Enhancement of melphalan (L-PAM) toxicity by reductive metabolites of 1-methyl-2-nitroimidazole, a model nitroimidazole chemosensitizing agent.

abstract：:The inductive effects of phenobarbitone (PB) and 1,4-bis[2-(3,5-dichloropyridyloxy)]benzene (TCPOBOP) were compared in C57BL/6J mice. Induction parameters included six substrates: ethylmorphine (EM), benzphetamine (Bph), biphenyl, ethoxycoumarin (EtoC), pentoxyresorufin and dichloro-p-nitroanisole (DPNA). In order to ...

journal_title：Biochemical pharmacology

authors： Heubel F,Reuter T,Gerstner E

更新日期：1989-04-15 00:00:00

abstract：:Endothelins exert their physiological effects through interaction with cell surface receptors that are members of the G-protein-coupled receptor family. The endothelin receptor subtype B (ET(B) receptor) is abundantly expressed in rat cerebellum. Since agonist binding to G-protein-coupled receptors may be modulated by...

journal_title：Biochemical pharmacology

authors： Ceccarelli F,Giusti L,Bigini G,Costa B,Grillotti D,Fiumalbi E,Lucacchini A,Mazzoni MR

更新日期：2001-09-01 00:00:00

abstract：:Two resistant K562 sublines have been developed by treatment with AZQ (2,5-bis(carboethoxyamino)-3,6-diaziridinyl-1,4-benzoquinone) and BZQ (2,5-bis(2-hydroxyethylamino)-3,6-diaziridinyl-1,4-benzoquinone). The ID50 values of for AZQ on K562, the AZQ-resistant sublines (AZQR) and the BZQ-resistant sublines (BZQR) were ...

journal_title：Biochemical pharmacology

authors： Ward TH,Haran MS,Whittaker D,Watson AJ,Howard TD,Butler J

更新日期：1995-08-08 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：:We have previously reported that Gen-27, a newly synthesized flavonoid, exhibits anticancer effects against human colorectal cancer cells. In this study, we investigated the anticancer effects in human breast cancer cell lines and its underlying mechanisms. We demonstrated that Gen-27 inhibited the growth and prolifer...

journal_title：Biochemical pharmacology

authors： Tao L,Wei L,Liu Y,Ding Y,Liu X,Zhang X,Wang X,Yao Y,Lu J,Wang Q,Hu R

更新日期：2017-02-01 00:00:00

abstract：:Rat aortic smooth muscle cells in culture (A-10; ATCC CRL 1476) exhibited low levels of beta-adrenergic receptors as determined by specific binding of [125I]cyanopindolol ([125I]CYP) and marginal stimulation of adenylate cyclase in plasma membranes by (-)isoproterenol. When these cells were exposed to 5 mM sodium buty...

journal_title：Biochemical pharmacology

authors： Nambi P,Whitman MH,Schmidt DB,Heckman GD,Stassen FL,Crooke ST

更新日期：1986-11-01 00:00:00

abstract：:Angiogenesis, the development of neovessels from pre-existing vessels, is obligatory for solid tumors survival, growth, invasion, and metastasis. Many anti-angiogenic agents are small molecules originated from natural sources. Recently, angiosuppressive effects of indirubin and its derivatives, the active components i...

journal_title：Biochemical pharmacology

authors： Chan YK,Kwok HH,Chan LS,Leung KS,Shi J,Mak NK,Wong RN,Yue PY

更新日期：2012-03-01 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：:Exposure of lung tissue to Co(II) ions both in vivo and in vitro results in toxicity, a relatively early event of which is the oxidation of cellular glutathione. In this study we have attempted to delineate the relationship between this oxidation of glutathione and the subsequent development of cellular dysfunction. S...

journal_title：Biochemical pharmacology

authors： Lewis CP,Demedts M,Nemery B

更新日期：1992-02-04 00:00:00

abstract：:The in vitro inhibition of the cytochrome P-450 (P-450) isozyme specific positional hydroxylation of androst-4-ene-3,17-dione (androstenedione) by the alkylamino containing compounds trans- and cis-tamoxifen, 4-hydroxytamoxifen, N-desmethyltamoxifen, SKF 525-A and the non-alkylamino containing compounds tamoxifen meta...

journal_title：Biochemical pharmacology

authors： Reidy GF,Murray M

更新日期：1989-01-01 00:00:00

abstract：:The metabolism of alpha,alpha,beta,beta- tetradeutero -N,N -dimethyltryptamine ( D4DMT ) in rat brain in vivo as a function of time and dose was examined. Quantification of D4DMT and its respective deutero-metabolites was accomplished using gas chromatographic/mass spectrometric/selected ion monitoring/isotope dilutio...

journal_title：Biochemical pharmacology

authors： Barker SA,Beaton JM,Christian ST,Monti JA,Morris PE

更新日期：1984-05-01 00:00:00

abstract：:Inflammatory cytokines and human immunodeficiency virus type 1 (HIV-1) gp120 are considered to play an important role in the pathogenesis of HIV-1-associated CNS disorders. These substances are produced predominantly by HIV-1-infected or activated macrophages and microglia in the brain and induce neural cell death. Ce...

journal_title：Biochemical pharmacology

authors： Okamoto M,Ono M,Baba M

更新日期：2001-09-15 00:00:00

abstract：:A large variety of 5-substituted 2'deoxyuridines (dUrds) and 2'-deoxyuridylates (dUMPs) have been evaluated for their inhibitory effects on the thymidine (dThd) kinase or thymidylate (dTMP) synthetase isolated from mouse leukemia L1210 cells. The most potent inhibitors of dThd kinase were 5-chloro-, 5-bromo- and 5-iod...

journal_title：Biochemical pharmacology

authors： Balzarini J,De Clercq E,Mertes MP,Shugar D,Torrence PF

更新日期：1982-11-15 00:00:00

abstract：:In the present study, the distribution and nature of esterases in the rat which hydrolysed fluazifop-butyl, carbaryl, paraoxon and phenylacetate were investigated. Vmax and Km values for the hydrolysis reactions were determined. Fluazifop-butyl was hydrolysed to fluazifop by rat liver (Vmax mumol/min/g microsomes 6.2 ...

journal_title：Biochemical pharmacology

authors： McCracken NW,Blain PG,Williams FM

更新日期：1993-01-07 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：:A series of trifluoromethanesulfonamides (TFMS) was synthesized and tested for uncoupling activity in rat liver mitochondria. With succinate as the mitochondrial substrate, and the respiratory control index (RCI) as an indicator of their uncoupling ability, we found that all of the TFMS tested were uncouplers of oxida...

journal_title：Biochemical pharmacology

authors： McCracken RO,Carr AW,Stillwell WH,Lipkowitz KB,Boisvenue R,O'Doherty GO,Wickiser DI

更新日期：1993-05-05 00:00:00

abstract：:Characteristics of erythromycin binding to Staphylococcus aureus were determined by using kinetics and equilibrium binding experiments. Both methods yielded identical values of the dissociation constant, i.e. 0.1 muM. This value was in accord with that found with a bacterial extract of ribosomes which are the organell...

journal_title：Biochemical pharmacology

authors： Barre J,Fournet MP,Zini R,Deforges L,Duval J,Tillement JP

更新日期：1986-03-15 00:00:00

abstract：:The 2-haloethylnitrosoureas have been shown to form the cross-linked structure 1-(3-cytosinyl),2-(1-guanyl)ethane in DNA. This cross-link has now been synthesized by the reaction of O6-(2-fluoroethyl)guanosine with deoxycytidine in dimethyl sulfoxide followed by removal of the sugars by acid hydrolysis. This synthetic...

journal_title：Biochemical pharmacology

authors： MacFarland JG,Kirk MC,Ludlum DB

更新日期：1990-01-01 00:00:00

abstract：:Since ginsenoside-Rg(3), one of the panaxadiol saponins isolated from the ginseng root, significantly inhibited the secretion of catecholamines from bovine adrenal chromaffin cells stimulated by acetylcholine (ACh), the properties of ginsenoside-Rg(3) inhibition were investigated. Although ginsenoside-Rg(3) inhibited ...

journal_title：Biochemical pharmacology

authors： Tachikawa E,Kudo K,Nunokawa M,Kashimoto T,Takahashi E,Kitagawa S

更新日期：2001-10-01 00:00:00

abstract：:Phentermine was shown in the 1970s to inhibit the metabolism of serotonin by monoamine oxidase (MAO), but never was labeled as an MAO inhibitor; hence, it was widely used in combination with fenfluramine, and continues to be used, in violation of their labels, with other serotonin uptake blockers. We examined the effe...

journal_title：Biochemical pharmacology

authors： Ulus IH,Maher TJ,Wurtman RJ

更新日期：2000-06-15 00:00:00

abstract：:To derive structure/function relationships for muscarinic receptor/G-protein coupling, the m2 and m5 muscarinic receptors and a series of m2/m5 chimeras were tested for agonist binding and functional responses in a cellular proliferation/transformation assay. m5, which mediates stimulation of phosphatidylinositol turn...

journal_title：Biochemical pharmacology

authors： Burstein ES,Spalding TA,Brann MR

更新日期：1996-02-23 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：:Cathepsin K is a cysteine protease that degrades type I human collagen during bone resorption. We have expressed the recombinant human cathepsin K in Chinese hamster ovary (CHO) cells as a pre-proenzyme and demonstrated that it is processed intracellularly to an active enzyme form and that only the proenzyme form is s...

journal_title：Biochemical pharmacology

authors： Claveau D,Riendeau D,Mancini JA

更新日期：2000-09-15 00:00:00

abstract：:Adriamycin (ADR), a well-known antitumoral drug, interacts with DNA (nuclear and mitochondrial) and cardiolipin. Moreover, ADR induces numerous mitochondrial modifications in sensitive cells. However, no results have yet been obtained as to the repercussions of drug effects on oxido-reductase activities in ADR-resista...

journal_title：Biochemical pharmacology

authors： Denis-Gay M,Petit JM,Mazat JP,Ratinaud MH

更新日期：1998-08-15 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：:The mechanism by which p-chlorophenoxyisobutyric acid (clofibric acid) induces striking changes in the proportion of the molecular species of phosphatidylcholine (PC) in rat liver was studied. Treatment of rats with clofibric acid strikingly increased the content of 1-palmitoyl-2-oleoyl (16:0-18:1) PC, but decreased t...

journal_title：Biochemical pharmacology

authors： Mizuguchi H,Kudo N,Kawashima Y

更新日期：2001-10-01 00:00:00

abstract：:Common marmosets (Callithrix jacchus) are potentially useful nonhuman primate models for preclinical studies. An anti-inflammatory drug, diclofenac is reportedly metabolized mainly by human cytochrome P450 (P450) 2C9 to 4'-hydroxydiclofenac and minorly by P450 3A4 to 5-hydroxydiclofenac that leads to reactive intermed...

journal_title：Biochemical pharmacology

authors： Nakanishi K,Uehara S,Kusama T,Inoue T,Shimura K,Kamiya Y,Murayama N,Shimizu M,Uno Y,Sasaki E,Yamazaki H

更新日期：2018-06-01 00:00:00

abstract：:Genistein, a natural isoflavone phytoestrogen present in soybeans, has been extensively studied as a chemopreventive or therapeutic agent in several types of cancer. The traditional Asian diet is rich in soy products may explain in part why the incidence of breast cancer in Asian women is relatively low. To improve th...

journal_title：Biochemical pharmacology

authors： Liao CH,Pan SL,Guh JH,Teng CM

更新日期：2004-06-01 00:00:00

abstract：:Toll-like receptors (TLRs) are key components of the innate immune system, functioning as pattern recognition receptors that recognise a wide range of microbial pathogens. TLRs represent a primary line of defence against invading pathogens in mammals, plants and insects. Recognition of microbial components by TLRs tri...

journal_title：Biochemical pharmacology

authors： Doyle SL,O'Neill LA

更新日期：2006-10-30 00:00:00

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