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：:A series of N-hydroxy-N'-aminoguanidine derivatives was studied for their effects on L1210 cell growth and ribonucleotide reductase activity. With the twelve compounds studied, there was a good correlation between the inhibition of L1210 cell growth and the inhibition of ribonucleotide reductase activity. The most pot...

journal_title：Biochemical pharmacology

authors： Cory JG,Carter GL,Bacon PE,T'ang A,Lien EJ

更新日期：1985-08-01 00:00:00

abstract：:The 2-hydroxylation of desmethylimipramine (DMI) correlates strongly with the 4-hydroxylation of debrisoquine (D) both in human volunteers and in vitro comparing human liver microsomes from different individuals. D competitively inhibits the 2-hydroxylation of DMI in vitro suggesting that DMI is hydroxylated by the 'd...

journal_title：Biochemical pharmacology

authors： von Bahr C,Spina E,Birgersson C,Ericsson O,Göransson M,Henthorn T,Sjöqvist F

更新日期：1985-07-15 00:00:00

abstract：:During attempts to isolate and identify an endogenous ligand for the glycoside binding sites on Na+,K+-ATPase, bovine adrenal glands were found to contain a potent inhibitor of isolated Na+,K+-ATPase. The inhibitory principle was extracted from adrenal cortex, following homogenization in NaHCO3 solution and separation...

journal_title：Biochemical pharmacology

authors： Ng YC,Akera T,Han CS,Braselton WE,Kennedy RH,Temma K,Brody TM,Sato PH

更新日期：1985-07-15 00:00:00

abstract：:The effects of nicardipine on sodium-calcium exchange activity of cardiac sarcolemma-enriched vesicles isolated from the rat heart were examined. Sodium-loaded, sarcolemma-enriched vesicles, when exposed to a medium containing 40 microM CaCl2, exhibited about 5 nmoles Ca2+/mg protein of the maximal calcium uptake; the...

journal_title：Biochemical pharmacology

authors： Takeo S,Adachi K,Sakanashi M

更新日期：1985-07-01 00:00:00

abstract：:A method is presented that determines the degree of attachment of cancer cells to normal cells. This method may be useful in determining the extent to which treatment of normal cells (or of a tumor-bearing host) with a particular chemotherapeutic agent may affect the degree of attachment of cancer cells to the normal ...

journal_title：Biochemical pharmacology

authors： Elliott RE,Karadsheh NS,Kole J,Canellakis ES

更新日期：1985-06-15 00:00:00

abstract：:The binding of [3H]nitrendipine to rat cortical membranes was reduced by phenytoin, phenobarbital, and pentobarbital. The IC50 values were 0.09, 0.40, and 0.76 mM respectively. The drugs reduced the apparent binding affinity of [3H]nitrendipine with little effect on the maximum number of binding sites. The inhibitory ...

journal_title：Biochemical pharmacology

authors： Harris RA,Jones SB,Bruno P,Bylund DB

更新日期：1985-06-15 00:00:00

abstract：:The stimulated uptake of 45Ca2+ into incubated cerebrocortical synaptosomes caused by veratrine (75 microM) was blocked by low concentrations of verapamil (0.5-30 microM) which did not prevent or reduce depolarization as judged by efflux of potassium (K+). However, verapamil did not prevent amino acid neutrotransmitte...

journal_title：Biochemical pharmacology

authors： Norris DK,Bradford HF

更新日期：1985-06-01 00:00:00

abstract：:Three grams of nafazatrom (Bay g 6575), given orally to healthy male volunteers in a single dose, significantly reduce the formation of leukotriene B4 in polymorphonuclear leukocytes. LTB4 synthesis fell from 57.1 +/- 17.0 ng/10(7) PMNL, mean +/- S.D., in control to 34.3 +/- 14.4 ng/10(7) PMNL 3 hr after nafazatrom (2...

journal_title：Biochemical pharmacology

authors： Strasser T,Fischer S,Weber PC

更新日期：1985-06-01 00:00:00

abstract：:5-Substituted-2,2'-anhydrouridines are a new class of competitive inhibitors of uridine phosphorylase. The most potent member of the series is 2,2'-anhydro-5-ethyluridine with an apparent Ki value of 25 nM. These compounds are selective inhibitors of uridine phosphorylase and have no effect on thymidine phosphorylase....

journal_title：Biochemical pharmacology

authors： Veres Z,Szabolcs A,Szinai I,Dénes G,Kajtár-Peredy M,Otvös L

更新日期：1985-05-15 00:00:00

abstract：:Incubation of adriamycin resistant Chinese hamster lung cells with the calmodulin inhibitor trifluoperazine (TFP) resulted in a significant increase in the cellular accumulation of drug. When resistant cells were prelabeled with 32Pi and then treated with TFP, a major increase also occurred in the phosphorylation of a...

journal_title：Biochemical pharmacology

authors： Center MS

更新日期：1985-05-01 00:00:00

abstract：:When rat peritoneal leucocytes were incubated with carbon tetrachloride, a PLA2 was activated, eicosanoids were generated and lysosomal and cytoplasmic enzymes were released. The predominant eicosanoid generated was TXB2 with lesser amounts of PGE2, 6-keto PGF1 alpha and LTB4. Preincubation of the cells with two struc...

journal_title：Biochemical pharmacology

authors： Lynch TJ,Blackwell GJ,Moncada S

更新日期：1985-05-01 00:00:00

abstract：:Glutathione (GSH) is important in protection of cells against electrophilic drug injury and against reactive oxygen species. Both steady-state concentrations and turnover of GSH are important determinants of susceptibility of the hepatocyte to injury. Chronic ethanol administration is known to enhance susceptibility t...

journal_title：Biochemical pharmacology

authors： Morton S,Mitchell MC

更新日期：1985-05-01 00:00:00

abstract：:The microsomal brush-border fraction of rat renal tissue contains enzymatic activity, optimally active at pH 9, that is capable of degrading human myelin basic protein (BP) peptide 43-88. In the present study, this degradation and the effect on it of selected drugs and hormones were examined further. Of the substances...

journal_title：Biochemical pharmacology

authors： Trestman RL,Heinemann MA,Whitaker JN,Seyer JM

更新日期：1985-04-15 00:00:00

abstract：:Two radiolabelled derivatives of deferrioxamine B (DF) have been synthesized: methyl-DF and acetyl-DF. Both derivatives are non cytotoxic and stable in cell culture but they are degraded in human plasma and more extensively in rat plasma. Methyl-DF, acetyl-DF and DF mobilize radioiron to the same extent from hepatocyt...

journal_title：Biochemical pharmacology

authors： Laub R,Schneider YJ,Octave JN,Trouet A,Crichton RR

更新日期：1985-04-15 00:00:00

abstract：:The effects of injections of a synthetic adrenocorticotropin (ACTH 1-17, Synchrodyn) on the rate of DNA labeling in the metaphyseal bone of CD2F1 mice were tested on a chronopharmacological dosing schedule. Groups of mice that had been conditioned to a 12-hr light/12-hr dark schedule were injected at one of six differ...

journal_title：Biochemical pharmacology

authors： Walker WV,Russell JE,Simmons DJ,Scheving LE,Cornelissen G,Halberg F

更新日期：1985-04-15 00:00:00

abstract：:The effects of two recently developed alpha 2-adrenergic antagonists, RX 781094 and WY 26703, on the synthesis of norepinephrine (NE), dopamine (DA) and serotonin (5-HT) in rat brain were compared to those of yohimbine, its diastereoisomer rauwolscine, and mianserin. Intraperitoneal administration of these compounds i...

journal_title：Biochemical pharmacology

authors： Pettibone DJ,Pfleuger AB,Totaro JA

更新日期：1985-04-01 00:00:00

abstract：:Miconazole and clotrimazole, members of a class of imidazole agents which have broad spectrum antimycotic activity, were shown to be potent inhibitors of steroid aromatase activity of human placental microsomes. The I50 values for the inhibition of aromatase activity by miconazole, clotrimazole, ketoconazole, and amin...

journal_title：Biochemical pharmacology

authors： Mason JI,Murry BA,Olcott M,Sheets JJ

更新日期：1985-04-01 00:00:00

abstract：:Aminoglycoside antibiotics induce a lysosomal phospholipidosis in kidney proximal tubules after conventional therapy in animals and man. We have previously demonstrated that these drugs bind to negatively charged phospholipid bilayers at acid pH and inhibit the activity of lysosomal acid phospholipases in vitro and in...

journal_title：Biochemical pharmacology

authors： Brasseur R,Carlier MB,Laurent G,Claes PJ,Vanderhaeghe HJ,Tulkens PM,Ruysschaert JM

更新日期：1985-04-01 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：:Female Wistar rats were treated with acetaminophen 3.0 g/kg BW and allyl alcohol 75 microliter/kg BW by gastric tube. Hepatic function, measured as galactose elimination capacity and prothrombin index, was reduced to about 0.40 times control value. Plasma alanine transferase activity was elevated more and earlier afte...

journal_title：Biochemical pharmacology

authors： Poulsen HE,Lerche A,Pedersen NT

更新日期：1985-03-15 00:00:00

abstract：:The metabolism of (1R)[1-3H]ethanol, [2-3H]lactate or [2-3H]xylitol was studied in hepatocytes from fed or T3-treated rats in the presence or absence of fructose or xylitol. The yields of tritium in ethanol, lactate, water, glycerol and glucose were determined. A simple model, describing the metabolic fate of tritium ...

journal_title：Biochemical pharmacology

authors： Vind C,Grunnet N

更新日期：1985-03-01 00:00:00

abstract：:We have reported previously that both dietary iron and selenium regulate intestinal cytochrome P-450 content by modulating the synthesis of its prosthetic heme moiety. Whether these elements are required for synthesis and/or viability of its apocytochrome moiety is unknown. We have examined the effects of intraluminal...

journal_title：Biochemical pharmacology

authors： Pascoe GA,Correia MA

更新日期：1985-03-01 00:00:00

abstract：:Administration of pentylenetetrazol (PTZ) (60 mg/kg, s.c.) to normal or carbaryl (200 mg/kg, p.o.) treated adult male albino rats produced characteristic changes in the steady-state levels of striatal dopamine (DA), noradrenaline (NA) and homovanillic acid (HVA) at different time intervals (0.5, 1.0 and 2.0 hr). The e...

journal_title：Biochemical pharmacology

authors： Ray SK,Poddar MK

更新日期：1985-02-15 00:00:00

abstract：:Anaesthetized rabbits were used to study the effect of bromobenzene-induced hepatic damage to the acinar zone 3 on bile flow, bile salt, sodium secretion as well as bilirubin transport in basal conditions or with infusion of sodium glycodeoxycholate. The bromobenzene-pretreated animals exhibited in basal conditions a ...

journal_title：Biochemical pharmacology

authors： González J,Esteller A

更新日期：1985-02-15 00:00:00

abstract：:To investigate the hypothesis that cyclic AMP (cAMP) regulates arachidonic acid metabolism in vascular tissue, we have studied the effects of forskolin (FSK), an activator of adenylate cyclase, and 3-isobutyl-1-methylxanthine (IBMX), a phosphodiesterase inhibitor, on hormone-stimulated prostacyclin (PGI2) synthesis in...

journal_title：Biochemical pharmacology

authors： Whorton AR,Collawn JB,Montgomery ME,Young SL,Kent RS

更新日期：1985-01-01 00:00:00

abstract：:The acute effects of carbon tetrachloride (CCl4) on the membrane structure of rat liver microsomes were studied using 31P-NMR and spin-labeling techniques. 31P-NMR spectra of rat liver microsomes were not changed appreciably after the oral administration of CCl4, indicating that the surface structures of microsomal me...

journal_title：Biochemical pharmacology

authors： Utsumi H,Murayama J,Hamada A

更新日期：1985-01-01 00:00:00

abstract：:The effect of the anti-tumor, anti-glutamine drug acivicin, L-(alpha S,5S)-alpha-amino-3-chloro-4,5-dihydro-5-isoxazoleacetic acid, was determined on the activity of the rate-limiting enzyme of de novo pyrimidine biosynthesis, carbamoyl-phosphate synthetase II (glutamine-hydrolyzing) (EC 6.3.5.5), in human colon carci...

journal_title：Biochemical pharmacology

authors： Sebolt JS,Aoki T,Eble JN,Glover JL,Weber G

更新日期：1985-01-01 00:00:00

abstract：:[3H]Spiperone binding sites were solubilized in high yield from human, dog and rat brain with a mixture of sodium cholate (0.3% w/v) and sodium chloride (1.4 M). The binding sites were not sedimented after one hour at 100,000 g, they passed freely through 0.20 micron filters, migrated as a single peak in gradient sedi...

journal_title：Biochemical pharmacology

authors： Wouters W,van Dun J,Laduron PM

更新日期：1984-12-15 00:00:00

abstract：:The effects of p-chloromercuribenzoate and N-ethylmaleimide were evaluated on the binding of (3H)-p-aminoclonidine, (3H)-rauwolscine and (3H)-prazosin on rat brain alpha-adrenergic receptors. Pretreatment of the particulate fraction with increasing concentrations of p-chloromercuribenzoate indicated that the binding o...

journal_title：Biochemical pharmacology

authors： Quennedey MC,Bockaert J,Rouot B

更新日期：1984-12-15 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：:Piperine and two of its derivatives, antiepilepsirine (AE or 3,4-methylendioxycynnamoylpiperine) and compound 7448 (N-isopropyl 3 (4 chloro-phenyl) propenoylamide) are very effective in stimulating serotonin (5HT) synthesis. AE raises the ratio of free-to-bound tryptophan (TP) in plasma and induces a long-lasting incr...

journal_title：Biochemical pharmacology

authors： Liu GQ,Algeri S,Ceci A,Garattini S,Gobbi M,Murai S

更新日期：1984-12-01 00:00:00

abstract：:The action of nystatin, a polyene antibiotic, was studied in rat myocardial cells, isolated rat hearts, and intact rats. Myocardial cells responded to 10 and 25 micrograms nystatin/ml with arrhythmias that could be minimized by elevated concentrations of K+ and Mg2+ or reversed by washing the cells. Similarly, the iso...

journal_title：Biochemical pharmacology

authors： Aszalos A,Bradlaw JA,Reynaldo EF,Yang GC,El-Hage AN

更新日期：1984-12-01 00:00:00

abstract：:Chortetracycline (CTC) inhibits chemotaxis, exocytosis and metabolic burst in rabbit polymorphonuclear leukocytes (PMNs), when these cells are activated in the absence of extracellular Ca2+. In the presence of extracellular Ca2+ CTC has little or no inhibiting effect on these functions. The inhibiting effect of CTC in...

journal_title：Biochemical pharmacology

authors： Elferink JG,Deierkauf M

更新日期：1984-11-15 00:00:00

abstract：:The microsomal fraction of bone marrow contains cytochrome P-450 (39 +/- 11 pmoles/mg microsomal protein) and monooxygenase activity could be demonstrated by the O-dealkylation of 7-ethoxycoumarin (114 +/- 65 pmoles/(min X mg microsomal protein] and the hydroxylation of benzene to phenol (51 +/- 8.6 pmol/45 min X mg m...

journal_title：Biochemical pharmacology

authors： Gollmer L,Graf H,Ullrich V

更新日期：1984-11-15 00:00:00

abstract：:Eleven naturally occurring flavonoids representing five different chemical classes were studied for their effects on human basophil histamine release triggered by six different stimuli. The flavonoids included flavone, quercetin, taxifolin, chalcone, apigenin, fisetin, rutin, phloretin, tangeretin, hesperetin, and nar...

journal_title：Biochemical pharmacology

authors： Middleton E Jr,Drzewiecki G

更新日期：1984-11-01 00:00:00

abstract：:Cilostamide derivatives are potent inhibitors of human platelet aggregation and selectively inhibit human platelet cyclic adenosine monophosphate (cyclic AMP) phosphodiesterase. N-Cyclohexyl-N-(2-hydroxybutyl)-5-[6-1,2,3,4-tetrahydro-2-oxoquinolyl oxy)] -butyramide (OPC-13135) is one of these derivatives, and the conc...

journal_title：Biochemical pharmacology

authors： Umekawa H,Tanaka T,Kimura Y,Hidaka H

更新日期：1984-11-01 00:00:00

abstract：:Endosulfan (E) is an organochloric insecticide, which is quickly metabolized and eliminated from the body system. Toxic effects of E and its metabolites have been reported. The influence of E and its metabolites, viz. endosulfan sulfate (ES), endosulfan diol (ED) and endosulfan lactone (EL), has been examined on rat l...

journal_title：Biochemical pharmacology

authors： Dubey RK,Beg MU,Singh J

更新日期：1984-11-01 00:00:00

abstract：:Administration to hamsters of a highly purified human leukocyte interferon subtype, IFN-alpha A, obtained by recombinant DNA methods, abolished the efficacy of high doses of cyclophosphamide (2.5 mg/hamster) against the TBD 932 lymphosarcoma. The effect was more pronounced with concomitant than with sequential treatme...

journal_title：Biochemical pharmacology

authors： Lee SH,Chiu H,Renton KW,Stebbing N

更新日期：1984-11-01 00:00:00

abstract：:Chronic oral phenobarbital treatment (50 mg/kg every 12 hr for 8 weeks), which was nontoxic and continuously protective against seizures in rats, significantly decreased folate concentration in liver (29%) but not in brain or plasma. The apparent activity of 5,10-methylenetetrahydrofolate reductase (MTR) in liver decr...

journal_title：Biochemical pharmacology

authors： Carl GF,Smith DB

更新日期：1984-11-01 00:00:00