abstract：:A form of cytochrome P-450, P-450-D3, cross reactive with antibodies to rat P-450d was purified from liver microsomes of polychlorinated biphenyl (PCB)-treated female Beagle dogs to an electrophoretic homogeneity. Judging from the result of sodium dodecylsulfate-polyacrylamide gel electrophoresis (SDS-PAGE), the molec...

journal_title：Biochemical pharmacology

authors： Ohta K,Motoya M,Komori M,Miura T,Kitada M,Kamataki T

更新日期：1989-01-01 00:00:00

abstract：:The cellular localization of vascular plasma membrane aminopeptidase M (AmM; EC3.4.11.2) was examined in cultured porcine aorta endothelium and smooth muscle cells. AmM was 14-fold higher on smooth muscle (117 +/- 16 units/mg) than on endothelium (8.4 +/- 0.2). Proportional to its cellular distribution, AmM hydrolyzed...

journal_title：Biochemical pharmacology

authors： Palmieri FE,Bausback HH,Ward PE

更新日期：1989-01-01 00:00:00

abstract：:The nonspecies specific immunosuppressive and anti-inflammatory properties of a major protein (SV-IV) secreted from the epithelium of rat seminal vesicles (SV) are described. To detect the immunosuppressive effect, peripheral blood lymphocytes (PBL) were pretreated for 2 hr at 37 degrees with SV-IV, and the protein wa...

journal_title：Biochemical pharmacology

authors： Metafora S,Peluso G,Persico P,Ravagnan G,Esposito C,Porta R

更新日期：1989-01-01 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：:Sulphate conjugation was investigated using extracts of human foetal liver cells in culture. The three reactions which are involved in sulphate conjugation were measured singly or in combination: they are (i) the PAPS generation catalyzed by ATP-sulphurylase and adenosine 5'-phosphosulphate (APS)-kinase, (ii) the phen...

journal_title：Biochemical pharmacology

authors： Tan TM,Sit KH,Wong KP

更新日期：1988-12-15 00:00:00

abstract：:The biotransformation and the hepato- and nephrotoxicity of the mercapturic acids (N-acetyl-1-cysteine S-conjugates) of three structurally related 2,2-difluoroethylenes were investigated in vivo in the rat. All mercapturic acids appeared to cause nephrotoxicity, without any measureable effect on the liver. The mercapt...

journal_title：Biochemical pharmacology

authors： Commandeur JN,Brakenhoff JP,De Kanter FJ,Vermeulen NP

更新日期：1988-12-01 00:00:00

abstract：:The effects of thiamine thiazolone (TT) and thiamine thiazolone pyrophosphate (TTPP) on the in vitro and in vivo inhibition of pyruvate dehydrogenase complex (PDHC) from rat cortex and hippocampus were characterized. TTPP decreased PDHC activity in vitro but had no effect in vivo following its direct chronic administr...

journal_title：Biochemical pharmacology

authors： Kandiko CT,Smith D,Yamamoto BK

更新日期：1988-11-15 00:00:00

abstract：:The formation, retention and biological activity of the polyglutamate metabolites of the thymidylate synthase (TS) inhibitor N10-propargyl-5,8-dideazafolic acid (CB3717) has been investigated in L1210 murine leukaemia cells grown in vitro. CB3717 polyglutamates were measured by HPLC using high specific activity 3H-CB3...

journal_title：Biochemical pharmacology

authors： Sikora E,Jackman AL,Newell DR,Calvert AH

更新日期：1988-11-01 00:00:00

abstract：:The intraperitoneal injection of methylglyoxal bis(cyclohexylamidinohydrazone) (MGBC), an inhibitor of S-adenosylmethionine decarboxylase and spermidine synthase, markedly increased (7-fold of the basal level at 4 hr) ornithine decarboxylase (ODC) activity in normal mouse liver. ODC activity was also increased 2.5-fol...

journal_title：Biochemical pharmacology

authors： Hibasami H,Maekawa S,Murata T,Nakashima K

更新日期：1988-11-01 00:00:00

abstract：:The effect of ethanol abuse on the lipid ordering of the human erythrocyte membranes was studied by steady-state and time-resolved fluorescence anisotropy measurements of DPH and its polar analogue TMA-DPH, which probe different membrane regions. Steady-state anisotropy values with DPH as a probe were slightly but sig...

journal_title：Biochemical pharmacology

authors： Beaugé F,Gallay J,Stibler H,Borg S

更新日期：1988-10-15 00:00:00

abstract：:Human immunodeficiency virus type 1 (HIV-1) gene expression is modulated by some virus-encoded proteins, possibly acting at multiple levels of control, which are also known to be involved in the regulation of gene expression in uninfected cells (transcriptional, post-transcriptional, nucleocytoplasmic transport, and t...

journal_title：Biochemical pharmacology

authors： Schröder HC,Sarin PS,Rottmann M,Wenger R,Maidhof A,Renneisen K,Müller WE

更新日期：1988-10-15 00:00:00

abstract：:The interaction of the anti-tumor anthraquinones, ametantrone and mitoxantrone, with rat hepatic microsomes has been studied with a fluorescence technique using 7,12-dimethylbenzanthracene as a new fluorescent probe. The two drugs were able to quench the intrinsic fluorescence of microsomal suspension. Mitoxantrone wa...

journal_title：Biochemical pharmacology

authors： al-Gailany KA,Alwan AH

更新日期：1988-10-15 00:00:00

abstract：:Adenosine potentiates mouse bone marrow-derived mast cell mediator release by a mechanism that appears to involve cell surface adenosine receptors. In an attempt to explore possible interactions between G proteins and adenosine receptors, mast cells were incubated with activated pertussis toxin, an agent that ADP-ribo...

journal_title：Biochemical pharmacology

authors： Marquardt DL,Walker LL

更新日期：1988-10-15 00:00:00

abstract：:The actions of alkylating pindolol (N8-bromoacetyl-N1-3'-(4-indolyloxy)-2'-hydroxypropyl[z]-1,8- diamino-p-menthane; BIM) have been examined on beta-adrenoceptors in guinea-pig left atria and trachea. In organ bath experiments, addition of BIM (greater than or equal to 0.1 microM), followed by washout, produced concen...

journal_title：Biochemical pharmacology

authors： Molenaar P,Russell F,Pitha J,Summers R

更新日期：1988-10-01 00:00:00

abstract：:Benzbromarone, a potent uricosuric agent, inhibited allantoin production in isolated hepatocytes at concentrations half to ten times greater than therapeutic plasma levels of the drug. In addition, the drug at these concentrations also markedly inhibited xanthine oxidase (EC 1.2.1.37), an enzyme involved in the regula...

journal_title：Biochemical pharmacology

authors： Rodilla F,Sanchez-Beltran MJ,Izquierdo R,Gomez-Ruiz MD,Cabo J

更新日期：1988-10-01 00:00:00

abstract：:We have studied the effect of low sulfate concentrations on the glycosaminoglycan synthesis in rat patellar cartilage in vivo as well as in vitro. The oral administration of 200 mg/kg paracetamol to male Wistar rats resulted in a significant reduction of the serum sulfate concentration. Reduced serum sulfate availabil...

journal_title：Biochemical pharmacology

authors： van der Kraan PM,de Vries BJ,Vitters EL,van den Berg WB,van de Putte LB

更新日期：1988-10-01 00:00:00

abstract：:The effect of naturally occurring aliphatic carboxylic acid n-butyrate on total and type-specific synthesis of sulfated proteoglycans and hyaluronic acid by rat liver fat-storing cells (Ito cells, vitamin A-storing cells), the main connective tissue producing cell type in liver, was studied. Concentrations of n-butyra...

journal_title：Biochemical pharmacology

authors： Gressner AM,Haarmann R

更新日期：1988-10-01 00:00:00

abstract：:We have studied the effects of the recently reported two new metabolites of the antitumor agent VP-16-213, the ortho-dihydroxy derivative or catechol and the ortho-quinone, on the biological activity of single-stranded and double-stranded phi X174 DNA, the binding of the metabolites to calf thymus DNA and the conversi...

journal_title：Biochemical pharmacology

authors： van Maanen JM,Lafleur MV,Mans DR,van den Akker E,de Ruiter C,Kootstra PR,Pappie D,de Vries J,Retèl J,Pinedo HM

更新日期：1988-10-01 00:00:00

abstract：:The cytotoxic effects of 10 mM acetaminophen (APAP) in primary cultures of non-induced mouse hepatocytes are accompanied by depletion of intracellular glutathione (GSH), arylation of protein, and loss of protein sulfhydryl (PSH) groups. Investigation of the stoichiometry of the covalent binding and PSH loss after APAP...

journal_title：Biochemical pharmacology

authors： Birge RB,Bartolone JB,Nishanian EV,Bruno MK,Mangold JB,Cohen SD,Khairallah EA

更新日期：1988-09-15 00:00:00

abstract：:Regenerating liver from partial hepatectomy (HPX) is known to exhibit a strong and transient deficiency in both spectrally detectable microsomal cytochrome P-450 (P-450) and related monooxygenase activities. Male Wistar rats (250-300 g) were HPX or sham operated and liver was excised at different times after operation...

journal_title：Biochemical pharmacology

authors： Marie IJ,Dalet C,Blanchard JM,Astre C,Szawlowski A,Saint Aubert B,Joyeux H,Maurel P

更新日期：1988-09-15 00:00:00

abstract：:In the past few years, substantial advances have been made in analyzing the structure and function of the GABA receptor-gated Cl- channel. A major goal is to identify the molecular characteristics of the GABAA receptor that are necessary for maintaining normal GABAergic neurotransmission. Future studies will undoubted...

journal_title：Biochemical pharmacology

authors： Schwartz RD

更新日期：1988-09-15 00:00:00

abstract：:Two antitumor antibiotics doxorubicin and daunorubicin were tested for their ability to influence the activation of protein kinase C in human platelets. Daunorubicin was found to inhibit the phosphorylation of the 40 K PKC substrate induced by thrombin and 12-O-tetradecanoyl-phorbol-13-acetate as well as the phosphory...

journal_title：Biochemical pharmacology

authors： Lanzi C,Banfi P,Ravagnani F,Gambetta RA

更新日期：1988-09-15 00:00:00

abstract：:Previous studies of platinum(II) compounds with bidentate leaving ligands have emphasized the contrast between the stability of the bidentate leaving ligand in vitro (T1/2 greater than 11 days in water) and the apparent reactivity of these bidentate platinum compounds in vivo. However, none of these studies actually m...

journal_title：Biochemical pharmacology

authors： Mauldin SK,Plescia M,Richard FA,Wyrick SD,Voyksner RD,Chaney SG

更新日期：1988-09-01 00:00:00

abstract：:DUP 785 (NSC 368390; Brequinar sodium) is a new inhibitor of pyrimidine de novo biosynthesis with antitumor activity against several experimental tumors. DUP 785 inhibits the mitochondrial enzyme dihydroorotate dehydrogenase, blocking the conversion of dihydroorotate to orotate. We examined the influence of exposure t...

journal_title：Biochemical pharmacology

authors： Schwartsmann G,Peters GJ,Laurensse E,de Waal FC,Loonen AH,Leyva A,Pinedo HM

更新日期：1988-09-01 00:00:00

abstract：:An enzyme (NADPH-dependent diaphorase) present in rat brain microsomes has been solubilised and shown to utilise both nitrobluetetrazolium and cytochrome c as electron acceptors, when reduced by NADPH. The kinetics of the enzyme have been determined using cytochrome c (Km = 1.3 microM), NADPH (Km = 1.4 microM) and the...

journal_title：Biochemical pharmacology

authors： Kemp MC,Kuonen DR,Sutton A,Roberts PJ

更新日期：1988-08-15 00:00:00

abstract：:The present study was carried out to analyze the sex differences in the retention of Cd in rats treated with a small amount of Cd, and its mechanisms. Cd and Zn concentrations in the kidney and liver of female rats treated with 28 nmol Cd or 1 nmole Zn were significantly higher than those in male rats. Pretreatment wi...

journal_title：Biochemical pharmacology

authors： Nishiyama S,Onosaka S,Taguchi T,Konishi Y,Tanaka K,Kinebuchi H

更新日期：1988-08-15 00:00:00

abstract：:The relationship between DNA crosslinks and cell death as a result of exposure to melphalan (MLN) was studied in the F1 variant of B16 melanoma cells. The formation of DNA crosslinks is believed to represent the lethal lesion following exposure of cells to bifunctional alkylating agents. The production of DNA crosslin...

journal_title：Biochemical pharmacology

authors： Garcia ST,McQuillan A,Panasci L

更新日期：1988-08-15 00:00:00

abstract：:Glipentide, a second generation sulfonylurea, raised the cellular concentration of fructose 2,6-bisphosphate in isolated rat hepatocytes. Parallel to accumulating this regulatory metabolite, glipentide inhibited basal gluconeogenesis and increased the rate of L-lactate production, as well as the metabolic flux through...

journal_title：Biochemical pharmacology

authors： López-Alarcón L,Berbil-Bautista PR,Guijarro C,Felíu JE

更新日期：1988-08-15 00:00:00

abstract：:The binding of indapamide to isolated serum proteins and erythrocytes was studied in order to understand its blood distribution. In serum, indapamide was mainly bound to alpha 1-acid glycoprotein with a high affinity (K = 73.4/mM), and to albumin and lipoproteins. Indapamide was bound to erythrocytes via a saturable p...

journal_title：Biochemical pharmacology

authors： Urien S,Riant P,Renouard A,Coulomb B,Rocher I,Tillement JP

更新日期：1988-08-01 00:00:00

abstract：:The 3'-fluoro-and 3'-azido-substituted derivatives of 2',3'-dideoxythymidine (ddThd), 2',3'-dideoxyuridine (ddUrd), 2',3'-dideoxy-5-ethyluridine (ddEtUrd) and 2',3'-dideoxycytidine (ddCyd) have been synthesized and evaluated for their anti-retrovirus activity [against human immunodeficiency virus (HIV) and murine Molo...

journal_title：Biochemical pharmacology

authors： Balzarini J,Baba M,Pauwels R,Herdewijn P,De Clerq E

更新日期：1988-07-15 00:00:00

abstract：:The effect of histamine on the release of endogenous noradrenaline and 5-hydroxytryptamine (5-HT) has been examined in slices of rat cerebral cortex. Histamine was found to produce a marked release of both amines from rat cerebral cortex at concentrations between 0.1 and 1 mM. This response to histamine was relatively...

journal_title：Biochemical pharmacology

authors： Young CS,Mason R,Hill SJ

更新日期：1988-07-15 00:00:00

abstract：:We have investigated the redox behavior of a series of structurally related flavonoids employing cyclic voltammetry under physiological conditions. The flavonoids that auto-oxidized and produced oxygen radicals had oxidation potentials (E 1/2) significantly lower [-30 to +60 mV vs (SCE)] than those that did not underg...

journal_title：Biochemical pharmacology

authors： Hodnick WF,Milosavljević EB,Nelson JH,Pardini RS

更新日期：1988-07-01 00:00:00

abstract：:Suramin, a drug intensively used in the chemotherapy of African trypanosomiasis and onchocerciasis, is currently being tested in clinical trials for AIDS treatment. Its effects on mitochondrial energy metabolism in mammals were studied. At low concentrations it inhibited ATP synthesis and ATPase activity in submitocho...

journal_title：Biochemical pharmacology

authors： Calcaterra NB,Vicario LR,Roveri OA

更新日期：1988-07-01 00:00:00

abstract：:MOLT-4 (T-), RAJI (B-), and KM-3 (non-B-non-T-, common ALL) malignant lymphoblasts demonstrated significant differences in their activities of purine de novo synthesis (PDNS) and purine salvage pathway and in their cell-kinetic parameters. Incubations with concentrations of methotrexate (0.02 and 0.2 microM), which ca...

journal_title：Biochemical pharmacology

authors： Bökkerink JP,De Abreu RA,Bakker MA,Hulscher TW,van Baal JM,Schretlen ED,De Bruijn CH

更新日期：1988-06-15 00:00:00

abstract：:Casein-elicited mouse peritoneal macrophages cultured in the presence of phorbol 12-myristate 13-acetate (PMA) express u-PA. Induction is maximal after 4 hr of stimulation and u-PA activity is mainly recovered with the membrane fraction of the cellular lysate. This enzymatic activity is inhibited by isopropylmethylpho...

journal_title：Biochemical pharmacology

authors： Dubois P,Lison D,Lauwerys R

更新日期：1988-06-01 00:00:00

abstract：:Specific binding of 35S-t-butylbicyclophosphorothionate (TBPS) was studied in synaptosomal membranes of rat cerebral cortex under nonequilibrium conditions. TBPS binding proved to be suitable for the characterization of not only the efficacy but also the potency of benzodiazepine (BZ) receptor ligands in vitro. Five B...

journal_title：Biochemical pharmacology

authors： Maksay G,Simonyi M

更新日期：1988-06-01 00:00:00

abstract：:Immunoliposomes were made by covalently linking Fab' fragments (from rabbit antimouse erythrocyte IgG) to reverse-phase evaporation vesicles (REV) via maleimido-4-(p-phenylbutyrate) phosphatidylethanolamine (MPB-PE) as anchor molecule. These immunoliposomes were characterized in terms of size, charge, stability and an...

journal_title：Biochemical pharmacology

authors： Peeters PA,Claessens CA,Eling WM,Crommelin DJ

更新日期：1988-06-01 00:00:00

abstract：:The oxidation of 14C-pyruvate by isolated rat pancreatic islets was inhibited competitively and in a concentration-dependent manner by alpha-cyano-4-hydroxycinnamate. A similar, though less marked inhibition was observed of U-14C-glucose oxidation, although oxidation of 1-14C-glucose was slightly enhanced in the prese...

journal_title：Biochemical pharmacology

authors： Best L,Tomlinson S

更新日期：1988-05-15 00:00:00

abstract：:L1210 and K562 leukaemic cells have been used to study the relationship between cytotoxicity and free radical production by two aziridinyl benzoquinones, 2,5-bis(carboethoxyamino)3,6-diaziridinyl-1,4-benzoquinone (AZQ) and 2,5-bis(2-hydroxyethylamino)-3,6-diaziridinyl-1,4-benzoquinone (BZQ). BZQ showed a high level of...

journal_title：Biochemical pharmacology

authors： Lea JS,Garner HJ,Butler J,Hoey BM,Ward TH

更新日期：1988-05-15 00:00:00

abstract：:This report characterizes the cytochrome P-450 isozyme involved in midazolam metabolism. This study was undertaken into liver microsomal fractions prepared from untreated rabbits or animals treated with drugs known to specifically induce various cytochrome P-450 isozymes such as form LM2 by phenobarbital, LM4 and LM6 ...

journal_title：Biochemical pharmacology

authors： Fabre G,Crevat-Pisano P,Dragna S,Covo J,Barra Y,Cano JP

更新日期：1988-05-15 00:00:00