abstract：:The cytoprotective effects of propylthiouracil (PTU) were studied in rats treated with the hepatotoxin D-galactosamine (D-GNH2). Five days of PTU pretreatment prior to D-GNH2 caused hypothyroidism and a significant reduction in liver injury as assessed by serum transaminase levels. When PTU was administered as a singl...

journal_title：Biochemical pharmacology

authors： Cooper DS,Carter EA,Kieffer JD,Wands JR

更新日期：1984-11-01 00:00:00

abstract：:Since chlorine placement and the degree of chlorination of the biphenyl nucleus play an important role in the metabolism and ultimate elimination of polychlorinated biphenyls (PCBs), we have studied the metabolism of 4,4'-dichlorobiphenyl (4-DCB) by human hepatic microsomes. This low molecular weight PCB congener is s...

journal_title：Biochemical pharmacology

authors： Schnellmann RG,Volp RF,Putnam CW,Sipes IG

更新日期：1984-11-01 00:00:00

abstract：:a synthetic seleno-organic compound, 2-phenyl-1,2-benzoisoselenazol-3(2H)-one (PZ 51), exhibits GSH peroxidase-like activity in vitro, in contrast to its sulfur analog, PZ 25. In addition, PZ 51 behaves as an antioxidant shown by a temporary protection of rat liver microsomes against ascorbate/ADP-Fe-induced lipid per...

journal_title：Biochemical pharmacology

authors： Müller A,Cadenas E,Graf P,Sies H

更新日期：1984-10-15 00:00:00

abstract：:1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) is a commercially available chemical reagent. Although little has been known about its biological effects, recently MPTP has been reported to cause irreversible Parkinson's disease-like symptoms in humans and in monkeys. We describe here another pharmacologic effect ...

journal_title：Biochemical pharmacology

authors： Fuller RW,Hahn RA,Snoddy HD,Wikel JH

更新日期：1984-10-01 00:00:00

abstract：:The indole alkaloid gramine is found in several plant families. Its effects on mammalian mitochondria and submitochondrial particles were studied. Low concentrations of gramine slightly stimulated basal electron transport, totally inhibited the Ca2+-induced respiratory control and partially abolished the enhancement o...

journal_title：Biochemical pharmacology

authors： Niemeyer HM,Roveri OA

更新日期：1984-10-01 00:00:00

abstract：:Methotrexate (MTX) polyglutamates were detected in osteogenic sarcoma tumor samples obtained from patients 24 or 48 h after receiving high-dose MTX/leucovorin rescue therapy. Tumor samples were assayed by high-performance liquid chromatography, and polyglutamyl metabolites, along with MTX, were quantitated using both ...

journal_title：Biochemical pharmacology

authors： Samuels LL,Feinberg A,Moccio DM,Sirotnak FM,Rosen G

更新日期：1984-09-01 00:00:00

abstract：:Improved syntheses, based on Lewis acid-catalyzed nucleosidation, are described for the preparation of 5-alkyl-2'-deoxyuridines. These were converted to their 5'-phosphates with the use of wheat shoot phosphotransferase. The dUMP analogues, 5-ethyl-dUMP and 5-propyl-dUMP, were competitive vs dUMP inhibitors of thymidy...

journal_title：Biochemical pharmacology

authors： Rode W,Kulikowski T,Kedzierska B,Jastreboff M,Shugar D

更新日期：1984-09-01 00:00:00

abstract：:Carbon tetrachloride (CCl4)-induced inhibition of very low density lipoprotein (VLDL) secretion was studied in isolated hepatocytes. The hypothesis that inhibition of secretion is due to altered calcium homeostasis following CCl4-dependent inhibition of endoplasmic reticulum calcium sequestration was investigated. Inh...

journal_title：Biochemical pharmacology

authors： Pencil SD,Brattin WJ Jr,Glende EA Jr,Recknagel RO

更新日期：1984-08-01 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：:Eighty pyrimidine base analogs were evaluated as inhibitors of mouse liver orotate phosphoribosyltransferase (OPRTase, EC 2.4.2.10). Based on these findings and an extensive literature review, a structure-activity relationship has been formulated for the binding of pyrimidine base analogs to OPRTase. This study provid...

journal_title：Biochemical pharmacology

authors： Niedzwicki JG,Iltzsch MH,el Kouni MH,Cha S

更新日期：1984-08-01 00:00:00

abstract：:8-Carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4-(3H )-one- mitozolomide (CCRG 81010, M & B 39565, NSC 353451) is a potent inhibitor of the growth of a number of experimental tumours and can potentially decompose to give either an isocyanate or the monochloroethyltriazene (MCTIC). In vitro CCRG 81010 is ...

journal_title：Biochemical pharmacology

authors： Horgan CM,Tisdale MJ

更新日期：1984-07-15 00:00:00

abstract：:In model experiments using human erythrocytes, glycochenodeoxycholate caused extensive membrane damage (as judged by release of membrane phospholipid and acetylcholinesterase and by cell lysis) at approximately 10-fold lower concentrations than glycocholate. Chenodeoxycholate feeding had no effect upon the total prote...

journal_title：Biochemical pharmacology

authors： Rahman K,Billington D

更新日期：1984-07-15 00:00:00

abstract：:The binding interactions of some aryl carboxylic acid derivatives have been examined by circular dichroism and fluorescence spectroscopy. With specific probes, we have shown that the seven ligands under study bind primarily to the benzodiazepine site on HSA. Their association constants are in the range of 10(5)-10(6) ...

journal_title：Biochemical pharmacology

authors： Urien S,D'Athis P,Tillement JP

更新日期：1984-07-15 00:00:00

abstract：:Novel hydroxynaphthoquinones have been shown to be potent and selective inhibitors of mitochondrial electron transport in the protozoan Eimeria tenella, inhibiting at concentrations of 10(-10) to 10(-11)M. The primary site of electron transport inhibition has been localized to the ubiquinol-cytochrome c reductase span...

journal_title：Biochemical pharmacology

authors： Fry M,Hudson AT,Randall AW,Williams RB

更新日期：1984-07-01 00:00:00

abstract：:The kinetics of methotrexate inhibition of dihydrofolate reductase from Neisseria gonorrhoeae have been investigated. Methotrexate was shown to be a tight-binding inhibitor (Kt = 13 pM) competitive with dihydrofolate. However, "stoichiometric" or "pseudoirreversible" inhibition could not be demonstrated. Progress curv...

journal_title：Biochemical pharmacology

authors： Baccanari DP,Tansik RL

更新日期：1984-07-01 00:00:00

abstract：:Glutathione transferases are believed to play an important protective role in the various tissues of animals and man by catalysing the glutathione conjugation of electrophilic drugs and electrophilic drug metabolites. Many of these compounds have the potential to react with vital cellular macromolecules in the absence...

journal_title：Biochemical pharmacology

authors： Ahokas JT,Davies C,Ravenscroft PJ,Emmerson BT

更新日期：1984-06-15 00:00:00

abstract：:Theophylline, caffeine, isobutylmethylxanthine, papaverine, N6-cyclohexyladenosine, N6-allyl-N6-cyclohexyladenosine ( ACHA ) and N6-L-phenylisopropyladenosine (L-PIA) inhibited the transport of adenosine, uridine and hypoxanthine in Novikoff rat hepatoma cells. The IC50 values for the inhibition of uridine transport r...

journal_title：Biochemical pharmacology

authors： Plagemann PG,Wohlhueter RM

更新日期：1984-06-01 00:00:00

abstract：:Human red blood cells and male Sprague-Dawley rats were treated in vitro and in vivo, respectively, with phenylhydrazine in order to determine whether the release of volatile hydrocarbons can serve as a suitable index for phenylhydrazine-induced red blood cell peroxidation. Lipid peroxidation following phenylhydrazine...

journal_title：Biochemical pharmacology

authors： Clemens MR,Remmer H,Waller HD

更新日期：1984-06-01 00:00:00

abstract：:N-Methyl-4-phenyl-1,2,5,6-tetrahydropyridine ( MPTP ) (10 mg/kg/day i.p.) was administered to rats for 16 days, which were then observed for a further 9-11 days. MPTP administration did not alter spontaneous locomotor activity or amphetamine (2.5 mg/kg ip)-induced locomotion. Apomorphine (0.25 mg/kg sc) did not alter ...

journal_title：Biochemical pharmacology

authors： Boyce S,Kelly E,Reavill C,Jenner P,Marsden CD

更新日期：1984-06-01 00:00:00

abstract：:Wild-type and repair-deficient cell lines ( EM9 ) of Chinese Hamster Ovary cells were utilized to assess cytotoxic responses towards metals that produce lesions in DNA. Alkaline elution studies indicated that both CaCrO4 and HgCl2 induced single-strand breaks in the DNA. CaCrO4 and HgCl2 treatments of intact Chinese h...

journal_title：Biochemical pharmacology

authors： Christie NT,Cantoni O,Evans RM,Meyn RE,Costa M

更新日期：1984-05-15 00:00:00

abstract：:Leydig and Sertoli cells of the rat testes differ with respect to the activities of the enzymes of the heme and hemoprotein degradative pathway and in their responses to Cd2+ treatment. The microsomal heme oxygenase activity in the Leydig cell preparations was nearly 9- to 10-fold greater than in Sertoli cell preparat...

journal_title：Biochemical pharmacology

authors： Maines MD

更新日期：1984-05-01 00:00:00

abstract：:Cellular glutathione concentrations in primary cultures of chick embryo hepatocytes were 15.3 +/- 5.3 nmoles/mg protein (mean +/- S.D.) and remained stable for up to 3 days in culture. The presence of insulin was not essential for the maintenance of glutathione concentrations. Induction of cytochrome P-450 by phenobar...

journal_title：Biochemical pharmacology

authors： Shedlofsky SI,Sinclair PR,Sinclair JF,Bonkovsky HL

更新日期：1984-05-01 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：:The metabolism of tienilic acid, a drug containing a thiophene ring, was reinvestigated in man, rat and dog. The major urinary metabolite in man and rat was isolated and completely characterized by comparison with a synthetic compound. This metabolite derives from the hydroxylation of the thiophene ring of tienilic ac...

journal_title：Biochemical pharmacology

authors： Mansuy D,Dansette PM,Foures C,Jaouen M,Moinet G,Bayer N

更新日期：1984-05-01 00:00:00

abstract：:The mechanism of the antiaggregating activity of flavonoids was studied in vitro. The activity of fifteen different compounds was tested on platelet aggregation and arachidonic acid metabolism. The effect of flavonoids on platelet adenosine 3',5'-cyclic monophosphate (cyclic AMP) levels under basal conditions, as well...

journal_title：Biochemical pharmacology

authors： Landolfi R,Mower RL,Steiner M

更新日期：1984-05-01 00:00:00

abstract：:Rats treated with six to eight doses (80 mg/kg, i.p.) of 4-pentenoic acid, an inhibitor of mitochondrial fatty acid oxidation in vitro, during a 48-hr starvation period developed microvesicular fatty infiltration of the liver similar to that observed in Reye's Syndrome. Hepatic triglycerides were elevated an average o...

journal_title：Biochemical pharmacology

authors： Thayer WS

更新日期：1984-04-15 00:00:00

abstract：:Pig articular cartilage, overlaid with a minced preparation of synovium from the same joint, underwent extensive matrix degradation during a two-week culture period. This degradation was associated with de novo synthesis by the synovium of specific neutral proteoglycan- and collagen-degrading enzymes. Both enzymes exh...

journal_title：Biochemical pharmacology

authors： Crossley MJ,Hunneyball IM

更新日期：1984-04-15 00:00:00

abstract：:Induction of cytosolic long-chain acyl-CoA hydrolases was investigated in rat liver after administration of various peroxisome proliferators and related compounds. Treatment of rats with di-(2-ethylhexyl)-phthalate, di-(2-ethylhexyl)-adipate or tiadenol induced hydrolases I and II, while acetylsalicylic acid induced o...

journal_title：Biochemical pharmacology

authors： Katoh H,Nakajima S,Kawashima Y,Kozuka H,Uchiyama M

更新日期：1984-04-01 00:00:00

abstract：:The composition of the glycerophosphatides in pancreas and liver was studied in rats fed an ethanol-containing diet and in pair-fed controls. The fraction of arachidonoyl-containing phosphatidylinositols in pancreas was much lower in the former rats, also when the rats were starved for a final 24 hr period. This fract...

journal_title：Biochemical pharmacology

authors： Cronholm T,Curstedt T

更新日期：1984-04-01 00:00:00

abstract：:The influence of delta 9-tetrahydrocannabinol (delta 9-THC) on the cellular levels of histone mRNAs and ribosomal RNAs was examined in several normal and transformed human cell lines--HeLa S3 cells, WI-38 human diploid fibroblasts, SV40-transformed WI-38 cells, and A549 lung carcinoma cells. RNA sequences were quantit...

journal_title：Biochemical pharmacology

authors： Green LG,Stein JL,Stein GS

更新日期：1984-04-01 00:00:00

abstract：:The study of binding is not an easy task especially because of the difficulty of interpreting the results in terms of binding on specific receptor sites. The problem is not new; what is new is the increasing amount of fanciful interpretation that such a technique has generated. The tendency to interpret anomalous or i...

journal_title：Biochemical pharmacology

authors： Laduron PM

更新日期：1984-03-15 00:00:00

abstract：:Logarithmically growing Chinese hamster ovary cells, cultured in the presence of [1,4-14C]putrescine, synthesize a protein(s) containing the unusual amino acid hypusine [N epsilon-(4-amino-2-hydroxybutyl)lysine]. This protein was separated and identified by two-dimensional gel electrophoresis and fluorography. The lab...

journal_title：Biochemical pharmacology

authors： Paz MA,Torrelio BM,Gallop PM

更新日期：1984-03-01 00:00:00

abstract：:The population growth rate of HeLa cells treated with 60 microM 5,6-dichloro-1-beta-D-ribofuranosylbenzimidazole (DRB) in reinforced Eagle's minimum essential medium was directly related to the concentration of fetal bovine serum in the range from 5 to 30%. Control cells proliferated at a maximal rate (doubling time: ...

journal_title：Biochemical pharmacology

authors： Tamm I

更新日期：1984-02-15 00:00:00

abstract：:Net cadmium uptake in the isolated perfused rat liver was half-maximal at 5 microM, and the maximal rate of uptake was 22 nmoles/min per gram liver wet weight. Uptake was augmented when a permeable thiol, dithioerythritol, was infused, whereas it was restricted when glutathione as a nonpermeable thiol or also when bov...

journal_title：Biochemical pharmacology

authors： Graf P,Sies H

更新日期：1984-02-15 00:00:00

abstract：:The inactive anthracycline analog 4-demethoxy-7,9-di-epi-daunorubicin was covalently coupled to polyglutaraldehyde microspheres. The polymer-bound analog acquired significant cytostatic activity as evaluated with doxorubicin resistant and sensitive murine L1210 leukemia cells. A suggested multiple membrane interaction...

journal_title：Biochemical pharmacology

authors： Rogers KE,Tökés ZA

更新日期：1984-02-15 00:00:00

abstract：:Two novel halogenated pyrrolopyrimidine analogues of adenosine, isolated from marine sources, have been examined for pharmacological and biochemical activities. 4-Amino-5-bromo-pyrrolo[2,3-d]pyrimidine, from a sponge of the genus Echinodictyum, had bronchodilator activity at least as potent as theophylline but with a ...

journal_title：Biochemical pharmacology

authors： Davies LP,Jamieson DD,Baird-Lambert JA,Kazlauskas R

更新日期：1984-02-01 00:00:00

abstract：:Ethyl 2[5(4-chlorophenyl)pentyl]oxirane-2-carboxylate (POCA) is strongly hypoglycaemic in fasted normal and diabetic rats [H. P. O. Wolf, K. Eistetter and G. Ludwig, Diabetologia 22, 456 (1982)]. POCA was fed for 12 weeks to rats on a standard low-fat (3%) diet at levels of 0.05% and 0.2% to give daily intakes of abou...

journal_title：Biochemical pharmacology

authors： Koundakjian PP,Turnbull DM,Bone AJ,Rogers MP,Younan SI,Sherratt HS

更新日期：1984-02-01 00:00:00

abstract：:The O2 dependence of the metabolism of benzylamine to benzaldehyde, benzoate and hippurate was studied in isolated rat hepatocytes. The initial oxidation to benzaldehyde, catalyzed by monoamine oxidase, had an apparent Kmo2 value of 34 microM in cells and 40 microM in isolated rat liver mitochondria. The conversion of...

journal_title：Biochemical pharmacology

authors： Jones DP

更新日期：1984-02-01 00:00:00

abstract：:Dichlorodi[U-14C]phenyltrichloroethane ( [14C]DDT), incubated with rat hepatic microsomes and NADPH, produced reactive intermediates which covalently bound to microsomal protein and lipids. In atmospheric oxygen, DDT bound to microsomal protein; however, binding was increased up to approximately 70% by oxygen depletio...

journal_title：Biochemical pharmacology

authors： Baker MT,Van Dyke RA

更新日期：1984-01-15 00:00:00

abstract：:A new analogue of methotrexate was synthesized from 4-amino-4-deoxy-N10-methylpteroic acid and D,L-homocysteic acid. The product (mAPA-HCysA) was bound tightly to L1210 mouse leukemia dihydrofolate reductase (IC50 = 1 nM), inhibited L1210 cell proliferation in culture (IC50 = 0.3 microM), and prolonged the survival of...

journal_title：Biochemical pharmacology

authors： Rosowsky A,Moran RG,Forsch R,Colman P,Uren J,Wick M

更新日期：1984-01-01 00:00:00