H1 and H2 histamine receptors in N-nitroso-N-methylurea (NMU)-induced carcinomas with atypical coupling to signal transducers.

abstract：:Cobalt is suspected to cause memory deficit in humans and was reported to induce neurotoxicity in animal models. We have studied the effects of cobalt in primary cultures of mouse astrocytes. CoCl(2) (0.2-0.8mM) caused dose-dependent ATP depletion, apoptosis (cell shrinkage, phosphatidylserine externalization and chro...

journal_title：Biochemical pharmacology

authors： Karovic O,Tonazzini I,Rebola N,Edström E,Lövdahl C,Fredholm BB,Daré E

更新日期：2007-03-01 00:00:00

abstract：:Characteristics of methotrexate (MTX) inhibition of dihydrofolic acid reductase (DHFR) enzyme activity and the effects of NADPH and NADH on enzyme-drug interaction were studied. Two highly sensitive assay procedures were used. The first utilized tritium-labeled MTX to measure direct binding properties of the enzyme an...

journal_title：Biochemical pharmacology

authors： Kamen BA,Whyte-Bauer W,Bertino JR

更新日期：1983-06-15 00:00:00

abstract：:A process of differentiation was observed when ob17 preadipocyte cells were stably transfected with a vector containing the cDNA of the human A1 adenosine receptor of adipose tissue. Growth of the cell lines continued but was slowed relative to untransfected cells and cells transfected with vector alone, never attaini...

journal_title：Biochemical pharmacology

authors： Tatsis-Kotsidis I,Erlanger BF

更新日期：1999-07-01 00:00:00

abstract：:HO-1 (heme oxygenase-1), an antioxidant enzyme, induced by rosiglitazone (PPAR ligands) can be a potential treatment of inflammation. However, the mechanisms of rosiglitazone-induced HO-1 expression in human pulmonary alveolar epithelial cells (HPAEpiCs) remain largely unknown. In this study, we found that upregulatio...

journal_title：Biochemical pharmacology

authors： Cho RL,Lin WN,Wang CY,Yang CC,Hsiao LD,Lin CC,Yang CM

更新日期：2018-02-01 00:00:00

abstract：:The influence of age on the mixed function oxidase system from a non-human primate was studied. Microsomes were isolated from the livers of female Macaca nemestrina ranging from 2 to 21 years of age. No significant age-related change was observed in either the cytochrome P-450 content or the NADPH cytochrome c reducta...

journal_title：Biochemical pharmacology

authors： Sutter MA,Wood WG,Williamson LS,Strong R,Pickham K,Richardson A

更新日期：1985-08-15 00:00:00

abstract：:N-Trifluoroacetyladriamycin-14-valerate (AD 32), a lipophilic, DNA non-binding analog of Adriamycin (ADR), was found to be a potent inhibitor of the membrane-bound enzyme, protein kinase C (PKC). PKC was isolated and purified from human leukemia ML-1 cells, and the enzyme activity was shown to be activated by the tumo...

journal_title：Biochemical pharmacology

authors： Chuang LF,Kung HF,Israel M,Chuang RY

更新日期：1992-02-18 00:00:00

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

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

abstract：:The cytoprotective effect of curcumin, a natural constituent of Curcuma longa, on the cytotoxicity of paracetamol in rat hepatocytes was studied. Paracetamol was selected as a model-toxin, since it is known to be bioactivated by 3-methylcholanthrene inducible cytochromes P450 presumably to N-acetyl-p-benzoquinone imin...

journal_title：Biochemical pharmacology

authors： Donatus IA,Sardjoko,Vermeulen NP

更新日期：1990-06-15 00:00:00

abstract：:Mevinolin is a potent competitive inhibitor of HMG-CoA reductase, the enzyme catalyzing the major rate-limiting step in cholesterol synthesis. In this study the drug was administered as an intragastric dose at 2.5 mg/kg/day to 10 to 12-week-old lean and obese Zucker female rats over a 5-day period. Mevinolin showed no...

journal_title：Biochemical pharmacology

authors： McCune SA,Jurin RR

更新日期：1987-03-15 00:00:00

abstract：:Oligodendrocytes and activated macrophages are involved in the immunopathology of demyelinating disease. In this study, we investigated the in vitro effect of dietary compounds, in particular flavonoids, on oxidative damage in OLN-93 oligodendrocytes and on nitric oxide (NO) production by NR8383 macrophages. Using a c...

journal_title：Biochemical pharmacology

authors： van Meeteren ME,Hendriks JJ,Dijkstra CD,van Tol EA

更新日期：2004-03-01 00:00:00

abstract：:Multidrug resistance (MDR) is a phenomenon where cancer cells become simultaneously resistant to anticancer drugs with different structures and mechanisms of action. MDR has been shown to be associated with overexpression of ATP-binding cassette (ABC) transporters. Here, we report that telatinib, a small molecule tyro...

journal_title：Biochemical pharmacology

authors： Sodani K,Patel A,Anreddy N,Singh S,Yang DH,Kathawala RJ,Kumar P,Talele TT,Chen ZS

更新日期：2014-05-01 00:00:00

abstract：:Chondrosarcoma is a common primary malignant tumor of the bone that can metastasize through the vascular system to other organs. A key step in the metastatic process, lymphangiogenesis, involves vascular endothelial growth factor-C (VEGF-C). However, the effects of lymphangiogenesis in chondrosarcoma metastasis remain...

journal_title：Biochemical pharmacology

authors： Su CM,Tang CH,Chi MJ,Lin CY,Fong YC,Liu YC,Chen WC,Wang SW

更新日期：2018-08-01 00:00:00

abstract：:Isothiazole dioxides have been shown to inhibit Trypanosoma brucei protein farnesyltransferase (PFTase) in isolated enzyme, but elicited only a minor effect on mammalian PFTase. In the present study we have evaluated the effect of 3-diethylamino-4-(4-methoxyphenyl)-isothiazole 1,1-dioxides with different substituents ...

journal_title：Biochemical pharmacology

authors： Ferri N,Clerici F,Yokoyama K,Pocar D,Corsini A

更新日期：2005-12-05 00:00:00

abstract：:The (Na+ + K+)-ATPase is localized to the cerebral endothelium, i.e. the blood-brain barrier, and is important for the maintenance of the brain electrolyte environment. Data from the present study indicate that Pb2+ inhibits the binding of [3H]ouabain to the cerebral microvascular (Na+ + K+)-ATPase in a time- and dose...

journal_title：Biochemical pharmacology

authors： Caspers ML,Kwaiser TM,Grammas P

更新日期：1990-06-15 00:00:00

abstract：:Petrosaspongiolide M (PT) is a potent secretory phospholipase A(2) inhibitor and anti-inflammatory agent. This marine metabolite reduced the production of nitrite, prostaglandin E(2), and tumor necrosis factor-alpha in the mouse air pouch injected with zymosan. These effects were also observed in mouse peritoneal macr...

journal_title：Biochemical pharmacology

authors： Posadas I,Terencio MC,Randazzo A,Gomez-Paloma L,Payá M,Alcaraz MJ

更新日期：2003-03-01 00:00:00

abstract：:The effects of the enantiomers of 2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl]methyl]-sulfinyl ]- 1H-benzimidazole (lansoprazole, AG-1749) on acid formation in isolated canine parietal cells and (H+ + K+)-ATPase activity in canine gastric microsomes were investigated. Both the (+)-and the (-)-enantiomer of lanso...

journal_title：Biochemical pharmacology

authors： Nagaya H,Inatomi N,Nohara A,Satoh H

更新日期：1991-10-24 00:00:00

abstract：:Calcipotriol (MC 903) is a novel analogue of the physiologically active metabolite of vitamin D3, 1 alpha,25-dihydroxycholecalciferol [1,25(OH)2D3]. MC 903 and 1,25(OH)2D3 have similar effects on cell proliferation and cell differentiation in vitro using the human histiocytic lymphoma cell line U 937, but in vivo MC90...

journal_title：Biochemical pharmacology

authors： Kissmeyer AM,Binderup L

更新日期：1991-06-01 00:00:00

abstract：:We have performed a systematic study of the interaction of 36 di- and tri-phenylethylene derivatives (DPEs and TPEs) with protein kinase C (PKC). The results were submitted to a multivariate analysis in order to identify the structural features that might be implicated in interference with the activity of three PKC su...

journal_title：Biochemical pharmacology

authors： Bignon E,Pons M,Doré JC,Gilbert J,Ojasoo T,Miquel JF,Raynaud JP,Crastes de Paulet A

更新日期：1991-09-12 00:00:00

abstract：:The peripheral benzodiazepine receptor (PBR), an integral protein of the mitochondrial membrane, is involved in the formation of mitochondrial permeability transition (MPT) pores. The opening of the MPT-leading to the dissipation of the inner-mitochondrial transmembrane potential (deltapsi(m))-is considered to be an e...

journal_title：Biochemical pharmacology

authors： Strohmeier R,Roller M,Sänger N,Knecht R,Kuhl H

更新日期：2002-07-01 00:00:00

abstract：:Duchenne muscular dystrophy (DMD) is caused by dystrophin deficiency, which results in muscle necrosis and the upregulation of heat shock/stress proteins (HSP). We hypothesized that reactive oxygen species, and in particular hydroxyl radicals (.OH), participate in muscle necrosis and HSP expression. It was assumed tha...

journal_title：Biochemical pharmacology

authors： Bornman L,Rossouw H,Gericke GS,Polla BS

更新日期：1998-09-15 00:00:00

abstract：:The chiral inversion properties of 4-(4-methylphenyl)-2-methylthiomethyl-4-oxobutanoic acid (KE-748), an active metabolite of 2-acetylthiomethyl-4-(4-methylphenyl)-4-oxobutanoic acid (KE-298), were compared with those of ibuprofen in rats. After administration of R(-)-[2 alpha-2H]KE-748, S(+)-KE-748 was present in the...

journal_title：Biochemical pharmacology

authors： Yoshida H,Kohno Y,Endo H,Yamaguchi J,Fukushima K,Suwa T,Hayashi M

更新日期：1997-01-24 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 levels and subcellular distribution of enzymes involved in defenses against reactive oxygen superoxide dismutase (SOD; E.C.1.15.1.1), glutathione peroxidase (GPX; E.C.1.11.1.9), catalase (CAT; E.C.1.11.1.6), and DT-diaphorase (DT; E.C.1.6.99.2) and of the conjugating enzymes glutathione transferase (GST; E.C.2.5.1...

journal_title：Biochemical pharmacology

authors： Eliasson M,Boström M,DePierre JW

更新日期：1999-10-15 00:00:00

abstract：:N417/AMSA cells, about 80-fold resistant to mAMSA [4'-(9-acridinylamino)-methanesulfon-m-anisidide], were obtained by serial passages of the parental human small cell lung carcinoma NCI-N417 (N417/p) in stepwise drug concentrations. The N417/AMSA cells were found to be 114-, 100-, and 9-fold cross-resistant to the top...

journal_title：Biochemical pharmacology

authors： Prost S,Riou G

更新日期：1994-08-30 00:00:00

abstract：:Nitric oxide sensitive guanylyl cyclase (NOsGC) is a heterodimeric enzyme consisting of an α and a β subunit. Two heterodimeric enzymes are known to be important for NO-signalling in humans: α(1)/β(1) and α(2)/β(1). No difference had so far been detected with respect to their pharmacological properties, but as we show...

journal_title：Biochemical pharmacology

authors： Haase N,Haase T,Kraehling JR,Behrends S

更新日期：2010-12-01 00:00:00

abstract：:Identification of the proximate peroxisome proliferator(s) derived from di (2-ethylhexyl) adipate (DEHA) has been achieved using primary hepatocyte cultures derived from different species and cyanide-insensitive fatty acyl CoA oxidase (PCO) as a marker enzyme for peroxisome proliferation. In rat and mouse hepatocytes,...

journal_title：Biochemical pharmacology

authors： Cornu MC,Lhuguenot JC,Brady AM,Moore R,Elcombe CR

更新日期：1992-05-28 00:00:00

abstract：:The serine esterase inhibitor diisopropyl fluorophosphate (DFP) had been reported previously to inhibit IgE-dependent histamine release. Recently, it has been demonstrated that lower concentrations of DFP enhance IgE-dependent histamine release and inhibit desensitization. This manuscript describes the abilities of se...

journal_title：Biochemical pharmacology

authors： Meier HL,Gross CL,Papirmeister B

更新日期：1986-12-01 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：:Monocrotaline is a pyrrolizidine alkaloid obtained from the seeds of Crotalaria spectabilis. When perfused through an isolated liver, monocrotaline is metabolized to Ehrlich reactive (E+) metabolites. Metabolism of monocrotaline was faster in livers from male rats than female rats, was inducible with phenobarbital pre...

journal_title：Biochemical pharmacology

authors： Lafranconi WM,Huxtable RJ

更新日期：1984-08-01 00:00:00

abstract：:Inflammatory events are tightly associated with the death caused by Herpes simplex virus 1 (HSV-1) infection of the brain. Heat shock protein 90 (Hsp90) is a molecular chaperone that is stimulated in response to many stressful conditions (e.g., inflammation and hypoxia) and Hsp90 inhibitors are suggested to be potent ...

journal_title：Biochemical pharmacology

authors： Li F,Song X,Su G,Wang Y,Wang Z,Qing S,Jia J,Wang Y,Huang L,Zheng K,Wang Y

更新日期：2019-08-01 00:00:00