Impairment of bromosulfophthalein hepatic transport and cholestasis induced by diethyl maleate in the rabbit.

abstract：:Resealed synaptic plasma membrane vesicles exhibit Na+-dependent Ca2+ transport activity which may participate in regulation of free Ca2+ concentrations in nerve endings. Sodium chloride-loaded vesicles took up Ca2+ from the external medium (150 mM KCl-25 mM Tris/HCl) in the presence of an outward-directed Na+ gradien...

journal_title：Biochemical pharmacology

authors： Michaelis ML,Michaelis EK

更新日期：1983-03-15 00:00:00

abstract：:4'-Deoxydoxorubicin (4'-deoxy) is a new adriamycin analogue with a similar spectrum of antitumour activity but is significantly more lipophilic than the parent compound. We report the kinetics and uptake of the two drugs by human non-small cell lung tumour cells in monolayer culture and the relationship between intrac...

journal_title：Biochemical pharmacology

authors： Kerr DJ,Kerr AM,Freshney RI,Kaye SB

更新日期：1986-08-15 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：:The effect of the adenosine deaminase (ADA) inhibitor 2'-deoxycoformycin (dCF) on the development of insulin-dependent diabetes mellitus (IDDM) was assessed in the BB Wistar rat. Sixty-one male rats were treated from days 30 to 120 with 0, 0.5, 1.0 or 1.5 mg dCF/kg/week. The incidence of IDDM was 78% in the controls a...

journal_title：Biochemical pharmacology

authors： Thliveris JA,Begleiter A,Kobrinsky NL,Verburg L,Dean HJ,Johnston JB

更新日期：1993-09-14 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：:The importance of polyglutamation for the activation of natural folates and classical antifolates and recent evidence for the role of dietary folate as a biochemical modulator of antifolate efficacy led us to investigate the influence of changes in dietary folate on folylpolyglutamate synthetase (FPGS) activity. Activ...

journal_title：Biochemical pharmacology

authors： Gates SB,Worzalla JF,Shih C,Grindey GB,Mendelsohn LG

更新日期：1996-11-08 00:00:00

abstract：:The spontaneous autoxidation of the neurotoxin 6-hydroxydopamine proceeds by a free radical chain reaction involving the superoxide anion radical and produces the corresponding chromogen 6-hydroxydopamine quinone and hydrogen peroxide. The rate of this reaction is increased in the presence of ceruloplasmin and peroxid...

journal_title：Biochemical pharmacology

authors： Padiglia A,Medda R,Lorrai A,Biggio G,Sanna E,Floris G

更新日期：1997-04-25 00:00:00

abstract：:Anti-idiotypic antibodies which recognize the opiate receptor were generated in guinea pigs following immunization against purified rabbit anti-morphine antibodies. The anti-idiotypic antibodies produced a concentration-dependent inhibition of [3H]naloxone binding to opiate receptors in a membranous mouse brain prepar...

journal_title：Biochemical pharmacology

authors： Ng DS,Isom GE

更新日期：1985-08-15 00:00:00

abstract：:Rat liver microsomes and purified NADPH-cytochrome c reductase metabolized [14C]misonidazole anaerobically to a reactive intermediate that covalently binds to tissue macromolecules. Air strongly inhibited the binding whereas carbon monoxide had no effect, indicating that misonidazole is activated via reduction and not...

journal_title：Biochemical pharmacology

authors： McManus ME,Lang MA,Stuart K,Strong J

更新日期：1982-02-15 00:00:00

abstract：:The cytotoxicity anti-tumour intercalating agents such as the anthraquinone mitoxantrone is thought to relate to DNA binding and the trapping of DNA topoisomerase II complexes on cellular DNA. We have studied the uptake, nuclear location, DNA binding mode and DNA damaging capacity of mitoxantrone in a small cell lung ...

journal_title：Biochemical pharmacology

authors： Smith PJ,Morgan SA,Fox ME,Watson JV

更新日期：1990-11-01 00:00:00

abstract：:9-(2-Phosphonylmethoxyethyl)-N6-cyclopropyl-2,6-diaminopurine (cpr-PMEDAP) is an acyclic nucleotide analog of the [9-(2-phosphonylmethoxyethyl)-] (PME) series containing a cyclopropyl substituent on the N6 position of the 2,6-diaminopurine (DAP) base. Growth inhibition assays in a broad range of tumor cell lines demon...

journal_title：Biochemical pharmacology

authors： Compton ML,Toole JJ,Paborsky LR

更新日期：1999-08-15 00:00:00

abstract：:Chronic blockade of nitric oxide (NO) synthesis attenuates the eosinophil infiltration into airways of allergic rats. This study was designed to investigate whether the inhibition of eosinophil influx to the lung of allergic rats reflects modifications in the pattern of cell mobilization from the bone marrow to periph...

journal_title：Biochemical pharmacology

authors： Ferreira HH,Costa RA,Jacheta JM,Martins AR,Medeiros MV,Macedo-Soares MF,De Luca IM,Antunes E,De Nucci G

更新日期：2004-08-15 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：:Adipogenesis plays a central role in obesity development. The processes of adipogenesis include migration, adhesion, proliferation and survival of preadipocytes and differentiation to mature adipocytes. Many of these biological functions are related to integrins. Here, we found that snake venom-derived arginine-glycin...

journal_title：Biochemical pharmacology

authors： Lin YT,Tang CH,Chuang WJ,Wang SM,Huang TF,Fu WM

更新日期：2005-11-15 00:00:00

abstract：:Alpha2-adrenoceptor agents as well as stress affect the activity of several hepatic monoxygenases including those related to CYP1A enzymes. This study was therefore designed to assess the role of central and/or peripheral catecholamines and, in particular, of adrenoceptors in the regulation of B(alpha)P-induced cytoch...

journal_title：Biochemical pharmacology

authors： Konstandi M,Kostakis D,Harkitis P,Marselos M,Johnson EO,Adamidis K,Lang MA

更新日期：2005-01-15 00:00:00

abstract：:The antiinflammatory drug ebselen (2-phenyl-1,2-benzisoselenazo-3(2H)-one) is known to bind covalently to thiols to form seleno disulfides that, directly or indirectly, are responsible for its pharmacological effects. Due to its reactive thiol group and high plasma concentration, albumin is a preferred target of ebsel...

journal_title：Biochemical pharmacology

authors： Ullrich V,Weber P,Meisch F,von Appen F

更新日期：1996-07-12 00:00:00

abstract：:The capacity of cultured bovine adrenal medullary cells to metabolize and export cyclic AMP has been studied. Basal cellular cyclic AMP levels were increased 50% by 100 microM 3-isobutyl-1-methylxanthine (IBMX) and rolipram, a class IV (cyclic AMP-specific) phosphodiesterase (PDE) inhibitor. They were not affected by ...

journal_title：Biochemical pharmacology

authors： Marley PD,Thomson KA

更新日期：1992-12-01 00:00:00

abstract：:The objective of this Commentary is to help clarify and illustrate what prodrugs are, what they are not, which benefits they can offer, and what their limits are. To this end, a number of criteria of classification and evaluation are presented. This is followed by a discussion of the pharmaceutical, pharmacokinetic an...

journal_title：Biochemical pharmacology

authors： Testa B

更新日期：2004-12-01 00:00:00

abstract：:The aldo-keto reductases (AKRs) represent a growing oxidoreductase superfamily. Forty proteins have been identified and characterized as AKRs, and an additional fourteen genes may encode proteins related to the superfamily. Found in eukaryotes and prokaryotes, the AKRs metabolize a wide range of substrates, including ...

journal_title：Biochemical pharmacology

authors： Jez JM,Flynn TG,Penning TM

更新日期：1997-09-15 00:00:00

abstract：:We studied whether gemfibrozil and clofibric acid alter isoprenoid lipid synthesis in rat hepatocytes. After incubation of the cells with the agent for 74 hr, [(14)C]acetate or [(3)H]mevalonate was added, and the cells were further incubated for 4 hr. Gemfibrozil and clofibric acid increased ubiquinone synthesis from ...

journal_title：Biochemical pharmacology

authors： Hashimoto F,Taira S,Hayashi H

更新日期：2000-05-15 00:00:00

abstract：:Chronic oral phenobarbital treatment (50 mg/kg every 12 hr for 8 weeks), which was nontoxic and continuously protective against seizures in rats, significantly decreased folate concentration in liver (29%) but not in brain or plasma. The apparent activity of 5,10-methylenetetrahydrofolate reductase (MTR) in liver decr...

journal_title：Biochemical pharmacology

authors： Carl GF,Smith DB

更新日期：1984-11-01 00:00:00

abstract：:The cysteine (Cys) precursor 2(RS)-n-propylthiazolidine-4(R)-carboxylic acid (PTCA) has been shown to protect against acetaminophen (APAP)-induced hepatic GSH, GSSG, and Cys depletion and hepatic necrosis. The aim of this study was to determine the effects of PTCA on the concentrations of sulfhydryl compounds in extra...

journal_title：Biochemical pharmacology

authors： Srinivasan C,Williams WM,Nagasawa HT,Chen TS

更新日期：2001-04-01 00:00:00

abstract：:The immunosuppressive and cytostatic agent 15-deoxyspergualin (DSG) binds to the Hsc70 class of molecular chaperones with a K(D) = 4 microM. Because Hsc70s represent a diverse group of cellular effectors and because Hsc70 function frequently requires a DnaJ molecular chaperone, the specificity of DSG for different Hsc...

journal_title：Biochemical pharmacology

authors： Brodsky JL

更新日期：1999-04-15 00:00:00

abstract：:Compounds of the mevalonate pathway containing a terminal di- or triphosphate (mev-PP or mev-PPP) were tested as substrates of several enzyme ligases (T4 RNA ligase, T4 DNA ligase, firefly luciferase and other ligases) for the synthesis of ATP derivatives of the mev-pppA or mev-ppppA type. T4 RNA ligase, in the presen...

journal_title：Biochemical pharmacology

authors： Sillero MA,de Diego A,Tavares JE,Silva JA,Pérez-Zúñiga FJ,Sillero A

更新日期：2009-08-15 00:00:00

abstract：:The salt-induced condensation of chromatin has been studied with flow-linear dichroism technique using an intercalative dye (methylene blue) to selectively monitor the linker orientation. At low ionic strength both linkers and chromatosomes (with their flat faces) are oriented preferentially parallel to the chromatin ...

journal_title：Biochemical pharmacology

authors： Kubista M,Nielsen PE,Nordén B

更新日期：1988-05-01 00:00:00

abstract：:We examined the tyrosine kinase inhibitor erbstatin and several derivatives for their ability to inhibit serine/threonine protein kinases in vitro. Erbstatin was found to inhibit protein kinase C (PKC) with an IC50 of 19.8 +/- 3.2 microM. A trihydroxy derivative of erbstatin inhibited PKC with similar potency, whereas...

journal_title：Biochemical pharmacology

authors： Bishop WR,Petrin J,Wang L,Ramesh U,Doll RJ

更新日期：1990-11-01 00:00:00

abstract：:Inflammation, especially chronic inflammation, is directly involvement in the pathogenesis of many diseases including cancer. An effective approach for managing inflammation is to employ chemicals to block activation of nuclear factor-κB (NF-κB), a key regulator for inflammatory processes. Piperlongumine (piplartine, ...

journal_title：Biochemical pharmacology

authors： Sun LD,Wang F,Dai F,Wang YH,Lin D,Zhou B

更新日期：2015-06-01 00:00:00

abstract：:The possible role of fluroacetate in the toxicity and antitumour activity of the fluroethylnitrosoureas, BFNU and FCNU has been studied in CBA mice bearing the TLX5 lymphoma either sensitive (TLXS) or resistant (TLXRT) to nitrosoureas. Treatment of mice bearing either TLXS or TLXRT tumours with either BFNU or FCNU cau...

journal_title：Biochemical pharmacology

authors： Tisdale MJ,Brennan RA

更新日期：1985-09-15 00:00:00

abstract：:Treatment of immature 21-day-old female Sprague-Dawley rats with 17 beta-estradiol (E2) (0.5 microgram/rat) caused a significant increase in uterine wet weight, DNA synthesis, progesterone receptor (PR) binding, and peroxidase activity. At doses as high as 40 mg/rat, the bioflavonoid naringenin did not cause a signifi...

journal_title：Biochemical pharmacology

authors： Ruh MF,Zacharewski T,Connor K,Howell J,Chen I,Safe S

更新日期：1995-10-26 00:00:00

abstract：:When INH was administered orally or intraperitoneally to pregnant female mice, the concentrations of acetyl INH and acetyl hydrazines did not vary significantly in circulating blood and in amniotic fluid. However, the concentration of INH in the amniotic fluid was significantly higher than that observed in the serum. ...

journal_title：Biochemical pharmacology

authors： Menon MM,Bhide SV

更新日期：1983-02-15 00:00:00