal_title：Biochemical pharmacology

authors： Di Micco B,Colonna G,Porta R,Metafora S

更新日期：1994-07-19 00:00:00

abstract：:The actions of eight cationic amphiphilic drugs on human platelets displayed three different effects according to drug concentration ranges. At lower concentrations (below approximately 25 microM), the drugs stimulated secretory responses induced by 0.2 U/mL of thrombin, while at concentrations in the 25-50 microM ran...

journal_title：Biochemical pharmacology

authors： Tharmapathy P,Fukami MH,Holmsen H

更新日期：2000-11-01 00:00:00

abstract：:The possibility of NQ12 (2-chloro-3-[4-(ethylcarboxy)-phenyl]-amino-1,4-naphthoquinone) as a novel antithrombotic agent and its mode of action were investigated. The effects of NQ12 on platelet aggregation in human platelet-rich plasma in vitro, in rats ex vivo, and on murine pulmonary thrombosis in vivo, as well as t...

journal_title：Biochemical pharmacology

authors： Yuk DY,Ryu CK,Hong JT,Chung KH,Kang WS,Kim Y,Yoo HS,Lee MK,Lee CK,Yun YP

更新日期：2000-10-01 00:00:00

abstract：:3,3-Dimethylbutanol (Dimbunol), a competitive inhibitor of choline dehydrogenase (CDH), and ethylcholine mustard aziridinium (ECMA), an effective irreversible inhibitor of both CDH and choline transport, were investigated for their effects upon the uptake and metabolism of [3H]choline in mice. Thirty minutes after Dim...

journal_title：Biochemical pharmacology

authors： Barlow P,Marchbanks RM

更新日期：1985-09-01 00:00:00

abstract：:A series of isoquinolines, N-methyl-1,2-dihydroisoquinolines, N-methyl-1,2,3,4-tetrahydroisoquinolines, 1,2,3,4-tetrahydroisoquinolines, and N-methylisoquinolinium ions were tested as inhibitors of monoamine oxidases A and B. All compounds were found to act as reversible and time-independent MAO inhibitors, often with...

journal_title：Biochemical pharmacology

authors： Thull U,Kneubühler S,Gaillard P,Carrupt PA,Testa B,Altomare C,Carotti A,Jenner P,McNaught KS

更新日期：1995-09-07 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：:The present study investigated the mechanism by which theophylline decreases cis-diamminedichloroplatinum(II) (DDP)-induced DNA crosslinking in L1210 cells. Alkaline elution of DNA from L1210 cells treated with DDP in the presence and absence of 1 mM theophylline showed that theophylline decreased interstrand crosslin...

journal_title：Biochemical pharmacology

authors： Ducore JM

更新日期：1986-02-15 00:00:00

abstract：:Metyrapone (2-methyl-1,2-di-3-pyridyl-1-propanone, MTP) is used as an inhibitor of cytochrome P-450 enzymes, particularly those induced by phenobarbital (PB). We examined the effects of MTP on the microsomal dependent mutagenesis of a newly isolated promutagen, 3-(2-chloroethoxy)-1,2-dichloropropene (CP), three S-chlo...

journal_title：Biochemical pharmacology

authors： Distlerath LM,Loper JC,Tabor MW

更新日期：1983-12-15 00:00:00

abstract：:Chronic inflammation has been implicated as the underlying factor in the pathogenesis of many disorders. In the past decade, inflammation-related endogenous production of reactive nitrogen species, similar to oxygen free radicals, has also been suggested as a risk factor for cancer, in addition to the well-studied exo...

journal_title：Biochemical pharmacology

authors： Chan MM,Fong D,Ho CT,Huang HI

更新日期：1997-12-15 00:00:00

abstract：:Metabolic activation to catechols and their oxidation products is variously considered to contribute to the genotoxic, cytotoxic, transforming and tumour-promoting activities of exogenous steroidal oestrogens. 2-Fluoro-17 alpha-ethynyloestradiol (2-FEE2) was synthesized as a prototype of pharmacologically active deriv...

journal_title：Biochemical pharmacology

authors： Morgan P,Maggs JL,Page PC,Park BK

更新日期：1992-11-03 00:00:00

abstract：:cis-platinum(II) (cis-diammine dichloroplatinum; cisplatin) is a potent antitumor compound that is widely used for the treatment of many malignancies. An important side-effect of cisplatin is nephrotoxicity, which results from injury to renal tubular epithelial cells and can be manifested as either acute renal failure...

journal_title：Biochemical pharmacology

authors： Lee RH,Song JM,Park MY,Kang SK,Kim YK,Jung JS

更新日期：2001-10-15 00:00:00

abstract：:The regulation of tissue transglutaminase (TG2) activity by the GPCR family is poorly understood. In this study, we investigated the modulation of TG2 activity by the A1 adenosine receptor in cardiomyocyte-like H9c2 cells. H9c2 cells were lysed following stimulation with the A1 adenosine receptor agonist N(6)-cyclopen...

journal_title：Biochemical pharmacology

authors： Vyas FS,Hargreaves AJ,Bonner PL,Boocock DJ,Coveney C,Dickenson JM

更新日期：2016-05-01 00:00:00

abstract：:To investigate the potential interactions between the angiotensin II (Ang II) and insulin signaling systems, regulation of IRS-1 phosphorylation and insulin-induced Akt activation by Ang II were examined in clone 9 (C9) hepatocytes. In these cells, Ang II specifically inhibited activation of insulin-induced Akt Thr(30...

journal_title：Biochemical pharmacology

authors： Arellano-Plancarte A,Hernandez-Aranda J,Catt KJ,Olivares-Reyes JA

更新日期：2010-03-01 00:00:00

abstract：:Smoking during pregnancy is the largest modifiable risk factor for pregnancy-related morbidity and mortality. The success of bupropion for smoking cessation warrants its investigation for the treatment of pregnant patients. Nevertheless, the use of bupropion for the treatment of pregnant smokers requires additional da...

journal_title：Biochemical pharmacology

authors： Wang X,Abdelrahman DR,Zharikova OL,Patrikeeva SL,Hankins GD,Ahmed MS,Nanovskaya TN

更新日期：2010-06-01 00:00:00

abstract：:The mechanism of aerobic resistance to the quinone-containing anti-tumour agents mitomycin C (MMC) and porfiromycin (PM) has been investigated using non-transformed human cells. One of the cell strains used (3437T) was derived from an afflicted member of a cancer-prone family. This cell strain had been shown previousl...

journal_title：Biochemical pharmacology

authors： Marshall RS,Paterson MC,Rauth AM

更新日期：1991-05-01 00:00:00

abstract：:The influence of various concentrations of ferrous iron and ascorbate on in vitro peroxidation and drug binding of diverse membrane preparations (cerebral cortex and liver) was studied. Peroxidation was not simply dose-related to ascorbate and ferrous iron, but a complex relationship between iron and ascorbate when ad...

journal_title：Biochemical pharmacology

authors： Courtiere A,Molard F,Reybaud J

更新日期：1995-11-27 00:00:00

abstract：:Tannins are polyphenols commonly found in plant-derived foods. When ingested they can have various harmful effects, but salivary proline-rich proteins (PRPs) may provide protection against dietary tannins. The aim of this study was to investigate whether basic PRPs, a major family of salivary proteins, can prevent int...

journal_title：Biochemical pharmacology

authors： Cai K,Hagerman AE,Minto RE,Bennick A

更新日期：2006-05-28 00:00:00

abstract：:Brain penetration of drugs which are subject to P-glycoprotein (Pgp)-mediated efflux is attenuated, as manifested by the fact that the cerebrospinal fluid concentration (C(CSF)), a good surrogate of the unbound brain concentration (C(ub)), is lower than the unbound plasma concentration (C(up)) for Pgp substrates. In r...

journal_title：Biochemical pharmacology

authors： Tang C,Kuo Y,Pudvah NT,Ellis JD,Michener MS,Egbertson M,Graham SL,Cook JJ,Hochman JH,Prueksaritanont T

更新日期：2009-09-15 00:00:00

abstract：:The ability of adrenergic catechol derivatives, including dobutamine, dopamine, and isoproterenol, to inhibit lipid peroxidation was examined. All the catechol derivatives we tested strongly inhibited lipid peroxidation. Dobutamine was a more powerful inhibitor of iron-catalyzed lipid peroxidation than the other agent...

journal_title：Biochemical pharmacology

authors： Miura T,Muraoka S,Ogiso T

更新日期：1998-06-15 00:00:00

abstract：:Celastrol, a quinone methide triterpenoid, was isolated as an inhibitor of NF-kappaB from Celastrus orbiculatus. This compound dose-dependently inhibited a variety of stimuli-induced NF-kappa B-regulated gene expression and the DNA-binding of NF-kappa B in different cell lines without affecting DNA-binding activity of...

journal_title：Biochemical pharmacology

authors： Lee JH,Koo TH,Yoon H,Jung HS,Jin HZ,Lee K,Hong YS,Lee JJ

更新日期：2006-11-15 00:00:00