Degradation of endomorphin-2 at the supraspinal level in mice is initiated by dipeptidyl peptidase IV: an in vitro and in vivo study.

abstract：:SR 4233 (3-amino-1,2,4-benzotriazine-1,4-dioxide) is a novel benzotriazine di-N-oxide which shows unusually high selective toxicity towards hypoxic cells, probably as a result of reductive bioactivation. Using an HPLC assay for the parent drug and its 2- and 4-electron reduction products (SR 4317 and SR 4330, respecti...

journal_title：Biochemical pharmacology

authors： Walton MI,Workman P

更新日期：1990-06-01 00:00:00

abstract：:Alcoholic ketoacidosis and diabetic ketoacidosis are life-threatening complications that share the characteristic features of high anion gap metabolic acidosis. Ketoacidosis is attributed in part to the massive release of ketone bodies (e.g., β-hydroxybutyrate; βOHB) from the liver into the systemic circulation. To da...

journal_title：Biochemical pharmacology

authors： Srinivasan MP,Shawky NM,Kaphalia BS,Thangaraju M,Segar L

更新日期：2019-02-01 00:00:00

abstract：:Cell based studies have suggested that the diabetes drug metformin may combine with the anaplastic lymphoma kinase receptor (ALK) inhibitor crizotinib to increase ALK positive lung cancer cell killing and overcome crizotinib resistance. We therefore tested metformin alone and in combination with crizotinib in vivo, by...

journal_title：Biochemical pharmacology

authors： Bland AR,Shrestha N,Bower RL,Rosengren RJ,Ashton JC

更新日期：2021-01-01 00:00:00

abstract：:The metabolism of tienilic acid, a drug containing a thiophene ring, was reinvestigated in man, rat and dog. The major urinary metabolite in man and rat was isolated and completely characterized by comparison with a synthetic compound. This metabolite derives from the hydroxylation of the thiophene ring of tienilic ac...

journal_title：Biochemical pharmacology

authors： Mansuy D,Dansette PM,Foures C,Jaouen M,Moinet G,Bayer N

更新日期：1984-05-01 00:00:00

abstract：:The NADPH oxidases (NOXs) play a recognized role in the development and progression of inflammation-associated disorders, as well as cancer. To date, several NOX inhibitors have been developed, through either high throughput screening or targeted disruption of NOX interaction partners, although only a few have reached...

journal_title：Biochemical pharmacology

authors： Lu J,Risbood P,Kane CT Jr,Hossain MT,Anderson L,Hill K,Monks A,Wu Y,Antony S,Juhasz A,Liu H,Jiang G,Harris E,Roy K,Meitzler JL,Konaté M,Doroshow JH

更新日期：2017-11-01 00:00:00

abstract：:MOLT-4 (T-), RAJI (B-), and KM-3 (non-B-non-T-, common ALL) malignant lymphoblasts demonstrated significant differences in their activities of purine de novo synthesis (PDNS) and purine salvage pathway and in their cell-kinetic parameters. Incubations with concentrations of methotrexate (0.02 and 0.2 microM), which ca...

journal_title：Biochemical pharmacology

authors： Bökkerink JP,De Abreu RA,Bakker MA,Hulscher TW,van Baal JM,Schretlen ED,De Bruijn CH

更新日期：1988-06-15 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：:Dolastatin 15, a seven-subunit depsipeptide derived from Dolabella auricularia, is a potent antimitotic agent structurally related to the antitubulin agent dolastatin 10, a five-subunit peptide obtained from the same organism. We have compared dolastatin 15 with dolastatin 10 for its effects on cells grown in culture ...

journal_title：Biochemical pharmacology

authors： Bai R,Friedman SJ,Pettit GR,Hamel E

更新日期：1992-06-23 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：:Naturally occurring amino acid substitutions conferring resistance to methotrexate (MTX) have been reported previously at codon positions 22 (leu-->arg, phe) and 31 (phe-->ser, trp) of mammalian dihydrofolate reductases (DHFR). To explore the character of other substitutions, a polymerase chain reaction (PCR)-assisted...

journal_title：Biochemical pharmacology

authors： Morris JA,McIvor RS

更新日期：1994-03-29 00:00:00

abstract：:The tissue distribution of captopril, an antihypertensive drug possessing a free sulfhydryl group, and its sulfur-conjugated metabolites was studied in rats by gas chromatography-mass spectrometry at 15, 30 and 60 min following a single 10 mg/kg oral dose of captopril. It was found that tissue accumulation of captopri...

journal_title：Biochemical pharmacology

authors： Drummer OH,Worland PJ,Jarrott B

更新日期：1983-05-15 00:00:00

abstract：:An inhibitor of diacylglycerol kinase, R59022, enhanced activation of the neutrophil oxidase stimulated by the Ca2+-ionophore, A23187 (1 microM), and by N-formyl-methionyl leucyl-phenylalanine (1 microM). The enhancement was reversed by two inhibitors of c-kinase, retinal (10 microM), and gossypol (20 microM). Activat...

journal_title：Biochemical pharmacology

authors： Cooke E,Al-Mohanna FA,Hallett MB

更新日期：1987-10-15 00:00:00

abstract：:Selective and marked 3-hydroxylase deficiency of lidocaine and its N-deethylated metabolite, MEGX, were observed in male and female DA rats. These findings suggest that cytochrome P450 isozymes metabolizing debrisoquine may be involved in the 3-hydroxylations of lidocaine and MEGX in rats and humans. ...

journal_title：Biochemical pharmacology

authors： Masubuchi Y,Umeda S,Chiba M,Fujita S,Suzuki T

更新日期：1991-07-15 00:00:00

abstract：:We recently found that simvastatin can modulate the nuclear factor-kappaB (NF-kappaB) activation pathway, but whether other statins have similar effects to those of simvastatin is unknown. Therefore, we evaluated the effect six different statins on TNF-induced NF-kappaB activation in human myeloid leukemia cells. We t...

journal_title：Biochemical pharmacology

authors： Ahn KS,Sethi G,Aggarwal BB

更新日期：2008-02-15 00:00:00

abstract：:U73122 ((1-[6-(( 17beta-3-methoxyestra-1,3,5(10)-trien-17-yl)amino)exyl]-1H-p yrrole-2,5-dione)) is generally used as a selective inhibitor of phospholipase C (PLC) and the related rise in cytosolic Ca2+. Recently, by using hepatocytes, it was suggested that its action sites are different for PLC activation and increa...

journal_title：Biochemical pharmacology

authors： Pulcinelli FM,Gresele P,Bonuglia M,Gazzaniga PP

更新日期：1998-12-01 00:00:00

abstract：:Pyridine N-oxide derivatives represent a new class of anti-HIV compounds for which some members exclusively inhibit HIV-1 RT, whereas other members act, additionally or alternatively, at a post-integrational event in the replicative cycle of HIV. A prototype pyridine N-oxide derivative, JPL-32, inhibited tumor necrosi...

journal_title：Biochemical pharmacology

authors： Stevens M,Pannecouque C,De Clercq E,Balzarini J

更新日期：2006-04-14 00:00:00

abstract：:Sodium orthovanadate is known to promote glucose uptake in muscle and adipose tissues and has been suggested as a possible oral hypoglycemic agent. In addition, insulin-dependent diabetes has been shown to alter the hepatobiliary clearance of several drugs in rats. This study has determined whether orthovanadate, like...

journal_title：Biochemical pharmacology

authors： Watkins JB 3rd,Bauman ME,Beaty TM

更新日期：1993-12-14 00:00:00

abstract：:Cyclodextrins generally exhibit hemolytic activity, some at concentrations as low as 1-10 mg/mL or lower. However, we found previously that a highly polysulfated cyclodextrin has no demonstrable hemolytic activity (Macarak et al., Biochem Pharmacol 42: 1502-1503, 1991). In the present study, we determined that, in fac...

journal_title：Biochemical pharmacology

authors： Weisz PB,Kumor K,Macarak EJ

更新日期：1993-03-09 00:00:00

abstract：:Partial hepatectomy (PH) (70% resection) causes within 4 hr an accumulation of ornithine decarboxylase (EC 4.1.1.17, ODC) mRNAs concomitant with an increase in ODC activity, maximum values being observed at 8 and 16 hr, respectively. In the early hours of hepatic regeneration, enhancement of transcriptional-rate of OD...

journal_title：Biochemical pharmacology

authors： Desiderio MA,Lugaro G,Galasso D,Colombo MP

更新日期：1990-10-01 00:00:00

abstract：:A strain of hyperlipidaemic Sprague-Dawley (HSD) rat was compared with normal Sprague-Dawley (SD) rats for expression of cholesterol 7alpha-hydroxylase activity (CYP7A1) and other cytochrome P450 (P450) enzymes in liver. Hepatic microsomal CYP7A1 activity in male HSD rats was 2-3-fold lower than in male SD rats with C...

journal_title：Biochemical pharmacology

authors： Brassil PJ,Debri K,Nakura H,Kobayashi S,Davies DS,Edwards RJ

更新日期：1998-07-15 00:00:00

abstract：:A number of synthetic manganese complexes exhibit both in vitro and in vivo catalytic antioxidant activities. This study reports that the antioxidant potencies of a new series of meso-N,N'-dialkyl-imidazolium substituted manganese(III) porphyrins are dependent, in part, on their ability to redox cycle with endogenous ...

journal_title：Biochemical pharmacology

authors： Kachadourian R,Johnson CA,Min E,Spasojevic I,Day BJ

更新日期：2004-01-01 00:00:00

abstract：AIM/HYPOTHESIS:The aim of this study was to develop an insulin-resistant cell culture model in skeletal muscle cell line by chronic presence of insulin in serum-free medium and to determine the effect of thiazolidinediones on insulin signaling. METHODS:We differentiated C2C12 in a combination of serum-free medium in p...

journal_title：Biochemical pharmacology

authors： Kumar N,Dey CS

更新日期：2003-01-15 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：:Cobalt is suspected to cause memory deficit in humans and was reported to induce neurotoxicity in animal models. We have studied the effects of cobalt in primary cultures of mouse astrocytes. CoCl(2) (0.2-0.8mM) caused dose-dependent ATP depletion, apoptosis (cell shrinkage, phosphatidylserine externalization and chro...

journal_title：Biochemical pharmacology

authors： Karovic O,Tonazzini I,Rebola N,Edström E,Lövdahl C,Fredholm BB,Daré E

更新日期：2007-03-01 00:00:00

abstract：:Prunetin is an O-methylated isoflavone, which is a type of flavonoid. There are a limited number of reports detailing the biological activities of prunetin. Although an anti-inflammatory effect of prunetin has been reported in vitro, to our knowledge, there have been no reports on anti-adipogenic effects of prunetin i...

journal_title：Biochemical pharmacology

authors： Ahn TG,Yang G,Lee HM,Kim MD,Choi HY,Park KS,Lee SD,Kook YB,An HJ

更新日期：2013-05-15 00:00:00

abstract：:Resistance to anti-cancer chemotherapies often leads to regional failure, and can be caused by biochemical and/or physiological mechanisms. Biochemical mechanisms include the overexpression of resistance-conferring proteins. In contrast, physiological resistance involves the tumor microenvironment, and can be caused b...

journal_title：Biochemical pharmacology

authors： Mahoney BP,Raghunand N,Baggett B,Gillies RJ

更新日期：2003-10-01 00:00:00

abstract：:Rational approaches to targeted cancer therapy have begun to predominate the pipelines of oncology drug development. Our rapidly increasing understanding of the "wiring" of tumor cells and the vulnerabilities of such cells that can potentially be exploited through targeted treatments has opened up enormous opportuniti...

journal_title：Biochemical pharmacology

authors： Sharma SV,Settleman J

更新日期：2010-09-01 00:00:00

abstract：:Staurosporine is one of the most potent and well known inhibitors of protein kinases, and it is often used to study the involvement of protein kinases in signal transduction pathways. We now report that staurosporine can induce the production of hepatocyte growth factor (HGF) independently of protein kinase inhibition...

journal_title：Biochemical pharmacology

authors： Yagi Y,Sotani T,Nagao T,Horio T,Yamamoto I,Gohda E

更新日期：2003-11-01 00:00:00

abstract：:Knowledge of the nature of the interaction between the stimulatory G protein (Gs) and the adenylyl cyclase catalytic unit (C) is essential for interpreting the effects of Gs mutations and expression levels on cellular response to a wide variety of hormones, drugs, and neurotransmitters. It has been proposed that beta-...

journal_title：Biochemical pharmacology

authors： Krumins AM,Lapeyre JN,Clark RB,Barber R

更新日期：1997-07-01 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