Effects of the enantiomers of lansoprazole (AG-1749) on (H+ + K+)-ATPase activity in canine gastric microsomes and acid formation in isolated canine parietal cells.

abstract：:Accumulating evidence indicates that dysfunction in amino acid neurotransmission contributes to the pathophysiology of depression. Consequently, the modulation of amino acid neurotransmission represents a new strategy for antidepressant development. While glutamate receptor ligands are known to have antidepressant eff...

journal_title：Biochemical pharmacology

authors： Valentine GW,Sanacora G

更新日期：2009-09-01 00:00:00

abstract：:Cannabis and cannabinoids are known to affect female reproduction. However, the role of the endocannabinoid system in mouse uterine contractility in the dioestrus and oestrus phases has not been previously investigated. The present study aimed at filling this gap. Endocannabinoid (anandamide and 2-arachidonoylglycerol...

journal_title：Biochemical pharmacology

authors： Pagano E,Orlando P,Finizio S,Rossi A,Buono L,Iannotti FA,Piscitelli F,Izzo AA,Di Marzo V,Borrelli F

更新日期：2017-01-15 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：:Glucuronidation of quinols of polycyclic aromatic hydrocarbons (PAHs) represents an important detoxication pathway preventing toxic quinone/quinol redox cycles. Therefore, mono- and diglucuronide formation of benzo(a)pyrene-3,6-quinol was investigated and compared to that of structurally related 3,6-dihydroxychrysene ...

journal_title：Biochemical pharmacology

authors： Gschaidmeier H,Seidel A,Burchell B,Bock KW

更新日期：1995-05-26 00:00:00

abstract：:The antimicrobial peptide human beta-defensin-3 (hBD-3) is produced by epidermal keratinocytes and protects the skin from infections. This peptide induces the release of a lipid mediator, prostaglandin D(2) from dermal mast cells. Prostaglandin D(2) binds to cell-surface G protein-coupled receptors, D prostanoid recep...

journal_title：Biochemical pharmacology

authors： Kanda N,Ishikawa T,Watanabe S

更新日期：2010-04-01 00:00:00

abstract：:Heat shock protein 90 (Hsp90) is a molecular chaperone engaging in multiple cellular signaling by stabilizing oncoproteins (e.g. Akt and c-Raf) in tumor cells. Whereas Hsp90 inhibitors such as 17-AAG exert promising antitumor effects in clinical trials, current efforts focus on developing agents targeting Hsp90 with i...

journal_title：Biochemical pharmacology

authors： Lu C,Liu D,Jin J,Deokar H,Zhang Y,Buolamwini JK,Yu X,Yan C,Chen X

更新日期：2013-05-01 00:00:00

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：:Certain anticonvulsant drugs require N-acetylation as a major route of metabolic clearance. Single point mutations of the polymorphic N-acetyltransferase gene (pNAT) are the primary cause for impaired drug acetylation. Pharmacokinetic parameters are altered in slow acetylator phenotypes and this may compromise drug sa...

journal_title：Biochemical pharmacology

authors： Borlak JT,Harsany V,Schneble H,Haegele KD

更新日期：1994-11-01 00:00:00

abstract：:The DNA-topoisomerase I (Topo I) inhibitor, camptothecin (CPT), is a plant alkaloid with an important antitumor activity. In order to investigate the cellular mechanism leading to the development of the resistance to this agent, we have established by progressive adaptation a P388 subline resistant to CPT. After 5 mon...

journal_title：Biochemical pharmacology

authors： Madelaine I,Prost S,Naudin A,Riou G,Lavelle F,Riou JF

更新日期：1993-01-26 00:00:00

abstract：:Poly (ADP-ribose) polymerases (PARPs) facilitate repairing of cancer cell DNA damage as a mean to promote cancer proliferation and metastasis. Inhibitors of PARPs which interfering DNA repair, in context of defects in other DNA repair mechanisms, can thus be potentially exploited to inhibit or even kill cancer cells. ...

journal_title：Biochemical pharmacology

authors： Zhou Q,Ji M,Zhou J,Jin J,Xue N,Chen J,Xu B,Chen X

更新日期：2016-05-01 00:00:00

abstract：:Nonsteroidal anti-inflammatory drugs are used extensively in clinical medicine. In spite of their therapeutic utility, however, they are known to cause significant gastrointestinal and renal toxicities, circumstances that limit their use. The side effects produced in these organs have been attributed mainly to the inh...

journal_title：Biochemical pharmacology

authors： Basivireddy J,Jacob M,Pulimood AB,Balasubramanian KA

更新日期：2004-02-01 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：:Oral administration of tobacco to rats for 21 days caused remarkable stimulation of the metabolism of phenacetin, aniline and benzo[a]pyrene, a carcinogen, by hepatic microsomal mixed function oxidases (MFO). Such treatment for 6 days resulted in a small increase in the activities of phenacetin O-dealkylase and aromat...

journal_title：Biochemical pharmacology

authors： Kaur S,Ali B

更新日期：1982-04-15 00:00:00

abstract：:Macrophages are key inflammatory cells in chronic obstructive pulmonary disease (COPD). The pathophysiology of cigarette smoke-induced lung emphysema is complex but there is a clear role for reactive oxygen species (ROS, such as peroxynitrite), tumor necrosis factor (TNF-alpha) and interleukin (IL)-8. We investigated ...

journal_title：Biochemical pharmacology

authors： Sarir H,Mortaz E,Janse WT,Givi ME,Nijkamp FP,Folkerts G

更新日期：2010-03-01 00:00:00

abstract：:The effect of the adenosine deaminase (ADA) inhibitor 2'-deoxycoformycin (dCF) on the development of insulin-dependent diabetes mellitus (IDDM) was assessed in the BB Wistar rat. Sixty-one male rats were treated from days 30 to 120 with 0, 0.5, 1.0 or 1.5 mg dCF/kg/week. The incidence of IDDM was 78% in the controls a...

journal_title：Biochemical pharmacology

authors： Thliveris JA,Begleiter A,Kobrinsky NL,Verburg L,Dean HJ,Johnston JB

更新日期：1993-09-14 00:00:00

abstract：:A number of tumour cells, including Ehrlich ascites tumour cells (EATC), possess a polyamine uptake system which selectively accumulates endogenous polyamines and structurally related compounds by an active energy dependent system(s). We suggest that it may be possible to utilize this uptake system to target certain c...

journal_title：Biochemical pharmacology

authors： Holley J,Mather A,Cullis P,Symons MR,Wardman P,Watt RA,Cohen GM

更新日期：1992-02-18 00:00:00

abstract：:Entrectinib is a new tyrosine kinase inhibitor that was recently approved for the treatment of ROS1-positive metastatic non-small cell lung cancer (NSCLC). In this study, we aimed to characterize its potential to act as a modulator of pharmacokinetic cytostatic resistance and perpetrator of drug interactions. In accum...

journal_title：Biochemical pharmacology

authors： Vagiannis D,Yu Z,Novotna E,Morell A,Hofman J

更新日期：2020-08-01 00:00:00

abstract：:Many tumors are resistant to drug-induced cell-cycle arrest and apoptosis. We have reported that apoptosis can be restored in human multidrug-resistant (MDR) hepatocellular carcinoma cell lines by celecoxib. Here we show that P-glycoprotein (P-gp) mediates cell-cycle arrest and autophagy induced by celecoxib in human ...

journal_title：Biochemical pharmacology

authors： Mazzanti R,Platini F,Bottini C,Fantappiè O,Solazzo M,Tessitore L

更新日期：2009-07-01 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：: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：:N-Trifluoroacetyladriamycin-14-valerate (AD 32), a lipophilic, DNA non-binding analog of Adriamycin (ADR), was found to be a potent inhibitor of the membrane-bound enzyme, protein kinase C (PKC). PKC was isolated and purified from human leukemia ML-1 cells, and the enzyme activity was shown to be activated by the tumo...

journal_title：Biochemical pharmacology

authors： Chuang LF,Kung HF,Israel M,Chuang RY

更新日期：1992-02-18 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 effect of macrophage supernatant on the recovery of wounds induced in rat gastric epithelial RGM1 monolayers was investigated. The repair of wounds induced in the monolayers of RGM1 cells was accelerated time-dependently by 10 ng/mL of transforming growth factor-alpha (TGF-alpha). TGF-alpha also significantly stim...

journal_title：Biochemical pharmacology

authors： Nakamura E,Takahashi S,Ishikawa M,Okabe S

更新日期：1999-10-01 00:00:00

abstract：:The release of the inflammatory mediators, prostaglandins (PGs), leukotrienes (LT) and lysosomal acid hydrolases (LAH), by macrophages is stimulated by endocytic stimuli such as zymosan. This process can be interfered with by specific inhibitors of phosphatidylcholine (PC) biosynthesis. The diphenylsulfone dapsone and...

journal_title：Biochemical pharmacology

authors： Bonney RJ,Wightman PD,Dahlgren ME,Sadowski SJ,Davies P,Jensen N,Lanza T,Humes JL

更新日期：1983-01-15 00:00:00

abstract：:The therapeutic efficacy of immunosuppressive agents has been intensively studied for colitis management. We synthesized a series of andrographolide derivatives and reported their structure-activity-relationship and anti-inflammatory activity in our previous studies. Among these derivatives, compound 3b exhibited the ...

journal_title：Biochemical pharmacology

authors： Guo BJ,Liu Z,Ding MY,Li F,Jing M,Xu LP,Wang YQ,Zhang ZJ,Wang Y,Wang D,Zhou GC,Wang Y

更新日期：2019-05-01 00:00:00

abstract：:Auranofin (AF) is a newly introduced oral gold compound having antirheumatic properties, and its efficacy in the treatment of bronchial asthma is now under investigation. In this study, we examined the effects of AF on leukotriene (LT) formation by human polymorphonuclear leukocytes (PMNs) stimulated with the calcium ...

journal_title：Biochemical pharmacology

authors： Honda Z,Iizasa T,Morita Y,Matsuta K,Nishida Y,Miyamoto T

更新日期：1987-05-01 00:00:00

abstract：:DNA-dependent protein kinase (DNA-PK) plays a key role in repair of radiation-induced DNA double strand breaks (DSB) by non-homologous end-joining. DNA-PK inhibitors (DNA-PKi) are therefore efficient radiosensitisers, but normal tissue radiosensitisation represents a risk for their use in radiation oncology. Here we d...

journal_title：Biochemical pharmacology

authors： Wong WW,Jackson RK,Liew LP,Dickson BD,Cheng GJ,Lipert B,Gu Y,Hunter FW,Wilson WR,Hay MP

更新日期：2019-11-01 00:00:00

abstract：:Somatostatin receptors from rabbit retinal membranes were solubilized in an active form using a mixture of the detergent n-octyl b-D-glucopyranoside (OG) and CHAPS. The binding of [125I]-Try11-somatostatin to the soluble extract was saturable and of high affinity, with an apparent affinity constant (Kd) of 0.60 +/- 0....

journal_title：Biochemical pharmacology

authors： Liapakis G,Politou E,Thermos K

更新日期：1993-05-05 00:00:00

abstract：:Nucleoside analogs conjugated with galactosyl-terminating peptides selectively enter liver cells and after intracellular release from the carrier partly exit into bloodstream, resulting in higher concentrations in liver blood than in systemic circulation. The aim of the present experiments was to ascertain whether, in...

journal_title：Biochemical pharmacology

authors： Di Stefano G,Busi C,Camerino A,Derenzini M,Trerè D,Fiume L

更新日期：2001-02-15 00:00:00

abstract：:Tumor-induced neoangiogenesis is an essential event for solid tumor growth. Therefore, a compound able to block angiogenesis-promoting factors could have antitumor activity. The polysulfonated naphthylurea suramin is hypothesized to have this mode of action. A series of sulfonated distamycin A derivatives have been sy...

journal_title：Biochemical pharmacology

authors： Ciomei M,Pastori W,Mariani M,Sola F,Grandi M,Mongelli N

更新日期：1994-01-20 00:00:00