In vivo metabolism of alpha,alpha,beta,beta-tetradeutero-N, N-dimethyltryptamine in rodent brain.

abstract：:A series of cytotoxic propenal (3-oxoprop-1-enyl) derivatives of pyrimidine bases and deoxynucleosides was evaluated for their ability to block thymidylate synthesis in intact and permeabilized murine leukemia L1210 cells. Several were potent inhibitors of this process, likely contributing to their cytotoxicity. The I...

journal_title：Biochemical pharmacology

authors： Kalman TI,Marinelli ER,Xu B,Reddy AR,Johnson F,Grollman AP

更新日期：1991-07-05 00:00:00

abstract：:AKT1 (c-AKT, PKBalpha) is the cellular homolog of the protein-serine/threonine kinase oncogene, v-akt. AKT1 is activated through the insulin and platelet-derived growth factor signaling pathways in transfected fibroblasts, but little is known about the regulation of endogenous AKT1 in tumor cells. AKT1 levels were hig...

journal_title：Biochemical pharmacology

authors： Ahmad S,Singh N,Glazer RI

更新日期：1999-08-01 00:00:00

abstract：:Mammary gland and liver microsomes of lactating rats were examined for the components of mixed function oxidase and related enzyme activities. Cytochrome b5, NADH- and NADPH- dependent cytochrome c reductase activities were 15-, 6- and 10-fold lower, respectively, in the mammary gland than in the liver microsomes. The...

journal_title：Biochemical pharmacology

authors： Ritter CL,Malejka-Giganti D

更新日期：1982-01-15 00:00:00

abstract：:Heme oxygenase (HO)-1 is the inducible isoform of the rate-limiting enzyme of heme degradation. HO regulates the cellular content of the pro-oxidant heme and produces catabolites with physiological functions. HO-1 is induced by a host of oxidative stress stimuli, and the activation of HO-1 gene expression is considere...

journal_title：Biochemical pharmacology

authors： Immenschuh S,Ramadori G

更新日期：2000-10-15 00:00:00

abstract：:In our search for NF-kappaB inhibitors from natural resources, we have previously identified two structurally related dilignans, manassantin A and B as specific inhibitors of NF-kappaB activation from Saururus chinensis. However, their molecular mechanism of action remains unclear. We here demonstrate that manassantin...

journal_title：Biochemical pharmacology

authors： Lee JH,Hwang BY,Kim KS,Nam JB,Hong YS,Lee JJ

更新日期：2003-11-15 00:00:00

abstract：:Resealed synaptic plasma membrane vesicles exhibit Na+-dependent Ca2+ transport activity which may participate in regulation of free Ca2+ concentrations in nerve endings. Sodium chloride-loaded vesicles took up Ca2+ from the external medium (150 mM KCl-25 mM Tris/HCl) in the presence of an outward-directed Na+ gradien...

journal_title：Biochemical pharmacology

authors： Michaelis ML,Michaelis EK

更新日期：1983-03-15 00:00:00

abstract：:ABT-263 induces MCL1 upregulation in cancer cells, which confers resistance to the drug. An increased understanding of the mechanism underlying ABT-263-induced MCL1 expression may provide a strategy to improve its tumor-suppression activity. The present study revealed that ABT-263 reduced the turnover of MCL1 mRNA, th...

journal_title：Biochemical pharmacology

authors： Lee YC,Wang LJ,Huang CH,Chiou JT,Shi YJ,Chang LS

更新日期：2020-08-01 00:00:00

abstract：:Cellular glutathione concentrations in primary cultures of chick embryo hepatocytes were 15.3 +/- 5.3 nmoles/mg protein (mean +/- S.D.) and remained stable for up to 3 days in culture. The presence of insulin was not essential for the maintenance of glutathione concentrations. Induction of cytochrome P-450 by phenobar...

journal_title：Biochemical pharmacology

authors： Shedlofsky SI,Sinclair PR,Sinclair JF,Bonkovsky HL

更新日期：1984-05-01 00:00:00

abstract：:Extrahepatic cytochrome P450 enzymes (CYP450) are pivotal in the metabolism of endogenous substrates and xenobiotics. CYP2J2 is a major cardiac CYP450 and primarily metabolizes polyunsaturated fatty acids such as arachidonic acid to cardioactive epoxyeicosatrienoic acids. Due to its role in endobiotic metabolism, CYP2...

journal_title：Biochemical pharmacology

authors： Karkhanis A,Hong Y,Chan ECY

更新日期：2017-07-01 00:00:00

abstract：:Cyclophosphamides are pro-drugs whose killing agent is produced from an aldehyde that is formed by the action of a P450 oxidation step. The mustard from the aldehyde can destroy bone marrow cells as well as the tumor. Aldehyde dehydrogenase (EC 1.2.1.3) can oxidize the aldehyde and hence inactivate the cytotoxic inter...

journal_title：Biochemical pharmacology

authors： Ho KK,Mukhopadhyay A,Li YF,Mukhopadhyay S,Weiner H

更新日期：2008-09-01 00:00:00

abstract：:Nitrogen dioxide (NO2), an environmental oxidant pollutant, is known to peroxidize membrane lipids of lung cells. We evaluated the ability of NO2 to alter the surface membrane fluidity, lipid composition, and insulin receptor binding of porcine pulmonary artery endothelial cells in culture. After 3- to 24-hr exposure ...

journal_title：Biochemical pharmacology

authors： Patel JM,Edwards DA,Block ER,Raizada MK

更新日期：1988-04-15 00:00:00

abstract：:Mitochondrial carriers are proteins that shuttle a variety of metabolites, nucleotides and coenzymes across the inner mitochondrial membrane. The mitochondrial ADP/ATP carriers (AACs) specifically translocate the ATP synthesized within mitochondria to the cytosol in exchange for the cytosolic ADP, playing a key role i...

journal_title：Biochemical pharmacology

authors： Todisco S,Di Noia MA,Onofrio A,Parisi G,Punzi G,Redavid G,De Grassi A,Pierri CL

更新日期：2016-01-15 00:00:00

abstract：:Chronic administration to rats of the anticonvulsant drug, valproate, induced proliferation of liver peroxisomes and selectively increased the activity of the enzymes involved in beta-oxidation in these organelles. In kidney cortex, only a moderate increase in enzyme activity could be recorded. Valproate (1% w/w in th...

journal_title：Biochemical pharmacology

authors： Ponchaut S,Draye JP,Veitch K,Van Hoof F

更新日期：1991-05-15 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：:Phomopsins comprise a family of peptide mycotoxins containing a 13-membered ring formed by an ether bridge, produced by the fungus Phomopsis leptostromiformis, the causal agent in lupin poisoning (lupinosis). The biochemical actions of two naturally occurring phomopsins, phomopsin A and B, and the chemical derivatives...

journal_title：Biochemical pharmacology

authors： Lacey E,Edgar JA,Culvenor CC

更新日期：1987-07-01 00:00:00

abstract：:Chlamydia pneumoniae is a universal pathogen that has been indicated to play a part in the development of asthma, atherosclerosis and lung cancer. The complete eradication of this intracellular bacterium is in practice impossible with the antibiotics that are currently in use and studies on new antichlamydial compound...

journal_title：Biochemical pharmacology

authors： Salin O,Alakurtti S,Pohjala L,Siiskonen A,Maass V,Maass M,Yli-Kauhaluoma J,Vuorela P

更新日期：2010-10-15 00:00:00

abstract：:The mechanism of activation of microsomal glutathione transferase in isolated liver cells by diisapropylidene acetone (phorone) was investigated. Phorone (1 mM) causes a time-dependent increase (up to 2.6-fold) in the glutathione transferase activity of microsomes isolated from treated hepatocytes. Since phorone react...

journal_title：Biochemical pharmacology

authors： Lundqvist G,Morgenstern R

更新日期：1992-01-22 00:00:00

abstract：:Runt-related transcription factor 1 (RUNX1), one subunit of core-binding factors in hematopoiesis and leukemia, was highly expressed in ovarian cancer (OC), but the role of RUNX1 in OC is largely unknown. Since we found that high expression of RUNX1 is correlated with poor survival in patients with OC through bioinfor...

journal_title：Biochemical pharmacology

authors： Xiao L,Peng Z,Zhu A,Xue R,Lu R,Mi J,Xi S,Chen W,Jiang S

更新日期：2020-10-01 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：:We have examined, relative to clofibric acid (CPIB), the effects of a chemical series of phenoxyacetic acids and of two asymmetric CPIB analogues, the R(+)- and S(-)-enantiomers of 2-(4-chlorophenoxy)propionic acid (4-CPPA) and 2-(4-chlorophenoxy)butyric acid (4-CPBA), on hepatic peroxisome proliferation both in vivo ...

journal_title：Biochemical pharmacology

authors： Esbenshade TA,Kamanna VS,Newman HA,Tortorella V,Witiak DT,Feller DR

更新日期：1990-09-15 00:00:00

abstract：:Stimulation of lipolysis in murine adipocytes in response to a lipid-mobilizing factor produced by a cachexia-inducing murine adenocarcinoma was inhibited by eicosapentaenoic acid (EPA) with a Ki value of 104 microM. The inhibitory effect was strictly structurally specific, since other related fatty acids of both the ...

journal_title：Biochemical pharmacology

authors： Tisdale MJ,Beck SA

更新日期：1991-01-01 00:00:00

abstract：:The cytotoxicity anti-tumour intercalating agents such as the anthraquinone mitoxantrone is thought to relate to DNA binding and the trapping of DNA topoisomerase II complexes on cellular DNA. We have studied the uptake, nuclear location, DNA binding mode and DNA damaging capacity of mitoxantrone in a small cell lung ...

journal_title：Biochemical pharmacology

authors： Smith PJ,Morgan SA,Fox ME,Watson JV

更新日期：1990-11-01 00:00:00

abstract：:L-Carnitine is a key molecule in the transfer of fatty acid across mitochondrial membranes. Bioavailable L-carnitine is either provided by an endogeneous biosynthesis or after intestinal absorption of dietary items containing L-carnitine. After intestinal absorption or hepatic biosynthesis, L-carnitine is transferred ...

journal_title：Biochemical pharmacology

authors： Georges B,Galland S,Rigault C,Le Borgne F,Demarquoy J

更新日期：2003-05-01 00:00:00

abstract：:We have studied the effect of low sulfate concentrations on the glycosaminoglycan synthesis in rat patellar cartilage in vivo as well as in vitro. The oral administration of 200 mg/kg paracetamol to male Wistar rats resulted in a significant reduction of the serum sulfate concentration. Reduced serum sulfate availabil...

journal_title：Biochemical pharmacology

authors： van der Kraan PM,de Vries BJ,Vitters EL,van den Berg WB,van de Putte LB

更新日期：1988-10-01 00:00:00

abstract：:2-Chloroacetaldehyde (CAA)-induced cytotoxicity in isolated hepatocytes was enhanced markedly if hepatocyte alcohol or aldehyde dehydrogenase was inhibited prior to CAA addition. Hepatocyte GSH depletion, ATP depletion and lipid peroxidation by CAA were also enhanced markedly. Furthermore, CAA was about 10- and 70-fol...

journal_title：Biochemical pharmacology

authors： Sood C,O'Brien PJ

更新日期：1994-08-30 00:00:00

abstract：:The effects of two new phthalazinone derivatives, azelastine (AZ) and flezelastine (FZ), on the reversal of resistance to doxorubicin (dox) were studied using two variants of the rat C6 glioblastoma cell line, selected with dox (C6 0.5) or with vincristine (C6 1V). Both lines presented a multidrug-resistant phenotype ...

journal_title：Biochemical pharmacology

authors： Hu YP,Robert J

更新日期：1995-07-17 00:00:00

abstract：:Gemcitabine and ara-C have multiple mechanisms of action: DNA incorporation and for gemcitabine also ribonucleotide reductase (RNR) inhibition. Since dCTP competes with their incorporation into DNA, dCTP depletion can potentiate their cytotoxicity. We investigated whether additional RNR inhibition by Triapine (3-AP), ...

journal_title：Biochemical pharmacology

authors： Sigmond J,Kamphuis JA,Laan AC,Hoebe EK,Bergman AM,Peters GJ

更新日期：2007-05-15 00:00:00

abstract：:Tetranitromethane (TNM) is a reagent which reacts with the tyrosine and cysteine residues of proteins. Chemical modification of partially purified human platelet alpha 2-adrenoceptors with TNM resulted in an irreversible loss of binding activity. Typically, an 80-90% decrease in binding activity occurred with a 60-min...

journal_title：Biochemical pharmacology

authors： Nakata H,Regan JW,Lefkowitz RJ

更新日期：1986-11-15 00:00:00

abstract：:The seminal vesicle protein No. 4 (SV-IV) secreted from the rat seminal vesicle epithelium, possesses immunosuppressive and anti-inflammatory properties and it is a potent inhibitor of platelet aggregation both in vivo and in vitro. This research aimed to investigate the possible effect of SV-IV on the process of huma...

journal_title：Biochemical pharmacology

authors： Di Micco B,Colonna G,Porta R,Metafora S

更新日期：1994-07-19 00:00:00

abstract：:Repertaxin is a new non-competitive allosteric blocker of interleukin-8 (CXCL8/IL-8) receptors (CXCR1/R2), which by locking CXCR1/R2 in an inactive conformation prevents receptor signaling and human polymorphonuclear leukocyte (PMN) chemotaxis. Given the unique mode of action of repertaxin it was important to examine ...

journal_title：Biochemical pharmacology

authors： Casilli F,Bianchini A,Gloaguen I,Biordi L,Alesse E,Festuccia C,Cavalieri B,Strippoli R,Cervellera MN,Di Bitondo R,Ferretti E,Mainiero F,Bizzarri C,Colotta F,Bertini R

更新日期：2005-02-01 00:00:00