abstract：:Following the administration of latex particles (0.46 micron), cytochrome P-450 dependent monooxygenase system was depressed in the livers of mice. These particles were taken up exclusively by Kupffer cells in the liver, and no particles were found in the hepatocytes which contain most of the monooxygenase capacity in...

journal_title：Biochemical pharmacology

authors： Peterson TC,Renton KW

更新日期：1986-05-01 00:00:00

abstract：:1-(3'-Chlorophenyl)-3-[2-(3,3-dimethyl-1-azetidinyl)ethyl] imidazolidin-2-one, zetidoline, a new neuroleptic agent, when incubated with rat liver microsomes was rapidly metabolized to six free (mets B, D, I, L, M and N) and two conjugated metabolites (mets E and F). Sites of the metabolic attack (oxidation) were prima...

journal_title：Biochemical pharmacology

authors： Assandri A,Galliani G,Zerilli L,Tuan G,Tarzia G,Barone D

更新日期：1986-05-01 00:00:00

abstract：:5-Fluorouracil (FUra) has been administered to mice bearing xenografts of human colon adenocarcinomas. In two tumor lines, HxGC3 and HxVRC5, intrinsically resistant to FUra, 2'-deoxyuridylate (dUMP) accumulated 13.4- and 23.9-fold above basal levels. In HxELC2 xenografts, which demonstrated some sensitivity to FUra, t...

journal_title：Biochemical pharmacology

authors： Houghton JA,Weiss KD,Williams LG,Torrance PM,Houghton PJ

更新日期：1986-04-15 00:00:00

abstract：:N-Acylurea derivatives of albumin and transferrin prepared with the water-soluble carbodiimides N-ethyl-N'-(3-dimethylaminopropyl)carbodiimide and N-ethyl-N'-(3-trimethylpropylammonium)carbodiimide iodide have been found to bind different types of DNA. The two proteins were reacted with varying amounts of carbodiimide...

journal_title：Biochemical pharmacology

authors： Huckett B,Gordhan H,Hawtrey R,Moodley N,Ariatti M,Hawtrey A

更新日期：1986-04-15 00:00:00

abstract：:Administration of phenobarbital to chick embryos increased hepatic microsomal UDP-glucuroyltransferase activity some 25-fold. The large phenobarbital-induced increase of UDP-glucuronyltransferase activity was correlated to an equivalent increase of immunochemically measurable UDP-glucuronyltransferase protein. Poly(A+...

journal_title：Biochemical pharmacology

authors： Jackson MR,Kennedy SM,Lown G,Burchell B

更新日期：1986-04-01 00:00:00

abstract：:Stimulation of hepatic glycogenolysis and vasoconstriction of the hepatic vasculature in response to acetyl glyceryl ether phosphocholine (AGEPC; platelet activating factor) was inhibited by two structural analogues of AGEPC, U66985 (1-O-octadecyl-2-O-acetyl-sn-glycero-3-phosphoric acid-6'-trimethyl ammonium hexyl est...

journal_title：Biochemical pharmacology

authors： Buxton DB,Hanahan DJ,Olson MS

更新日期：1986-03-15 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 antidepressant minaprine (3-(2-morpholino-ethylamino) 4-methyl 6-phenyl pyridazine, dihydrochloride) and its main metabolites were examined for their monoamine oxidase (MAO) inhibitory effects in the rat. In our experimental conditions, minaprine displayed in vitro a very weak affinity for brain MAO A and B with I...

journal_title：Biochemical pharmacology

authors： Kan JP,Mouget-Goniot C,Worms P,Biziere K

更新日期：1986-03-15 00:00:00

abstract：:Products derived from arachidonic acid (AA) via both the cyclo-oxygenase and lipoxygenase pathways play a role in inflammation: prostaglandins (PGs), particularly PGE2, contribute to the formation of oedema, erythema and hyperalgesia whereas leukotriene B4 (LTB4), a product of the 5' lipoxygenase, may modulate the rec...

journal_title：Biochemical pharmacology

authors： Terano T,Salmon JA,Higgs GA,Moncada S

更新日期：1986-03-01 00:00:00

abstract：:Relatively low concentrations of ascorbic acid inhibited the binding of the alpha-1 adrenergic antagonist [125I]HEAT [DL-[beta(3-iodo-4-hydroxyphenyl)-ethyl-aminomethyl]-tetralone) in rat submandibular gland and rat aorta. However, no inhibition was observed with this ligand in several other tissues, nor with several ...

journal_title：Biochemical pharmacology

authors： Jones SB,Bylund DB

更新日期：1986-02-15 00:00:00

abstract：:The effects of streptozotocin (STZ)-induced diabetes on acetaminophen metabolism and hepatotoxicity in male Sprague-Dawley (SD) and Long Evans Hooded (LEH) rats were compared. In agreement with earlier studies, normal SD rats were more resistant to acetaminophen-induced hepatic necrosis than normal LEH rats. In contra...

journal_title：Biochemical pharmacology

authors： Price VF,Jollow DJ

更新日期：1986-02-15 00:00:00

abstract：:The present study investigated the mechanism by which theophylline decreases cis-diamminedichloroplatinum(II) (DDP)-induced DNA crosslinking in L1210 cells. Alkaline elution of DNA from L1210 cells treated with DDP in the presence and absence of 1 mM theophylline showed that theophylline decreased interstrand crosslin...

journal_title：Biochemical pharmacology

authors： Ducore JM

更新日期：1986-02-15 00:00:00

abstract：:A comparison was made between 4-substituted pyrazoles and short-chain alcohols as inducers of cytochrome P-450. A quantitative structure-activity analysis of the data led to the following equations: (I) Pyrazoles: Log 1/C = 0.85 (+/- 0.21) Log P + 1.93 (+/- 0.38), r = 0.970 (II) Alcohols: Log 1/C = 0.78 (+/- 0.14) Log...

journal_title：Biochemical pharmacology

authors： Sinclair J,Cornell NW,Zaitlin L,Hansch C

更新日期：1986-02-15 00:00:00

abstract：:Adult male CD-1 mice were treated with various levels of vanadate in drinking water for 30 days. The levels of catecholamine and indoleamine neurotransmitters and their major metabolites were measured in six different brain regions. Vanadium caused a dose-related decrease in norepinephrine (NE) levels in hypothalamus,...

journal_title：Biochemical pharmacology

authors： Sharma RP,Coulombe RA Jr,Srisuchart B

更新日期：1986-02-01 00:00:00

abstract：:On the basis of previous electrophysiological studies, it has been proposed that there are three main classes of excitatory amino acid receptor in the mammalian central nervous system, which are activated preferentially by kainic acid, quisqualic acid and N-methyl-D-aspartate respectively. Although the pharmacology of...

journal_title：Biochemical pharmacology

authors： Anand H,Roberts PJ,Badman G,Dixon AJ,Collins JF

更新日期：1986-02-01 00:00:00

abstract：:To study the effect of sex hormones and alcohol on the hepatic activities of alcohol metabolizing enzymes, estradiol or testosterone were administered for 4 weeks to ovarectomized or sham operated adult female rats pair-fed nutritionally adequate liquid diets containing either alcohol (36% of total calories) or isocal...

journal_title：Biochemical pharmacology

authors： Teschke R,Wannagat FJ,Löwendorf F,Strohmeyer G

更新日期：1986-02-01 00:00:00

abstract：:After rats were injected with the reduced glutathione (GSH) depletor phorone (diisopropylidene acetone, 250 mg/kg, i.p.), there was a significant increase in microsomal glutathione S-transferase activity in the liver. The maximum activity was observed 24 hr after injection and was about 2-fold that of the control acti...

journal_title：Biochemical pharmacology

authors： Masukawa T,Iwata H

更新日期：1986-02-01 00:00:00

abstract：:The amino acid conjugation of the phenoxyherbicides 2,4-dichlorophenoxyacetate (2,4-D) and 2,4,5-trichlorophenoxyacetate (2,4,5-T) by animals was examined at the level of the enzymes catalyzing the reactions. The phenoxyherbicides were not substrates for the bile acid conjugating system but were substrates for the mit...

journal_title：Biochemical pharmacology

authors： Kelley M,Vessey DA

更新日期：1986-01-15 00:00:00

abstract：:The antiinflammatory effect of superoxide dismutase was studied in rats with kidney intoxication induced by the injection of nephrotoxic serum. The urinary excretion of protein was increased significantly by the administration of an intravenous injection of nephrotoxic serum. The daily injection of superoxide dismutas...

journal_title：Biochemical pharmacology

authors： Adachi T,Fukuta M,Ito Y,Hirano K,Sugiura M,Sugiura K

更新日期：1986-01-15 00:00:00

abstract：:Intact brain cell aggregates were dissociated from adult rat brains, by a simple sieving technique, and were used to study the binding characteristics of [3H]N-methylscopolamine to muscarinic acetylcholine receptors. The magnitude of binding of this ligand was related linearly to the amount of cell protein in the bind...

journal_title：Biochemical pharmacology

authors： Lee JH,el-Fakahany EE

更新日期：1985-12-15 00:00:00

abstract：:The interaction of the vasodilator, hydralazine, with the molybdenum hydroxylases, aldehyde oxidase and xanthine oxidase has been investigated. A potent progressive inhibition of rabbit liver aldehyde oxidase, in the presence of substrate, by low concentrations of hydralazine (0.1-1 microM) was observed in vitro but n...

journal_title：Biochemical pharmacology

authors： Johnson C,Stubley-Beedham C,Stell JG

更新日期：1985-12-15 00:00:00

abstract：:Chronic administration of the beta-adrenergic receptor agonist isoproterenol (5 mg/200 g animal for 10 days) resulted in rat parotid and submandibular gland hypertrophy, and it induced synthesis of a series of proline-rich proteins (PRPs) and glycoproteins. Treated parotid glands additionally exhibit an increase in ac...

journal_title：Biochemical pharmacology

authors： Wells DJ,Humphreys-Beher MG

更新日期：1985-12-15 00:00:00

abstract：:African trypanosomes, like Trypanosoma brucei, depend on antigenic variation to evade the immune response of the vertebrate host. An antigenic switch corresponds to the activation of a variable surface glycoprotein (VSG) gene from a large silent repertoire. Most switches require the duplicative transposition of a VSG ...

journal_title：Biochemical pharmacology

authors： Cornelissen AW,Michels PA,Borst P,Spanjer W,Versluijs-Broers JA,Van der Meer C,Farzaneh F,Shall S

更新日期：1985-12-01 00:00:00

abstract：:Double-labelled [methyl-14C,5-3H]CDPcholine has been synthesized and subjected to a pharmacokinetic analysis in several biological systems. In transport experiments with intact human erythrocytes no incorporation of radioactivity is observable. On the other hand the results obtained with perfused rat liver suggest a r...

journal_title：Biochemical pharmacology

authors： Galletti P,De Rosa M,Nappi MA,Pontoni G,del Piano L,Salluzzo A,Zappia V

更新日期：1985-12-01 00:00:00

abstract：:Phosphatidylinositol specific phospholipase C from Staphylococcus aureus could solubilize acetylcholinesterase up to 55% from sheep platelets in the presence of ethylenediaminetetra acetic acid (EDTA). The endogenous phosphatidylinositol specific phospholipase C of platelets activated by deoxycholate (at 3-5 mM) could...

journal_title：Biochemical pharmacology

authors： Majumdar R,Balasubramanian AS

更新日期：1985-12-01 00:00:00

abstract：:Adenosine (Ado, 10 microM) did not inhibit ADP-induced human platelet aggregation in whole blood. However, if the blood was preincubated with dipyridamole (10 microM), a potent inhibitor of the erythrocytic nucleoside transport system (NTS), Ado acted as a strong inhibitor of platelet aggregation. Similarly, Ado inhib...

journal_title：Biochemical pharmacology

authors： Dawicki DD,Agarwal KC,Parks RE Jr

更新日期：1985-11-15 00:00:00

abstract：:We have studied the effects of TPA on the metabolism of porcine thyroid cells cultured for 1-4 days in the absence (control cells) and in the presence of 0.1 mU/ml TSH (TSH cells). The phospholipid turnover, evaluated after a 2 hr incorporation of 32P-phosphate into phospholipids, is markedly modified by the presence ...

journal_title：Biochemical pharmacology

authors： Haye B,Aublin JL,Champion S,Lambert B,Jacquemin C

更新日期：1985-11-01 00:00:00

abstract：:Administration of non-cholestatic doses of manganese (Mn2+) followed by injection of bilirubin (BR) results in a severe reduction in rat bile flow. Male Sprague-Dawley rats were given various doses of Mn2+ (2, 4.5, 8, and 18 mg/kg, i.v.) and killed 0.25, 1, 3, or 5 hr later. 54Mn2+ was used to evaluate Mn2+ content (m...

journal_title：Biochemical pharmacology

authors： Ayotte P,Plaa GL

更新日期：1985-11-01 00:00:00

abstract：:ATP-dependent Ca2+ sequestration by rat liver microsomes was assayed using three different methods, and characterized with regard to the effect of various inhibitors. When glucose and hexokinase were added in combination to deplete ATP in the incubation, Ca2+ uptake was followed by rapid release of Ca2+ from the micro...

journal_title：Biochemical pharmacology

authors： Thor H,Hartzell P,Svensson SA,Orrenius S,Mirabelli F,Marinoni V,Bellomo G

更新日期：1985-10-15 00:00:00

abstract：:The ex vivo sensitivity of murine pluripotent hematopoietic stem cells (CFU-S) and myeloid progenitor cells (CFU-GM) to 4-hydroperoxycyclophosphamide, ASTA Z 7557, phosphoramide mustard, acrolein, melphalan, and cis-platinum was determined in the absence and presence of known (disulfiram, diethyldithiocarbamate, cyana...

journal_title：Biochemical pharmacology

authors： Kohn FR,Sladek NE

更新日期：1985-10-01 00:00:00

abstract：:Histamine H-1 receptors in human peripheral lung were characterized by radioligand and biochemical assays employing binding of the H-1 receptor antagonist [3H]pyrilamine to plasma membrane preparations. Simultaneous computerized analyses of the data from fourteen separate equilibrium-binding assays indicated the prese...

journal_title：Biochemical pharmacology

authors： Casale TB,Rodbard D,Kaliner M

更新日期：1985-09-15 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：:The azoreduction of N,N-dimethyl-4-aminoazobenzene (DAB) and N-methyl-4-amino-azobenzene (MAB) by rat liver microsomes was investigated. It was shown that measurement of azoreduction of DAB and structurally related azo dyes by the conventional method of substrate disappearance required an anaerobic environment since N...

journal_title：Biochemical pharmacology

authors： Levine WG

更新日期：1985-09-15 00:00:00

abstract：:Histrionicotoxin, a spiropiperidine alkaloid, and twenty-two analogs inhibited binding of [3H]perhydrohistrionicotoxin [( 3H]H12-HTX) and of [3H]phencyclidine [( 3H]PCP) to sites on the acetylcholine receptor-ion complex of Torpedo electroplax membranes. Structural alterations to the nitrogen (secondary amine) or oxyg...

journal_title：Biochemical pharmacology

authors： Aronstam RS,King CT Jr,Albuquerque EX,Daly JW,Feigl DM

更新日期：1985-09-01 00:00:00

abstract：:3,3-Dimethylbutanol (Dimbunol), a competitive inhibitor of choline dehydrogenase (CDH), and ethylcholine mustard aziridinium (ECMA), an effective irreversible inhibitor of both CDH and choline transport, were investigated for their effects upon the uptake and metabolism of [3H]choline in mice. Thirty minutes after Dim...

journal_title：Biochemical pharmacology

authors： Barlow P,Marchbanks RM

更新日期：1985-09-01 00:00:00

abstract：:The influence of age on the mixed function oxidase system from a non-human primate was studied. Microsomes were isolated from the livers of female Macaca nemestrina ranging from 2 to 21 years of age. No significant age-related change was observed in either the cytochrome P-450 content or the NADPH cytochrome c reducta...

journal_title：Biochemical pharmacology

authors： Sutter MA,Wood WG,Williamson LS,Strong R,Pickham K,Richardson A

更新日期：1985-08-15 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：:The effects of methylxanthines and non-xanthine phosphodiesterase-inhibitors on the low Km cyclic AMP phosphodiesterase of intact rat adipocytes were studied. Methylxanthines and papaverine stimulated rather than inhibited the enzyme when intact adipocytes were incubated in their presence. The effect of papaverine was...

journal_title：Biochemical pharmacology

authors： Wong EH,Ooi SO

更新日期：1985-08-15 00:00:00

abstract：:Male ddY mice were given one injection of (1) mercury (mercuric chloride) simultaneously with various doses of selenium (sodium selenite), (2) mercury alone, or (3) various doses of selenium alone. The interaction between mercury and selenium in the liver and kidneys at 1, 5, 24, 120, and 240 hr after administration w...

journal_title：Biochemical pharmacology

authors： Yamamoto I

更新日期：1985-08-01 00:00:00

abstract：:To determine if both the Ca2+-calmodulin system and the cyclic AMP system may regulate tyrosine hydroxylase (TH) activity in situ, rat striatal tissue slices that contain all of the components of the TH, cyclic AMP and Ca2+-calmodulin systems were subjected to experimental manipulations. Incubation of striatal tissue ...

journal_title：Biochemical pharmacology

authors： Hirata Y,Nagatsu T

更新日期：1985-08-01 00:00:00