Comparative study of clofibric acid and bilirubin glucuronidation in human liver microsomes.

abstract：:Thromboxane A2 is a potent mediator of inflammation and platelet aggregation exerting its effects through the activation of a G protein-coupled receptor (GPCR), termed TP. Although the existence of dimers/oligomers in Class A GPCRs is widely accepted, their functional significance still remains controversial. Recently...

journal_title：Biochemical pharmacology

authors： Capra V,Mauri M,Guzzi F,Busnelli M,Accomazzo MR,Gaussem P,Nisar SP,Mundell SJ,Parenti M,Rovati GE

更新日期：2017-01-15 00:00:00

abstract：:Tannic acid (TA) is a naturally occurring phenol, which has been found to display an antipromotion effect on mouse skin carcinogenesis. In order to explore the molecular mechanism, we have examined the process of 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced protein kinase C (PKC) activation, including phorbol es...

journal_title：Biochemical pharmacology

authors： Kuo ML,Wu WS,Lee KC,Lin JK

更新日期：1993-10-19 00:00:00

abstract：:1-(3'-Chlorophenyl)-3-[2-(3,3-dimethyl-1-azetidinyl)ethyl] imidazolidin-2-one, zetidoline, a new neuroleptic agent, when incubated with rat liver microsomes was rapidly metabolized to six free (mets B, D, I, L, M and N) and two conjugated metabolites (mets E and F). Sites of the metabolic attack (oxidation) were prima...

journal_title：Biochemical pharmacology

authors： Assandri A,Galliani G,Zerilli L,Tuan G,Tarzia G,Barone D

更新日期：1986-05-01 00:00:00

abstract：:The effect of metformin (N,N-dimethylbiguanide) on the rate-limiting enzymes of cholesterol metabolism was observed. 3-Hydroxy-3-methylglutaryl-CoA reductase (HMG-CoA reductase) and acyl-CoA-cholesterol acyltransferase (ACAT) activities were estimated in hepatic microsomal and intestinal cell preparations from normal ...

journal_title：Biochemical pharmacology

authors： Scott LM,Tomkin GH

更新日期：1983-03-01 00:00:00

abstract：:Squalene synthase (SQS) catalyses a step following the final branch in the pathway of cholesterol biosynthesis. Inhibition of this enzyme, therefore, is an approach for the treatment of atherosclerosis with the potential for low side effects. We have characterised the inhibition of rat liver microsomal SQS by 3-(biphe...

journal_title：Biochemical pharmacology

authors： Ward WH,Holdgate GA,Freeman S,McTaggart F,Girdwood PA,Davidson RG,Mallion KB,Brown GR,Eakin MA

更新日期：1996-06-14 00:00:00

abstract：:Incubation of adriamycin resistant Chinese hamster lung cells with the calmodulin inhibitor trifluoperazine (TFP) resulted in a significant increase in the cellular accumulation of drug. When resistant cells were prelabeled with 32Pi and then treated with TFP, a major increase also occurred in the phosphorylation of a...

journal_title：Biochemical pharmacology

authors： Center MS

更新日期：1985-05-01 00:00:00

abstract：:We investigated whether morphine and its pro-drug codeine are substrates of the highly genetically polymorphic organic cation transporter OCT1 and whether OCT1 polymorphisms may affect morphine and codeine pharmacokinetics in humans. Morphine showed low transporter-independent membrane permeability (0.5 × 10⁻⁶ cm/s). ...

journal_title：Biochemical pharmacology

authors： Tzvetkov MV,dos Santos Pereira JN,Meineke I,Saadatmand AR,Stingl JC,Brockmöller J

更新日期：2013-09-01 00:00:00

abstract：:U73122 ((1-[6-(( 17beta-3-methoxyestra-1,3,5(10)-trien-17-yl)amino)exyl]-1H-p yrrole-2,5-dione)) is generally used as a selective inhibitor of phospholipase C (PLC) and the related rise in cytosolic Ca2+. Recently, by using hepatocytes, it was suggested that its action sites are different for PLC activation and increa...

journal_title：Biochemical pharmacology

authors： Pulcinelli FM,Gresele P,Bonuglia M,Gazzaniga PP

更新日期：1998-12-01 00:00:00

abstract：:Arsenic, still a significant environmental threat in several regions in the world, induces various cancers, including lungs, skin, and bladder. Arsenic-induced Bowen's disease (As-BD) is generally an indolent cutaneous intraepithelial carcinoma in susceptible people. Patients with As-BD have been found to have attenua...

journal_title：Biochemical pharmacology

authors： Lee CH,Hong CH,Yu CL,Wang LF,Clausen BE,Liao WT,Huang SK,Chen GS,Yu HS

更新日期：2012-05-01 00:00:00

abstract：:Macrophage migration inhibitory factor (MIF) plays some pivotal roles in innate immunity and inflammation. Ursolic acid (UA), an anti-inflammatory triterpene carboxylic acid, was recently reported to induce the release of pro-inflammatory mediators in resting macrophages (Mvarphi). We investigated the effects of UA on...

journal_title：Biochemical pharmacology

authors： Ikeda Y,Murakami A,Ohigashi H

更新日期：2005-11-15 00:00:00

abstract：:Selective and marked 3-hydroxylase deficiency of lidocaine and its N-deethylated metabolite, MEGX, were observed in male and female DA rats. These findings suggest that cytochrome P450 isozymes metabolizing debrisoquine may be involved in the 3-hydroxylations of lidocaine and MEGX in rats and humans. ...

journal_title：Biochemical pharmacology

authors： Masubuchi Y,Umeda S,Chiba M,Fujita S,Suzuki T

更新日期：1991-07-15 00:00:00

abstract：:The effect of low M(r) heparin fragments (CY222) and fetal calf serum (FCS) on the level of fibronectin and fibrillar collagen mRNAs was investigated in smooth muscle cells (SMC) in culture. In the absence of FCS, addition of CY222 (100 micrograms/10(6) cells) to postconfluent early passage SMC resulted in a decrease ...

journal_title：Biochemical pharmacology

authors： Asselot-Chapel C,Combacau L,Labat-Robert J,Kern P

更新日期：1995-03-01 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：:Arylamine N-acetyltransferase 1 (NAT1) conjugates several aromatic amines and their N-hydroxylated metabolites by N- or O-acetylation. NAT1 genotype and phenotype is known to be variable in human populations. In this study, we set out to measure the functional relevance of the frequent NAT1 gene variants for the activ...

journal_title：Biochemical pharmacology

authors： Bruhn C,Brockmöller J,Cascorbi I,Roots I,Borchert HH

更新日期：1999-12-01 00:00:00

abstract：:The effects of the anti-inflammatory drugs diclofenac, piroxicam, indomethacin, naproxen, nabumetone, nimesulide, and meloxicam on mitochondrial respiration, ATP synthesis, and membrane potential were determined. Except for nabumetone and naproxen, the other drugs stimulated basal and uncoupled respiration, inhibited ...

journal_title：Biochemical pharmacology

authors： Moreno-Sánchez R,Bravo C,Vásquez C,Ayala G,Silveira LH,Martínez-Lavín M

更新日期：1999-04-01 00:00:00

abstract：:A comparison of the effects of various phosphodiesterase (PDE) inhibitors upon cellular cAMP levels was undertaken in human neuroblastoma SH-SY5Y cells. When inhibitors such as rolipram and Ro 20 1724 (selective for the low Km cAMP-specific PDE) were used, cAMP levels were seen to rise dramatically under basal (< or =...

journal_title：Biochemical pharmacology

authors： Morgan AJ,Murray KJ,Challiss RA

更新日期：1993-06-22 00:00:00

abstract：:To study the effect of sex hormones and alcohol on the hepatic activities of alcohol metabolizing enzymes, estradiol or testosterone were administered for 4 weeks to ovarectomized or sham operated adult female rats pair-fed nutritionally adequate liquid diets containing either alcohol (36% of total calories) or isocal...

journal_title：Biochemical pharmacology

authors： Teschke R,Wannagat FJ,Löwendorf F,Strohmeyer G

更新日期：1986-02-01 00:00:00

abstract：:A nuclear envelope-associated epoxide hydrolase in mouse liver that hydrates trans-stilbene oxide has been identified and characterized. This epoxide hydrolase is distinct from the enzyme in nuclear envelopes that hydrates benzo[a]pyrene 4,5-oxide and other arene oxides. This distinction was demonstrated by the criter...

journal_title：Biochemical pharmacology

authors： Guenthner TM

更新日期：1986-10-01 00:00:00

abstract：:Indicators of mitochondrial function were studied in two different cell culture models of cis-diamminedichloroplatinum-II (CDDP) resistance: the intrinsically resistant human ovarian cancer cell line CI-80-13S, and resistant clones (HeLa-S1a and HeLa-S1b) generated by stable expression of the serine protease inhibitor...

journal_title：Biochemical pharmacology

authors： Dong Y,Berners-Price SJ,Thorburn DR,Antalis T,Dickinson J,Hurst T,Qiu L,Khoo SK,Parsons PG

更新日期：1997-06-01 00:00:00

abstract：:LLC-PK(1) is a proximal tubular cell line derived from normal pig kidney which has a structure and function similar to those of renal proximal tubular cells and which expresses baseline levels of P-glycoprotein. We isolated by drug selection a doxorubicin-resistant cell line (LLC-PK(1)/ADR) that exhibited a multidrug-...

journal_title：Biochemical pharmacology

authors： Decorti G,Rosati A,Candussio L,Giraldi T,Bartoli Klugmann F

更新日期：2001-01-01 00:00:00

abstract：:The release of the inflammatory mediators, prostaglandins (PGs), leukotrienes (LT) and lysosomal acid hydrolases (LAH), by macrophages is stimulated by endocytic stimuli such as zymosan. This process can be interfered with by specific inhibitors of phosphatidylcholine (PC) biosynthesis. The diphenylsulfone dapsone and...

journal_title：Biochemical pharmacology

authors： Bonney RJ,Wightman PD,Dahlgren ME,Sadowski SJ,Davies P,Jensen N,Lanza T,Humes JL

更新日期：1983-01-15 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：:A selected number of 1,3-diaminobenzo[f]quinazolines and 1,3-diamino-5,6-dihydrobenzo[f]quinazolines, which may be viewed as tricyclic analogues of the lipid-soluble antifolates pyrimethamine (PM), metoprine (DDMP), and etoprine (DDEP), were tested as inhibitors of purified dihydrofolate reductase (DHFR) from WI-L2 ly...

journal_title：Biochemical pharmacology

authors： Rosowsky A,Freisheim JH,Hynes JB,Queener SF,Bartlett M,Smith JW,Lazarus H,Modest EJ

更新日期：1989-08-15 00:00:00

abstract：:5-Lipoxygenase (5-LO) is a crucial enzyme of the arachidonic acid (AA) cascade and catalyzes the formation of bioactive leukotrienes (LTs) which are involved in inflammatory diseases and allergic reactions. The pathophysiological effects of LTs are considered to be prevented by 5-LO inhibitors. In this study we presen...

journal_title：Biochemical pharmacology

authors： Wisniewska JM,Rödl CB,Kahnt AS,Buscató El,Ulrich S,Tanrikulu Y,Achenbach J,Rörsch F,Grösch S,Schneider G,Cinatl J Jr,Proschak E,Steinhilber D,Hofmann B

更新日期：2012-01-15 00:00:00

abstract：:African trypanosomes, like Trypanosoma brucei, depend on antigenic variation to evade the immune response of the vertebrate host. An antigenic switch corresponds to the activation of a variable surface glycoprotein (VSG) gene from a large silent repertoire. Most switches require the duplicative transposition of a VSG ...

journal_title：Biochemical pharmacology

authors： Cornelissen AW,Michels PA,Borst P,Spanjer W,Versluijs-Broers JA,Van der Meer C,Farzaneh F,Shall S

更新日期：1985-12-01 00:00:00

abstract：:A cyclic nucleotide phosphodiesterase from guinea-pig heart is activated by calmodulin in the presence of calcium ions. Activation was measured over a range of calmodulin concentrations, and is antagonised by several tricyclic psychotropic drugs including trifluoperazine, imipramine, chlorpromazine and amitriptyline. ...

journal_title：Biochemical pharmacology

authors： Reynolds CH,Claxton PT

更新日期：1982-02-01 00:00:00

abstract：:This study demonstrates that the exposure of phenobarbitone-treated rats to halothane at an oxygen concentration of either 10% or 14% results in marked decreases in cytochrome P-450 content and aminopyrine demethylase activity in animals sacrificed from 1 to 48 hr post-exposure. The alterations observed in the hepatic...

journal_title：Biochemical pharmacology

authors： Knights KM,Gourlay GK,Cousins MJ

更新日期：1987-03-15 00:00:00

abstract：:N-Acylurea derivatives of albumin and transferrin prepared with the water-soluble carbodiimides N-ethyl-N'-(3-dimethylaminopropyl)carbodiimide and N-ethyl-N'-(3-trimethylpropylammonium)carbodiimide iodide have been found to bind different types of DNA. The two proteins were reacted with varying amounts of carbodiimide...

journal_title：Biochemical pharmacology

authors： Huckett B,Gordhan H,Hawtrey R,Moodley N,Ariatti M,Hawtrey A

更新日期：1986-04-15 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：:The effects of the transmembrane pH gradient (delta pH) and the transmembrane potential gradient (delta psi) on the uptake of several sympathomimetic amines were investigated, using bovine adrenal chromaffin granules isolated in isotonic sucrose. As previously described [R. Johnson and A. Scarpa, J. Biol. Chem. 254 37...

journal_title：Biochemical pharmacology

authors： Johnson RG,Carty SE,Hayflick S,Scarpa A

更新日期：1982-03-01 00:00:00