Competition between paraquat and putrescine for uptake by suspensions of rat alveolar type II cells.

abstract：:Using a continuous perfusion system, synaptosomes prepared from rat brain released [3H]norepinephrine in a Ca2+-dependent manner when pulse depolarized by briefly elevating external potassium concentrations. Tetrodotoxin (10(-7) M), a sodium channel blocker, inhibited 48% of this pulsed release, and D595 (10(-5) M), a...

journal_title：Biochemical pharmacology

authors： Clark JM,Brooks MW

更新日期：1989-07-15 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 binding of nimodipine, a 1,4-dihydropyridine Ca2+ channel antagonist, and of Bay K 8644, a Ca2+ channel activator, was measured in several regions of rat brain and compared to the distribution of K+ depolarization-induced 45Ca2+ uptake into synaptosomes. The maximum binding densities (Bmax) of [3H]nimodipine and [...

journal_title：Biochemical pharmacology

authors： Skattebøl A,Triggle DJ

更新日期：1987-12-01 00:00:00

abstract：:Rats were made vitamin K-deficient by feeding them a diet devoid of vitamin K and by rigorously preventing coprophagy. After one week, circulating prothrombin concentrations were between 5 and 10% of initial values, and various amounts of phylloquinone, menaquinone-4, and menaquinone-9 were given in a single dose eith...

journal_title：Biochemical pharmacology

authors： Groenen-van Dooren MM,Ronden JE,Soute BA,Vermeer C

更新日期：1995-09-07 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：:Comparison has been made of the effects on brain dopamine function of chronic administration of haloperidol or clozapine to rats for up to 12 months. In rats treated for 1-12 months with haloperidol (1.4-1.6 mg/kg/day), purposeless chewing jaw movements emerged. These movements were only observed after 12 months' trea...

journal_title：Biochemical pharmacology

authors： Rupniak NM,Hall MD,Mann S,Fleminger S,Kilpatrick G,Jenner P,Marsden CD

更新日期：1985-08-01 00:00:00

abstract：:Purification of functional nucleoside transporters has been hampered by the instability of detergent-solubilized proteins. The present study was undertaken to determine if the presence of specific transporter ligands in the solubilization medium could enhance the functional stability of the isolated proteins. Ehrlich ...

journal_title：Biochemical pharmacology

authors： Hammond JR

更新日期：1997-03-07 00:00:00

abstract：:A number of tumour cells, including Ehrlich ascites tumour cells (EATC), possess a polyamine uptake system which selectively accumulates endogenous polyamines and structurally related compounds by an active energy dependent system(s). We suggest that it may be possible to utilize this uptake system to target certain c...

journal_title：Biochemical pharmacology

authors： Holley J,Mather A,Cullis P,Symons MR,Wardman P,Watt RA,Cohen GM

更新日期：1992-02-18 00:00:00

abstract：:The peroxisome proliferator activated receptor-γ (PPAR-γ) is involved in the pathogenesis of diabetic retinopathy. Diabetic retinopathy is a preventable microvascular diabetic complication that damages human retinal pigment epithelial cells. Taurine is abundant in the fruit of Lycium barbarum (Goji Berry), and is repo...

journal_title：Biochemical pharmacology

authors： Song MK,Salam NK,Roufogalis BD,Huang TH

更新日期：2011-11-01 00:00:00

abstract：:We have investigated the effects of fatty acids on the Na+-H+ exchanger and other carrier-mediated transport systems in intestinal brush-border membrane vesicles. The Na+-H+ exchanger (i.e. H+ gradient-dependent, dimethylamiloride-sensitive Na+ uptake) was strongly inhibited by fatty acids and the inhibition was conce...

journal_title：Biochemical pharmacology

authors： Tiruppathi C,Miyamoto Y,Ganapathy V,Leibach FH

更新日期：1988-04-01 00:00:00

abstract：:The present study investigated the presence of ryanodine receptors in the trematode Schistosoma mansoni. [3H]Ryanodine specific binding sites were found in the four subcellular fractions of S. mansoni; however, more binding sites were recovered in the heterogeneous fraction P1 and the microsomal fraction P4, as was th...

journal_title：Biochemical pharmacology

authors： Silva CL,Cunha VM,Mendonça-Silva DL,Noël F

更新日期：1998-10-15 00:00:00

abstract：:The C-18 hydroxy fatty acids ricinelaidic acid and ricinoleic acid diminish the oleic acid-stimulated agonist benzodiazepine binding in the rat brain in vitro. The oleic acid-induced enhancement of [3H]diazepam binding was completely abolished in membranes from the cerebellum, but only partially decreased in membranes...

journal_title：Biochemical pharmacology

authors： Witt MR,Nielsen M

更新日期：1994-02-11 00:00:00

abstract：:The lack of effective chemotherapies in hepatocellular carcinoma (HCC) is still an unsolved problem and underlines the need for new strategies in liver cancer treatment. In this study, we present a novel approach to improve the efficacy of Sorafenib, today's only routinely used chemotherapeutic drug for HCC, in combin...

journal_title：Biochemical pharmacology

authors： Lange M,Abhari BA,Hinrichs TM,Fulda S,Liese J

更新日期：2016-10-15 00:00:00

abstract：:We analysed how interactions between protein kinase-dependent intracellular signalling pathways were implicated in the control of the production of tissue-type plasminogen activator (tPA) and the generation of neurite outgrowth by PC12 cells. To that aim, cells were treated with agents that interact with the trk recep...

journal_title：Biochemical pharmacology

authors： Leprince P,Bonvoisin C,Rogister B,Mazy-Servais C,Moonen G

更新日期：1996-11-08 00:00:00

abstract：:We have shown previously that acetaldehyde forms stable covalent adducts with tubulin, resulting in impaired microtubule formation. The present study explored the mechanism responsible for impaired microtubule formation caused by the substoichiometric stable binding of acetaldehyde to tubulin. The free tubulin dimer w...

journal_title：Biochemical pharmacology

authors： Smith SL,Jennett RB,Sorrell MF,Tuma DJ

更新日期：1992-07-07 00:00:00

abstract：:Most in vivo studies demonstrating decreased activities of hepatic cytochromes P450 with inflammation have used Gram-negative bacterial lipopolysaccharide (LPS) as the inflammatory stimulant. But products of Gram-positive bacteria, such as staphylococcal enterotoxin B (SEB), also stimulate inflammatory mediators, albe...

journal_title：Biochemical pharmacology

authors： Shedlofsky SI,Tosheva RT,Snawder JA

更新日期：2000-05-15 00:00:00

abstract：:Membranes of neuroblastoma N1E-115 cells contain a specific protein carboxyl methyltransferase that methylates a 70 kD protein and a group of 21-23 kD proteins which are tightly bound to the membranes. The enzyme catalyzes the transfer of [methyl-3H] groups from [methyl-3H]S-adenosyl-L-methionine (Km = 0.22 microM) to...

journal_title：Biochemical pharmacology

authors： Haklai R,Kloog Y

更新日期：1990-09-15 00:00:00

abstract：:25-Hydroxycholesterol stimulated acyl-CoA:cholesterol acyltransferase (ACAT) activity in rat liver microsomes in vitro with half-maximal stimulation at 16.8 microM oxysterol and a maximal activity that was three times that in its absence. The current study was conducted to determine the effect of 25-hydroxycholesterol...

journal_title：Biochemical pharmacology

authors： Bhuvaneswaran C,Synouri-Vrettakou S,Mitropoulos KA

更新日期：1997-01-10 00:00:00

abstract：:The substrate specificity of highly purified pig liver catechol-O-methyltransferase has been investigated kinetically. This enzyme shows stereospecificity towards the naturally occurring L-isomer of 3,4-dihydroxyphenylalanine (DOPA) which has a higher affinity and maximal velocity as a substrate than the D-form. We ha...

journal_title：Biochemical pharmacology

authors： Gordonsmith RH,Raxworthy MJ,Gulliver PA

更新日期：1982-02-01 00:00:00

abstract：:Studies have shown that CYP2C9.1 mediated metabolism of flurbiprofen or naproxen is activated by co-incubation with dapsone. However, dapsone activation has not been examined in the known variant forms of CYP2C9. Six concentrations of flurbiprofen (2-300microM) or naproxen (10-1800 microM) were co-incubated with six c...

journal_title：Biochemical pharmacology

authors： Hummel MA,Dickmann LJ,Rettie AE,Haining RL,Tracy TS

更新日期：2004-05-15 00:00:00

abstract：:3 alpha-Hydroxysteroid dehydrogenase (EC 1.1.1.50) of rat liver cytosol catalyzes the second step in glucocorticoid metabolism, namely the NADPH-dependent reduction of 5 beta-dihydrocortisol to tetrahydrocortisol. The purified enzyme is potently inhibited by the nonsteroidal anti-inflammatory drugs [Penning and Talala...

journal_title：Biochemical pharmacology

authors： Penning TM

更新日期：1986-12-01 00:00:00

abstract：:This study demonstrates that the exposure of phenobarbitone-treated rats to halothane at an oxygen concentration of either 10% or 14% results in marked decreases in cytochrome P-450 content and aminopyrine demethylase activity in animals sacrificed from 1 to 48 hr post-exposure. The alterations observed in the hepatic...

journal_title：Biochemical pharmacology

authors： Knights KM,Gourlay GK,Cousins MJ

更新日期：1987-03-15 00:00:00

abstract：:The dithiol-reducing thioredoxin/thioredoxin reductase system normally maintains the reduced state of key enzymes responsible for the cell's anti-oxidant defences. We therefore addressed the question of whether AW 464--a novel thioredoxin inhibitor--as well as broad spectrum dithiol ligands diamide and phenylarsine ox...

journal_title：Biochemical pharmacology

authors： Pallis M,Bradshaw TD,Westwell AD,Grundy M,Stevens MF,Russell N

更新日期：2003-11-01 00:00:00

abstract：:2,3,7,8-Tetrachlorodibenzo-p-dioxin (TCDD) is a widespread environmental pollutant, which causes a variety of severe health effects, e.g. immunosuppression, hepatotoxicity, and carcinogenesis. The main mediator of TCDD toxicity is the arylhydrocarbon receptor (AhR), which, upon activation, translocates into the nucleu...

journal_title：Biochemical pharmacology

authors： Haarmann-Stemmann T,Bothe H,Abel J

更新日期：2009-02-15 00:00:00

abstract：:The effects of ticlopidine and six of its analogues on mitochondrial functions were studied in isolated rat liver mitochondria. The influence of ticlopidine and each of the following analogues: PCR 5325, PCR 4099, PCR 3787, PCR 2362, PCR 4499 and PCR 0665 was evaluated by determining their interaction with three major...

journal_title：Biochemical pharmacology

authors： Abou-Khalil WH,Lim LO,Yunis AA,Abou-Khalil S

更新日期：1984-12-01 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：:Within the tissue surrounding the necrotic lesion, following a cryogenic injury of the brain, there is a definite activation of phospholipase A2 (at 2 and 4 hr post lesion) that accounts, at least in part, for the phospholipid breakdown. There is also an activation of cholinephosphotransferase (at 2 hr post lesion) th...

journal_title：Biochemical pharmacology

authors： Arrigoni E,Averet N,Cohadon F

更新日期：1987-11-01 00:00:00

abstract：:Activation of protein kinase C (PKC) has been suggested to play a role in bone resorption. However, phorbol esters, which activate PKC, have been reported to have both stimulatory and inhibitory effects on bone resorption. To study the role of PKC in bone resorption further, we have measured calcium release elicited b...

journal_title：Biochemical pharmacology

authors： Lee SK,Stern PH

更新日期：2000-10-01 00:00:00

abstract：:The elimination and metabolism of a single dose (100 mg/kg) of 2,4-dinitrotoluene (2,4-DNT) in A/J mice were examined. After intraperitoneal administration, elimination was rapid, with 70% of the dose appearing in the urine within 4 hr. Four hours after oral administration, only 28.5% of the dose was excreted in the u...

journal_title：Biochemical pharmacology

authors： Schut HA,Dixit R,Loeb TR,Stoner GD

更新日期：1985-04-01 00:00:00

abstract：:Alzheimer disease (AD) is a progressive neurodegenerative disorder characterized by severe cognitive impairment, inability to perform activities of daily living and mood changes. Statins, long known to be beneficial in conditions where dyslipidemia occurs by lowering serum cholesterol levels, also have been proposed f...

journal_title：Biochemical pharmacology

authors： Barone E,Di Domenico F,Butterfield DA

更新日期：2014-04-15 00:00:00