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：: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

abstract：:Only very low levels of peroxidase activity were detected in castrated male hamster kidneys [1.0 +/- 0.8(S.E.) units/g protein], and chronic estrogen administration, either diethylstilbestrol (DES) or 17 beta-estradiol, for 1-5 months did not result in any appreciable increase in this activity. In contrast, hamster li...

journal_title：Biochemical pharmacology

authors： Klicka JK,Li SA,Li JJ

更新日期：1983-02-01 00:00:00

abstract：:Antibodies raised against purified hog renal or intestinal brush border protein or against purified hog kidney angiotensin I converting enzyme (ACE) were used to characterize renal and intestinal brush border ACE by techniques of differential solubilization, fused-rocket, line absorption and crossed-immunoelectrophore...

journal_title：Biochemical pharmacology

authors： Ward PE,Sheridan MA

更新日期：1983-01-15 00:00:00

abstract：:The binding of 1,1-dichloroethane (1,1-DCE) to the substrate binding site of hepatic microsomal cytochrome P-450, and the stimulation of hepatic microsomal CO-inhibitable NADPH oxidation by 1,1-DCE and 1,2-dichloroethane (1,2-DCE) were enhanced by induction with phenobarbital but not with beta-naphthoflavone. Incubati...

journal_title：Biochemical pharmacology

authors： McCall SN,Jurgens P,Ivanetich KM

更新日期：1983-01-15 00:00:00

abstract：:The protective action of cysteine or mercaptopropionylglycine (MPG) in acute ethanol-induced liver injury has been investigated in the rat. Cysteine accelerated clearance of ethanol and acetaldehyde from blood and liver and prevented an increase in hepatic content of triglyceride and serum ornithine carbamoyl transfer...

journal_title：Biochemical pharmacology

authors： Hirayama C,Kishimoto Y,Wakushima T,Murawaki Y

更新日期：1983-01-15 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：:Preincubation with (S)-alpha-fluoromethylhistidine, an irreversible inhibitor of histidine decarboxylase, was found to markedly reduce, but not eliminate, the uptake of [3H]histidine by rat peritoneal mast cells. The Vmax for histidine transport for cells in which decarboxylation of histidine had been completely inhib...

journal_title：Biochemical pharmacology

authors： Bauza MT,Lagunoff D

更新日期：1983-01-01 00:00:00

abstract：:The abilities of the naturally occurring polyamines, putrescine, spermidine and spermine, to affect variables related to the bioenergetic functions of isolated rat liver mitochondria were studied. At concentrations comparable to those present intracellularly, the polyamines inhibited state 4 respiration, but they had ...

journal_title：Biochemical pharmacology

authors： Byczkowski JZ,Zychlinski L,Porter CW

更新日期：1982-12-15 00:00:00

abstract：:A comparative study of the N-B transition and the drug binding properties of human serum albumin samples from various sources has been carried out with the help of circular dichroism and equilibrium dialysis. It was found that when warfarin was used as a marker the midpoint pH and the cooperative nature of the N-B tra...

journal_title：Biochemical pharmacology

authors： Dröge JH,Wilting J,Janssen LH

更新日期：1982-12-01 00:00:00

abstract：:Our results indicate that sex hormones play an important role in the regulation of brain and hepatic GST protein during maturity. The conjugating factor GSH does not appear to be under the influence of sex hormones. These observations are of great significance in view of the possibility of continued exposure to neurot...

journal_title：Biochemical pharmacology

authors： Das M,Agarwal AK,Seth PK

更新日期：1982-12-01 00:00:00

abstract：:The source of urinary catecholamines and the mechanisms by which tyrosine administration raises these compounds were investigated in rats. Adrenalectomy blocked the tyrosine-induced rise in urinary epinephrine but not dopamine or norepinephrine. Following chemical sympathectomy with 6-hydroxydopamine (6-OHDA), the tyr...

journal_title：Biochemical pharmacology

authors： Agharanya JC,Wurtman RJ

更新日期：1982-11-15 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：:Purified ornithine decarboxylase (EC 4.1.1.17, ODC) transamidated with four putrescine moieties on four glutamine residues through the action of transglutaminase (EC 2.3.2.13, TGase) purified from guinea pig liver, when added to isolated rat liver nuclei, stoichiometrically increased the activity of RNA polymerase I (...

journal_title：Biochemical pharmacology

authors： Russell DH,Manen CA

更新日期：1982-11-01 00:00:00

abstract：:Chlorpromazine, imipramine and amitriptyline, drugs structurally related to riboflavin, each inhibited the formation in vivo of flavin adenine dinucleotide (FAD) from riboflavin in rat heart at 2-5 mg/kg body weight, doses comparable on a weight basis to those used clinically. All three drugs inhibited FAD formation i...

journal_title：Biochemical pharmacology

authors： Pinto J,Huang YP,Pelliccione N,Rivlin RS

更新日期：1982-11-01 00:00:00

abstract：:The crude mitochondrial fraction of rat brain contains an active dehydrogenase involved in the direct oxidation of gamma-aminobutyric acid. INT (p-iodonitrotetrazolium violet) can serve as an efficient acceptor of electrons in this dehydrogenase reaction. During this oxidation of GABA, ammonia is not produced. In vitr...

journal_title：Biochemical pharmacology

authors： Banerjee A,Turner AJ,Guha SR

更新日期：1982-10-15 00:00:00

abstract：:Change in the membrane fluidity of human erythrocytes on transformation to stomatocytes was observed by ESR spectroscopy using 12-doxyl stearic acid or its methyl ester as a probe. When the transformation to stomatocytes was induced by four qualitatively different methods, i.e. (a) addition of cationic amphiphilic age...

journal_title：Biochemical pharmacology

authors： Noji S,Takahashi T,Kon H

更新日期：1982-10-15 00:00:00

abstract：:Phenylbutazone (PBZ) is known to inhibit the oriented migration of human polymorphonuclear leukocytes (PMNs) induced by formyl-methionyl-leucyl-phenylalanine (FMLP), and to protect these cells against the deactivation caused by their prior incubation with FMLP. To gain insight into the mechanism of these effects, we m...

journal_title：Biochemical pharmacology

authors： Perianin A,Labro MT,Hakim J

更新日期：1982-10-01 00:00:00

abstract：:A calcium antagonist, verapamil, enhanced the cellular uptake and cytotoxicity of vincristine (VCR) in adriamycin-resistant P388 leukemia (P388/ADM) cells and also enhanced the cellular uptake and cytotoxicity of adriamycin (ADM) in vincristine-resistant P388 leukemia (P388/VCR) and P388/ADM cells. The enhancement of ...

journal_title：Biochemical pharmacology

authors： Tsuruo T,Iida H,Yamashiro M,Tsukagoshi S,Sakurai Y

更新日期：1982-10-01 00:00:00

abstract：:The treatment of rats with 10 mumoles/kg (s.c.) of mercuric chloride (Hg2+) caused time-dependent decreases in the activities of the enzymes of the glutathione (GSH) metabolism pathway in the kidney. Twenty-four hours after administration of Hg2+, the activities of gamma-glutamylcysteine synthetase and glutathione dis...

journal_title：Biochemical pharmacology

authors： Chung AS,Maines MD,Reynolds WA

更新日期：1982-10-01 00:00:00

abstract：:Low molecular weight cadmium-binding proteins were studed in lung tissue from rabbits exposed to aerosols of CdCl2. Lungs obtained from animals exposed by inhalation to aerosols of 800 or 1600 micrograms/m3 CdCl2 for 2-hr periods/day, every other day for a 5-day period, were found to contain at least three low molecul...

journal_title：Biochemical pharmacology

authors： Post CT,Squibb KS,Fowler BA,Gardner DE,Illing J,Hook GE

更新日期：1982-09-15 00:00:00

abstract：:The sensitivity to barbiturates of [3H]GABA binding to synaptosomal membrane fractions from rat cortex has been examined. We show that a range of anaesthetic/sedative barbiturates enhance GABA binding in the presence of chloride or other ions that interact with the associated ionophore. Furthermore, picrotoxinin and t...

journal_title：Biochemical pharmacology

authors： Whittle SR,Turner AJ

更新日期：1982-09-15 00:00:00

abstract：:Phospholipase A2 activity was detected in 7-day-old carrageenin-induced inflammatory tissue of rats using a synthetic substrate. 1-acyl-2-[3H]arachidonyl-phosphatidylcholine. The inflammatory tissue was homogenized in saline containing 1 M KCl, and the 105,000 g supernatant fraction was placed on a Sephadex G-100 colu...

journal_title：Biochemical pharmacology

authors： Ohuchi K,Watanabe M,Numajiri N,Tsurufuji S

更新日期：1982-09-15 00:00:00

abstract：:The deamination of 5-hydroxytryptamine, tryptamine and benzylamine by porcine dental pulp membrane preparations is brought about not only by monoamine oxidase, but also by a clorgyline (and deprenyl) resistant), semicarbazide sensitive enzyme. The semicarbazide sensitive enzyme was also inhibited by aminoguanidine, hy...

journal_title：Biochemical pharmacology

authors： Norqvist A,Oreland L,Fowler CJ

更新日期：1982-09-01 00:00:00

abstract：:Three therapeutic inhibitors of vertebrate alpha-glucosidases recently assayed in research on diabetes control, show high inhibitory potencies towards the p-NP-alpha-D-glucosidase activity of honeybee haemolymph. BAYe 4609 is an allosteric V-type (pure non-competitive) inhibitor with: Ki congruent to K'i congruent to ...

journal_title：Biochemical pharmacology

authors： Bounias M

更新日期：1982-09-01 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：:Casein-elicited rat peritoneal polymorphonuclear leukocytes (PMNL) and rabbit platelets were prelabelled with [1-14C]arachidonic acid, and the effect of timegadine, a new anti-inflammatory agent, on the release and metabolism of arachidonic acid induced by A23187 (PMNL) and thrombin (platelets) was studied and compare...

journal_title：Biochemical pharmacology

authors： Ahnfelt-Rønne I,Arrigoni-Martelli E

更新日期：1982-08-15 00:00:00

abstract：:The effects of estradiol on the endogenous fatty acid (specifically, arachidonic acid) composition of cellular phospholipid fractions and the 12-lipoxygenase activity in rat platelets in vivo were studied. Estradiol had no significant effect on the endogenous fatty acid composition of cellular phospholipid fractions. ...

journal_title：Biochemical pharmacology

authors： Chang WC,Nakao J,Orimo H,Tai HH,Murota SI

更新日期：1982-08-15 00:00:00

abstract：:3-alpha-Methyl substituted digitoxigenin-3-beta-glucoside (methyl-dtg-gluc) displays unusual features, e.g. a high dissociation rate constant from its binding site leading to rapid reversibility of the inotropic and toxic effects, and a flat dose-response curve attaining higher inotropic maxima thus indicating an incr...

journal_title：Biochemical pharmacology

authors： Lüllmann H,Mohr K

更新日期：1982-08-01 00:00:00

abstract：:Disodium cromoglycate and compounds which elevated levels of cyclic AMP in the mast cell variously inhibited cytotoxic histamine release induced by the surface active agents melittin, Tween 20 and Triton X-100. These results are inconsistent with the postulated effects of the drugs on receptor mediated calcium channel...

journal_title：Biochemical pharmacology

authors： Pearce FL,Clements J

更新日期：1982-07-01 00:00:00

abstract：:The effect of 5 consecutive daily i.p. doses of CPZ (5 mg/kg), PZ (10 mg/kg) and PMZ (10 mg/kg) on the activity of kynurenine hydrolase and kynurenine aminotransferase in mouse liver was studied. All three phenothiazines effected an increase in the activity of kynurenine hydrolase per unit weight of liver with CPZ sho...

journal_title：Biochemical pharmacology

authors： Mostafa MH,El-Sewedy SM,El-Bassiouni EA,Abdel-Tawab GA

更新日期：1982-07-01 00:00:00

abstract：:The major metabolic products of the endogeneous catecholamine dopamine are its 3- and 4-O-sulphates which have also been implicated as intermediates in noradrenaline biosynthesis. Because of the unsatisfactory status of the literature concerning the synthesis, isolation, purity and characterisation of the dopamine O-s...

journal_title：Biochemical pharmacology

authors： Osikowska BA,Idle JR,Swinbourne FJ,Sever PS

更新日期：1982-07-01 00:00:00

abstract：:Phenylethanolamine-N-methyltransferase (PNMT) catalyzes the conversion of norepinephrine to epinephrine. The enzyme, obtained from bovine adrenal gland, was incubated with PbCl2 at 23 degrees for various times prior to assay at 37 degrees. Inhibition developed slowly and reached a maximum after 45 min. In the presence...

journal_title：Biochemical pharmacology

authors： Caspers ML

更新日期：1982-06-01 00:00:00

abstract：:Although clofibrate has been shown to inhibit platelet aggregation that is caused by thrombin, ADP and epinephrine, by blocking the release of arachidonic acid from platelet phospholipids [8], here we have demonstrated that clofibrate enhanced platelet aggregation by arachidonic acid and PLC and reversed the effects o...

journal_title：Biochemical pharmacology

authors： Huzoor-Akbar,Witiak DT,Newman HA,Fertel RH,Feller DR

更新日期：1982-06-01 00:00:00

abstract：:In this study, 1,4,6-androstatriene-3,17-dione (ATD) was demonstrated to cause time-dependent loss of aromatase activity in rat ovarian microsomes in vitro. In vivo, an injection of ATD caused inhibition of ovarian aromatase and reduced estrogen secretion in pregnant mare's serum gonadotropin-primed rats for at least ...

journal_title：Biochemical pharmacology

authors： Brodie AM,Brodie HJ,Garrett WM,Hendrickson JR,Marsh DA,Tsai-Morris CH

更新日期：1982-06-01 00:00:00

abstract：:The primary objective of this research was to test the hypothesis that low level lead (Pb) exposure during early life leads to disruption in blood-brain barrier (BBB) function in the young rat. Newborn rats received lead via milk from lactating dams that were drinking water containing 0.1% lead acetate Pb(Ac)2. Pups w...

journal_title：Biochemical pharmacology

authors： Michaelson IA,Bradbury M

更新日期：1982-05-15 00:00:00

abstract：:To assess the relative contributions that the sodium channel blocking activity of propranolol may play in a variety of its therapeutic applications, its effects were examined in vitro with a sodium channel specific 22Na+ uptake system, using rat brain membranes. Propranolol inhibited 22Na+ uptake in the rat brain memb...

journal_title：Biochemical pharmacology

authors： Matthews JC,Baker JK

更新日期：1982-05-01 00:00:00

abstract：:The present study was designed to prepare and characterize subcellular fractions from the liver of the Northern pike (Esox lucius), with special emphasis on the preparation of microsomal fractions suitable for studying xenobiotic metabolism. The purity of the different fractions obtained by differential centrifugation...

journal_title：Biochemical pharmacology

authors： Balk L,Meijer J,Bergstrand A,Aström A,Morgenstern R,Seidegård J,DePierre JW

更新日期：1982-04-15 00:00:00

abstract：:Oral administration of tobacco to rats for 21 days caused remarkable stimulation of the metabolism of phenacetin, aniline and benzo[a]pyrene, a carcinogen, by hepatic microsomal mixed function oxidases (MFO). Such treatment for 6 days resulted in a small increase in the activities of phenacetin O-dealkylase and aromat...

journal_title：Biochemical pharmacology

authors： Kaur S,Ali B

更新日期：1982-04-15 00:00:00

abstract：:Prostaglandin synthetase has the ability to catalyze the metabolism of paracetamol to a reactive metabolite, which binds to protein and reduced glutathione (GSH). This was demonstrated with microsomes isolated from both sheep seminal vesicles (SSV) and rabbit kidney medulla. The activation of paracetamol occurred thro...

journal_title：Biochemical pharmacology

authors： Moldéus P,Andersson B,Rahimtula A,Berggren M

更新日期：1982-04-01 00:00:00