abstract：:The reactivities of sulfite (SO23-) with DNA in the presence of metal ions were investigated by a DNA sequencing technique using 32P-labeled DNA fragments obtained from human c-Ha-ras-1 protooncogene. Sulfite caused DNA damage in the presence of Co2+, Cu2+ and Mn2+, although sulfite alone or metal ion alone did not. T...

journal_title：Biochemical pharmacology

authors： Kawanishi S,Yamamoto K,Inoue S

更新日期：1989-10-15 00:00:00

abstract：:The abilities of lipophilic cannabinoid drugs to regulate adenylate cyclase activity in neuroblastoma cell membranes were analyzed by thermodynamic studies. Arrhenius plots of hormone-stimulated adenylate cyclase activity exhibited a break point at 20 degrees. The break point was reduced to 14 degrees by benzyl alcoho...

journal_title：Biochemical pharmacology

authors： Howlett AC,Scott DK,Wilken GH

更新日期：1989-10-01 00:00:00

abstract：:Cells commonly resist growth inhibition by purine and pyrimidine bases and nucleosides by restricting intracellular formation of the corresponding 5'-mononucleotides. Nucleotide derivatives that can act as effective membrane-transport precursors of the poorly membrane-permeable nucleotides have not been identified so ...

journal_title：Biochemical pharmacology

authors： Freed JJ,Farquhar D,Hampton A

更新日期：1989-10-01 00:00:00

abstract：:The in vitro metabolic ketone reduction of warfarin and its 4'-analogues acenocoumarol (4'-nitrowarfarin) and 4'-chlorowarfarin has been investigated using microsomal and cytosolic fractions of several species. Both subcellular fractions showed ketone reductase activity. The cytosolic fractions, in most species, exhib...

journal_title：Biochemical pharmacology

authors： Hermans JJ,Thijssen HH

更新日期：1989-10-01 00:00:00

abstract：:The formation of morphine glucuronides is enantio- and regioselective in rats and humans. In rat liver microsomes, natural (-)-morphine formed only the 3-O-glucuronide, whereas the unnatural (+)-morphine formed glucuronides at both the 3-OH and 6-OH positions, with the 6-O-glucuronide being the principal product. In h...

journal_title：Biochemical pharmacology

authors： Coughtrie MW,Ask B,Rane A,Burchell B,Hume R

更新日期：1989-10-01 00:00:00

abstract：:Several hepatotoxic agents with varied chemical mechanisms of toxicity (acetaminophen, diquat, and CCl4) depress membrane calcium pumps and/or enhance the permeability of membranes to calcium. To probe the relevance of these findings to maintenance of calcium homeostasis after toxins in vivo, we measured the activity ...

journal_title：Biochemical pharmacology

authors： Tsokos-Kuhn JO

更新日期：1989-09-15 00:00:00

abstract：:The beta 2-adrenoceptor agonist, clenbuterol (initially 5 mg/kg), was found to significantly reduce plasma tyrosine and raise brain tryptophan levels (P less than 0.01). By comparison, decreases in plasma tryptophan and increases in brain tyrosine were small and often nonsignificant. Amino acid levels measured in diff...

journal_title：Biochemical pharmacology

authors： Edwards DJ,Sorisio DA,Knopf S

更新日期：1989-09-15 00:00:00

abstract：:The effects on metabolism of the fluorinated dicarboxylic acid, perfluorosuccinate, were examined in hepatocytes from fasted rats. Perfluorosuccinate (5 mM) inhibited gluconeogenesis from lactate by 80% and from pyruvate by 40%. Significant inhibition (up to 30%) occurred at a concentration of perfluorosuccinate of 50...

journal_title：Biochemical pharmacology

authors： Gregory RB,Berry MN

更新日期：1989-09-01 00:00:00

abstract：:Cannabidiol (CBD) has been shown to inhibit mouse hepatic mixed-function oxidations of several drugs after acute treatment, whereas repetitive treatment resulted in the restoration of drug-metabolizing capabilities. We have found that acute CBD treatment modestly decreased cytochrome P-450 content but markedly decreas...

journal_title：Biochemical pharmacology

authors： Bornheim LM,Correia MA

更新日期：1989-09-01 00:00:00

abstract：:A selected number of 1,3-diaminobenzo[f]quinazolines and 1,3-diamino-5,6-dihydrobenzo[f]quinazolines, which may be viewed as tricyclic analogues of the lipid-soluble antifolates pyrimethamine (PM), metoprine (DDMP), and etoprine (DDEP), were tested as inhibitors of purified dihydrofolate reductase (DHFR) from WI-L2 ly...

journal_title：Biochemical pharmacology

authors： Rosowsky A,Freisheim JH,Hynes JB,Queener SF,Bartlett M,Smith JW,Lazarus H,Modest EJ

更新日期：1989-08-15 00:00:00

abstract：:Diazepam (DZ), N-desmethyl diazepam (NOR) and temazepam (TEM) were used as substrates in drug metabolism studies to characterize the changes in cytochrome P-450 mono-oxygenase pathways in hepatocytes isolated from cynomolgus monkeys, during culture for 6 days. Hepatocytes were incubated with DZ (20 microM), NOR (6 mic...

journal_title：Biochemical pharmacology

authors： Seddon T,Lockwood GF,Chenery RJ

更新日期：1989-08-15 00:00:00

abstract：:The effects of 2,5-hexanedione (2,5 HD) on skeletal proteins of red blood cells (RBCs) were investigated both in vitro (human RBCs) and in vivo in male Sprague-Dawley rats which had been treated with the drug for several days. We found that 2,5 HD induced the following major changes in the electrophoretic pattern of t...

journal_title：Biochemical pharmacology

authors： Mallozzi C,Scorza G,Frontali N,Minetti M

更新日期：1989-08-15 00:00:00

abstract：:Bezafibrate is one of the main drugs used in the treatment of human hyperlipemic diseases. Its action on the biosynthesis of fatty acids has been studied and the following conclusions have been drawn: (1) Lipogenesis from glucose is inhibited in hepatocytes and adipocytes isolated from "refed" rats previously treated ...

journal_title：Biochemical pharmacology

authors： Villanueva C,Fabregat I,Machado A

更新日期：1989-08-01 00:00:00

abstract：:Rats were killed after 6 weeks of continuous ingestion of the pneumotoxic alkaloid monocrotaline (2.2 mg/kg/day), the neutrophil elastase inhibitor SC39026 (60 mg/kg/day), or both. Pulmonary reactions were evaluated by light and electron microscopy. Lung endothelial function was monitored by angiotensin converting enz...

journal_title：Biochemical pharmacology

authors： Molteni A,Ward WF,Ts'ao CH,Hinz JM

更新日期：1989-08-01 00:00:00

abstract：:gamma-Aminobutyric acid (GABA) uptake was studied in bovine chromaffin cells maintained in primary culture. Uptake was found to be dependent on Na+, but not on K+ and Ca2+ ions; it was found that 2 Na+ ions were necessary for each molecule of GABA transported. 2,4-Dinitrophenol, ouabain and vanadate inhibited GABA upt...

journal_title：Biochemical pharmacology

authors： Oset-Gasque MJ,Aunis D

更新日期：1989-07-15 00:00:00

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 inhibitory effects of anion channel blockers were evaluated on aggregation, intracellular Ca2+ rises, and the production of arachidonic acid metabolites in human platelets. Inhibitors included five anion channel blockers: phloretin, probenecid, pyridoxal phosphate, 4,4'-diisothiocyano-2,2'-disulfonic acid stilbene...

journal_title：Biochemical pharmacology

authors： Ozaki Y,Matsumoto Y,Yatomi Y,Higashihara M,Kariya T,Shoji K

更新日期：1989-07-01 00:00:00

abstract：:The partition coefficients (Kp) of three prototype Ca2+ antagonists, nitrendipine, (-)-desmethoxyverapamil and flunarizine were determined in native synaptic plasma membranes (SPM) isolated from sheep brain cortex and in liposomes prepared with the total lipids extracted from the membranes. We found that at 25 degrees...

journal_title：Biochemical pharmacology

authors： Carvalho CM,Oliveira CR,Lima MP,Leysen JE,Carvalho AP

更新日期：1989-07-01 00:00:00

abstract：:In a previous study, we demonstrated that the serum of rats treated chronically with the anticancer agent Adriamycin contains lipid peroxides associated with neutral lipids (W. S. Thayer, Biochem Pharmacol 33: 2259-2263, 1984). In the present study, hearts from untreated control rats were perfused with medium containi...

journal_title：Biochemical pharmacology

authors： Thayer WS

更新日期：1989-06-15 00:00:00

abstract：:Short-term agonist-induced loss of cell surface muscarinic receptors and desensitization of receptor-mediated cyclic GMP (cGMP) formation and phosphoinositide hydrolysis were examined in mouse neuroblastoma cells (clone N1E-115) in suspension. This treatment resulted in a time-dependent reduction of approximately 40% ...

journal_title：Biochemical pharmacology

authors： Cioffi CL,el-Fakahany EE

更新日期：1989-06-01 00:00:00

abstract：:The effect of the calcium channel blocker verapamil (VRP) on the accumulation and retention of vincristine (VCR) has been examined in mice bearing xenografts of human rhabdomyosarcomas. The tumors were Rh18, moderately sensitive to VCR, and its subline, Rh18/VCR3, selected in vivo for primary resistance to VCR. Admini...

journal_title：Biochemical pharmacology

authors： Horton JK,Thimmaiah KN,Houghton JA,Horowitz ME,Houghton PJ

更新日期：1989-06-01 00:00:00

abstract：:The effect of ifosfamide and its metabolites on intracellular levels of glutathione in P388 cells in vitro has been studied. It is demonstrated that glutathione depletion occurs only in the presence of 4-hydroperoxyifosfamide and chloroacetaldehyde. In contrast isophosphoramide mustard had no effect on glutathione lev...

journal_title：Biochemical pharmacology

authors： Lind MJ,McGown AT,Hadfield JA,Thatcher N,Crowther D,Fox BW

更新日期：1989-06-01 00:00:00

abstract：:Glucose metabolism and hemoglobin reactivity in intact human erythrocytes were assessed in the presence of the tryptophan metabolites, 3-hydroxyanthranilate (3-HAT), quinolinate and picolinate. Of these compounds, only 3-HAT altered red cell oxidative status by inducing, in a dose-dependent manner, formation of methem...

journal_title：Biochemical pharmacology

authors： Dykens JA,Sullivan SG,Stern A

更新日期：1989-05-15 00:00:00

abstract：:Foetal rat whole brain reaggregate cultures were prepared in a serum-supplemented (S+) or serum-free medium (S-). Ethylcholine mustard aziridinium (ECMA) was added to the cultures at 9 days in vitro (DIV) at concentrations of 12.5, 25 or 50 microM. Choline acetyltransferase (ChAT) activity was measured at +2, +48 and ...

journal_title：Biochemical pharmacology

authors： Atterwill CK,Collins P,Meakin J,Pillar AM,Prince AK

更新日期：1989-05-15 00:00:00

abstract：:The biological effects of 1-methyl-2-nitrosoimidazole (INO), the 2 electron reduction product of biologically active 1-methyl-2-nitroimidazole, were examined in HT-29 human colon cancer cells by clonogenic assay and glutathione (GSH) determination. INO was very toxic towards HT-29 cells and was equally toxic under aer...

journal_title：Biochemical pharmacology

authors： Mulcahy RT,Gipp JJ,Ublacker GA,Panicucci R,McClelland RA

更新日期：1989-05-15 00:00:00

abstract：:The activities of the xenobiotic metabolizing enzymes, aldehyde oxidase and xanthine oxidase, were determined in partially purified fractions of adult guinea-pig liver at given times in the day or night. A marked circadian variation in aldehyde oxidase activity was observed with several substrates (phthalazine, phenan...

journal_title：Biochemical pharmacology

authors： Beedham C,Padwick DJ,al-Tayib Y,Smith JA

更新日期：1989-05-01 00:00:00

abstract：:Treatment of human, peripheral blood neutrophils with gamma-interferon both "primed" their ability to generate reactive oxidants and increased their rate of protein synthesis. This increased rate of protein synthesis was greatest 60 min after the addition of 100 U/ml gamma-interferon and was not due to an increased in...

journal_title：Biochemical pharmacology

authors： Humphreys JM,Hughes V,Edwards SW

更新日期：1989-04-15 00:00:00

abstract：:We tested the ability of a wide variety of organic compounds, including benzene and phenol derivatives, aromatic amines, pyrazoline derivatives and other non-steroidal anti-inflammatory drugs, to act as cosubstrates during the horseradish peroxidase/hydrogen peroxide-mediated oxygenation of arachidonic acid. Structura...

journal_title：Biochemical pharmacology

authors： Lehmann FM,Bretz N,von Bruchhausen F,Wurm G

更新日期：1989-04-15 00:00:00

abstract：:The inductive effects of phenobarbitone (PB) and 1,4-bis[2-(3,5-dichloropyridyloxy)]benzene (TCPOBOP) were compared in C57BL/6J mice. Induction parameters included six substrates: ethylmorphine (EM), benzphetamine (Bph), biphenyl, ethoxycoumarin (EtoC), pentoxyresorufin and dichloro-p-nitroanisole (DPNA). In order to ...

journal_title：Biochemical pharmacology

authors： Heubel F,Reuter T,Gerstner E

更新日期：1989-04-15 00:00:00

abstract：:Rat liver microsomal 4-hydroxycoumarin binding was studied by assaying specific [14C]warfarin binding. Microsomes of warfarin-sensitive rats contained about 40 pmole of specific binding sites per mg of microsomal protein. There was no difference for R- or S-[14C]warfarin. Neither was there any difference between the e...

journal_title：Biochemical pharmacology

authors： Thijssen HH,Baars LG

更新日期：1989-04-01 00:00:00

abstract：:Microsomal and cytosolic epoxide hydrolase (mEH and cEH respectively) and glutathione S-transferase (GST) activities were measured in the liver, kidney, and gills of rainbow trout. Assays were optimized for time, pH, and temperature, using trans-stilbene oxide (TSO) and cis-stilbene oxide (CSO) as substrates for cEH a...

journal_title：Biochemical pharmacology

authors： Laurén DJ,Halarnkar PP,Hammcock BD,Hinton DE

更新日期：1989-03-15 00:00:00

abstract：:Cephaloridine and cephaloglycin are the two most nephrotoxic cephalosporins released for human use. Cephaloridine has been shown to produce both oxidative and mitochondrial respiratory injury in renal cortex in patterns of dose (or concentration) and time that are consistent with pathogenicity. Cephaloglycin also prod...

journal_title：Biochemical pharmacology

authors： Tune BM,Fravert D,Hsu CY

更新日期：1989-03-01 00:00:00

abstract：:The dopamine (D2) receptor blocking property of antipsychotic medications has been proposed as the mechanism of the therapeutic activity of this class of drugs. This property has also been exploited as a method to quantify therapeutic levels of these drugs in patients. However, the lack of correlation among dosage, bl...

journal_title：Biochemical pharmacology

authors： Hoffman DW,Shillcutt SD,Edkins RD

更新日期：1989-03-01 00:00:00

abstract：:Binding of the selective D-1 dopamine receptor ligand 125I SCH 23982 was studied using crude plasma membranes derived from human renal cortex. 125I SCH 23982 bound saturably to a single high affinity site (Kd = 650 pM, Bmax = 19 fmol/mg protein). Binding at 37 degrees was rapid and reversible with forward and reverse ...

journal_title：Biochemical pharmacology

authors： Hughes A,Sever P

更新日期：1989-03-01 00:00:00

abstract：:In this study, using a combination of immunological and enzymatic characterizations, we compared the forms of cytochrome P-450 induced by ethanol and glutethimide in primary cultures of chicken embryo hepatocytes. Recently we purified a cytochrome P-450 of 50K molecular weight from chicken embryo liver using glutethim...

journal_title：Biochemical pharmacology

authors： Sinclair JF,Wood SG,Smith EL,Sinclair PR,Koop DR

更新日期：1989-02-15 00:00:00

abstract：:The extraction and partial purification of endogenous "monoamine oxidase (MAO) inhibitor-like" material from the monkey brain are described. The endogenous material (F-1 and F-2) obtained after Bio-Gel P-2 gel filtration and silica column chromatography inhibited MAO in the monkey brain mitochondria toward 5-hydroxytr...

journal_title：Biochemical pharmacology

authors： Egashira T,Obata T,Nagai T,Kimba Y,Takano R,Yamanaka Y

更新日期：1989-02-15 00:00:00

abstract：:Fetal bovine serum acetylcholinesterase (FBS-AChE, EC 3.1.1.7) was titrated, both in vitro and in vivo, with a highly toxic anti-ChE organophosphate, 7-(methylethoxyphosphinyloxy)-1-methyl-quinolinium iodie (MEPQ). Approximately 1:1 stoichiometry was obtained for the sequestration of MEPQ by FBS-AChE in mice. A quanti...

journal_title：Biochemical pharmacology

authors： Raveh L,Ashani Y,Levy D,De La Hoz D,Wolfe AD,Doctor BP

更新日期：1989-02-01 00:00:00

abstract：:Diethyldithiocarbamate-methyl ester (DDTC-Me), a metabolite of disulfiram, has been shown recently to produce a disulfiram-ethanol reaction (DER). Studies were carried out to compare the ethanol-sensitizing properties of DDTC-Me with those of disulfiram and diethyldithiocarbamate (DDTC) in the rat. All three drugs inh...

journal_title：Biochemical pharmacology

authors： Yourick JJ,Faiman MD

更新日期：1989-02-01 00:00:00

abstract：:P-450-male is a male specific form of cytochrome P-450 in rat liver microsomes. Cytochrome P-450 crossreactive with anti-P-450-male antibodies was purified to an electrophoretical homogeneity from liver microsomes of male beagle dogs. The specific content of the purified cytochrome P-450 (P-450-D1) was 16.9 nmol/mg pr...

journal_title：Biochemical pharmacology

authors： Komori M,Shimada H,Miura T,Kamataki T

更新日期：1989-01-15 00:00:00

abstract：:Rats fed 1% paracetamol in the diet failed to grow and a dose-dependent inhibition of growth was observed and found to be independent of hepatoxicity. Addition of 0.5% D- or L-methionine, or L-cysteine to a diet containing 1% paracetamol restored growth. Addition of L-methionine to the drinking water was equally effec...

journal_title：Biochemical pharmacology

authors： McLean AE,Armstrong GR,Beales D

更新日期：1989-01-15 00:00:00