A study of the expression of the xenobiotic-metabolising cytochrome P450 proteins and of testosterone metabolism in bovine liver.

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：:The increase in life expectancy has resulted in a high occurrence of dementia and Alzheimer's disease (AD). Research on AD has undergone a paradigm shift from viewing it as a disease of old age to taking a life course perspective. Several vascular, lifestyle, psychological and genetic risk factors influencing this lat...

journal_title：Biochemical pharmacology

authors： Imtiaz B,Tolppanen AM,Kivipelto M,Soininen H

更新日期：2014-04-15 00:00:00

abstract：:Triapine is an α-N-heterocyclic thiosemicarbazone with promising anticancer activity against hematologic malignancies but widely ineffective against solid tumor types in clinical trials. The anticancer activity of thiosemicarbazones can be dramatically increased by terminal dimethylation. KP1089 is a gallium compound ...

journal_title：Biochemical pharmacology

authors： Heffeter P,Pirker C,Kowol CR,Herrman G,Dornetshuber R,Miklos W,Jungwirth U,Koellensperger G,Keppler BK,Berger W

更新日期：2012-06-15 00:00:00

abstract：:L1210 and K562 leukaemic cells have been used to study the relationship between cytotoxicity and free radical production by two aziridinyl benzoquinones, 2,5-bis(carboethoxyamino)3,6-diaziridinyl-1,4-benzoquinone (AZQ) and 2,5-bis(2-hydroxyethylamino)-3,6-diaziridinyl-1,4-benzoquinone (BZQ). BZQ showed a high level of...

journal_title：Biochemical pharmacology

authors： Lea JS,Garner HJ,Butler J,Hoey BM,Ward TH

更新日期：1988-05-15 00:00:00

abstract：:The effects of sulfobromophthalein (SBP) and ethacrynic acid (ECA), both inhibitors of glutathione S-transferase (GST), or glyceryl trinitrate (GTN)-induced vasorelaxation were investigated in rabbit aortic strips. The aortic strips were pre-contracted with phenylephrine, followed by relaxation with 0.5 microM GTN, wi...

journal_title：Biochemical pharmacology

authors： Lau DT,Benet LZ

更新日期：1992-05-28 00:00:00

abstract：:A critical processing step in endothelin biosynthesis is the conversion of the intermediate "big endothelin" to its biologically active product catalysed by endothelin converting enzyme (ECE). In this commentary we discuss critically the cellular location, structure, and activity of the isoforms of ECE. The current ev...

journal_title：Biochemical pharmacology

authors： Turner AJ,Murphy LJ

更新日期：1996-01-26 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：: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：:The bactericidal effect of metronidazole on Escherichia coli and Bacteroides fragilis can be partially reversed by cysteamine under conditions that lead to the formation of an adduct, the thioether, 4-(2-aminoethyl)thio-2-methylimidazole-1-ethanol (4-ATME). This adduct, which is not mutagenic for the Ames histidine au...

journal_title：Biochemical pharmacology

authors： Yeung TC,Goldman P

更新日期：1983-11-01 00:00:00

abstract：:The effect of methotrexate (MTX) on 6-mercaptopurine (6-MP) metabolism was studied in four human leukemic cell lines in vitro. CCRF-CEM, WI-L2, TBJ, and HL-60 all expressed thiopurine methyltransferase (TPMT) activity. The cells were grown in horse serum-supplemented RPMI 1640 medium to which was added 4 microM of 6-M...

journal_title：Biochemical pharmacology

authors： Giverhaug T,Loennechen T,Aarbakke J

更新日期：1998-05-15 00:00:00

abstract：:The effects of schisanhenol (Sal) on Adriamycin (ADM)-induced rat heart mitochondrial toxicity in vitro were investigated. Malondialdehyde formation, lysis, disintegration and membrane rigidification in mitochondria treated with ADM were reduced significantly by Sal. In the electron spin resonance studies, Sal did not...

journal_title：Biochemical pharmacology

authors： Lin TJ,Liu GT,Pan Y,Liu Y,Xu GZ

更新日期：1991-10-09 00:00:00

abstract：:The aim of the present study was to investigate the effects of myricitrin, a flavonoid with anti-inflammatory and antinociceptive action, upon persistent neuropathic and inflammatory pain. The neuropathic pain was caused by a partial ligation (2/3) of the sciatic nerve and the inflammatory pain was induced by an intra...

journal_title：Biochemical pharmacology

authors： Meotti FC,Missau FC,Ferreira J,Pizzolatti MG,Mizuzaki C,Nogueira CW,Santos AR

更新日期：2006-12-15 00:00:00

abstract：:beta-Antiadrenergic properties are part of the pharmacological characteristics of amiodarone. In the present study, the action of amiodarone on rat-heart beta-adrenoceptors was investigated. [125I]Cyanopindolol (CYP) was used to label beta-adrenoceptors in crude rat-heart microsomes. In competition binding experiments...

journal_title：Biochemical pharmacology

authors： Nokin P,Clinet M,Schoenfeld P

更新日期：1983-09-01 00:00:00

abstract：:This report characterizes the cytochrome P-450 isozyme involved in midazolam metabolism. This study was undertaken into liver microsomal fractions prepared from untreated rabbits or animals treated with drugs known to specifically induce various cytochrome P-450 isozymes such as form LM2 by phenobarbital, LM4 and LM6 ...

journal_title：Biochemical pharmacology

authors： Fabre G,Crevat-Pisano P,Dragna S,Covo J,Barra Y,Cano JP

更新日期：1988-05-15 00:00:00

abstract：:The population growth rate of HeLa cells treated with 60 microM 5,6-dichloro-1-beta-D-ribofuranosylbenzimidazole (DRB) in reinforced Eagle's minimum essential medium was directly related to the concentration of fetal bovine serum in the range from 5 to 30%. Control cells proliferated at a maximal rate (doubling time: ...

journal_title：Biochemical pharmacology

authors： Tamm I

更新日期：1984-02-15 00:00:00

abstract：:The remarkable effects exhibited by classical psychedelics in recent clinical trials have spawned considerable interest in 5-HT2A receptor (5-HT2AR) activation as a treatment strategy for several psychiatric/cognitive disorders. In this study we have continued our development of 25CN-NBOH, one of the most 5-HT2AR-sele...

journal_title：Biochemical pharmacology

authors： Jensen AA,Halberstadt AL,Märcher-Rørsted E,Odland AU,Chatha M,Speth N,Liebscher G,Hansen M,Bräuner-Osborne H,Palner M,Andreasen JT,Kristensen JL

更新日期：2020-07-01 00:00:00

abstract：:Uracil incorporation into DNA occurs under conditions that limit thymidine biosynthesis; uracil is removed by two isoforms of uracil DNA glycosylase (UNG; EC 3.2.2.3), UNG1 and UNG2. We hypothesize that UNG is important in protecting the mid-organogenesis stage [gestational day (GD) 10-12] rat conceptus against condit...

journal_title：Biochemical pharmacology

authors： Vinson RK,Hales BF

更新日期：2002-08-15 00:00:00

abstract：:The interactions of the anticonvulsant drug milacemide (2-n-pentylaminoacetamide) with rat liver mitochondrial monoamine oxidases-A and -B have been studied. The compound acts as a substrate for the B-form of the enzyme, with an apparent Km value of 49 +/- 4.7 microM and a Vmax value of 1.1 +/- 0.2 nmol/min/mg. It is ...

journal_title：Biochemical pharmacology

authors： O'Brien EM,Tipton KF,McCrodden JM,Youdim MB

更新日期：1994-02-11 00:00:00

abstract：:Glutathione (GSH) contributes to the detoxification of anticancer drugs through the operation of specific glutathione S-transferases (GST) and innate, or acquired, overexpression of this enzyme family has been frequently observed in tumor cell lines. In the GMA32 line of Chinese hamster fibroblasts, we showed that GSH...

journal_title：Biochemical pharmacology

authors： Lunel-Orsini C,Buttin G,De Saint Vincent BR

更新日期：1995-01-31 00:00:00

abstract：:The formation of 4-[1,4-13C]hydroxybutyric acid ([13C]gamma-hydroxybutyric acid; [13C]GHB) in rat brain was studied following intracerebroventricular (i.c.v.) administration of either 4-[1,4-13C]aminobutyric acid ([13C]GABA or 1,4-[1,4-13C]butanediol ([13C]1,4-BD) to awake, freely moving animals. GHB and [13C]GHB were...

journal_title：Biochemical pharmacology

authors： Snead OC 3rd,Furner R,Liu CC

更新日期：1989-12-15 00:00:00

abstract：:We have previously reported that Gen-27, a newly synthesized flavonoid, exhibits anticancer effects against human colorectal cancer cells. In this study, we investigated the anticancer effects in human breast cancer cell lines and its underlying mechanisms. We demonstrated that Gen-27 inhibited the growth and prolifer...

journal_title：Biochemical pharmacology

authors： Tao L,Wei L,Liu Y,Ding Y,Liu X,Zhang X,Wang X,Yao Y,Lu J,Wang Q,Hu R

更新日期：2017-02-01 00:00:00

abstract：:The microbial alkaloid staurosporine is a member of a recently described family of protein kinase inhibitors. [N,N-dimethyl-3H]N-dimethylstaurosporine ([3H]DMS) was prepared from staurosporine by methylation with [3H]methyl iodide. Since staurosporine inhibits protein kinase C (PKC) most potently, the binding of [3H]D...

journal_title：Biochemical pharmacology

authors： Gross JL,Herblin WF,Do UH,Pounds JS,Buenaga LJ,Stephens LE

更新日期：1990-07-15 00:00:00

abstract：:The kidney plays an important role in the homeostasis of carnitine by its ability to reabsorb carnitine almost completely from the glomerular filtrate. The transport process responsible for this reabsorption has been investigated thus far only in laboratory animals. Here we report on the characteristics of carnitine u...

journal_title：Biochemical pharmacology

authors： Huang W,Shaikh SN,Ganapathy ME,Hopfer U,Leibach FH,Carter AL,Ganapathy V

更新日期：1999-10-15 00:00:00

abstract：:Autophagy is generally regarded as a mechanism to promote cell survival. However, autophagy can occasionally be the mechanism responsible of cell demise. We have found that a concomitant depletion of glucose, nutrients and growth factors provoked cell death in a variety of cell lines. This death process was contingent...

journal_title：Biochemical pharmacology

authors： Mattiolo P,Yuste VJ,Boix J,Ribas J

更新日期：2015-12-15 00:00:00

abstract：:Vanadate (VO3-) was found to activate adenylyl cyclase (AC) in ocular ciliary process membrane. This response was additive to that of isoproterenol (ISO) and vasoactive intestinal peptide (VIP), but it was potentiative with forskolin (FSK) and also with Ca2+/calmodulin activation of AC activity. The potentiated respon...

journal_title：Biochemical pharmacology

authors： Mittag TW,Guo WB,Taniguchi T

更新日期：1993-03-24 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：:CYP2C19 (formerly known as CYP2C75), highly homologous to human CYP2C19, has been identified in cynomolgus and rhesus macaques, non-human primate species widely used in drug metabolism studies. CYP2C19 is predominantly expressed in liver and encodes a functional drug-metabolizing enzyme. Genetic variants in human CYP2...

journal_title：Biochemical pharmacology

authors： Uno Y,Matsushita A,Shukuya M,Matsumoto Y,Murayama N,Yamazaki H

更新日期：2014-09-15 00:00:00

abstract：:5-Phenylthioacyclouridine (PTAU or 1-[(2-hydroxyethoxy)methyl]-5-phenylthiouracil) was synthesized as a highly specific and potent inhibitor of uridine phosphorylase (UrdPase, EC 2.4.2.3). PTAU has inhibition constant (K(is)) values of 248 and 353 nM towards UrdPase from mouse and human livers, respectively. PTAU was ...

journal_title：Biochemical pharmacology

authors： el Kouni MH,Goudgaon NM,Rafeeq M,Al Safarjalani ON,Schinazi RF,Naguib FN

更新日期：2000-09-15 00:00:00

abstract：:Enhanced aggregation of platelets was observed in platelet-rich plasma, but not in washed platelet suspension (WPS), during acute inflammation in rats. Incubation of WPS with inflammatory plasma increased the aggregatory response to ADP, but the plasma itself did not cause aggregation of platelets. It potentiated the ...

journal_title：Biochemical pharmacology

authors： Srivastava R,Srimal RC

更新日期：1990-07-15 00:00:00

abstract：:Glycerol enhances pulmonary tumorigenesis in mice treated with 4-nitroquinoline 1-oxide (4NQO). The present study shows that active oxygen formation by glycerol may be responsible for this enhanced tumorigenesis. Male ddY mice were treated with 4NQO and given a 5% glycerol solution instead of drinking water for up to ...

journal_title：Biochemical pharmacology

authors： Yano T,Ichikawa T

更新日期：1992-06-23 00:00:00