Inhibitions of acid secretion by E3810 and omeprazole, and their reversal by glutathione.


:A substituted benzimidazole ([4-(3-methoxypropoxy)-3-methylpyridine-2-yl]methylsulfinyl)- 1H-benzimidazole sodium salt (E3810), is a gastric proton pump (H+, K(+)-ATPase) inhibitor. E3810 and omeprazole inhibited acid accumulation dose dependently as measured with aminopyrine uptake in isolated rabbit gastric glands, their IC50 values being 0.16 and 0.36 microM, respectively. The addition of exogenous reduced glutathione (GSH) to the gland suspension reactivated dose dependently the acid secretion which had been inhibited by 2 microM E3810 or omeprazole as a function of the incubation time. Furthermore, GSH at 1 and 3 mM reversed the antisecretory effect of E3810 more quickly than it did that of omeprazole. The antisecretory effect of E3810 was slightly greater than that of omeprazole in histamine-stimulated fistula dogs in vivo. The duration of the antisecretory activity of E3810 at concentrations of 2 and 4 mg/kg was shorter than that of omeprazole at the same concentrations in pentagastrin-stimulated fistula dogs. The reversal of the antisecretory activity of the inhibitors in dogs is suggested to be due to the action of endogenous extracellular GSH, in addition to de novo synthesis of the proton pump, because bullfrog gastric mucosae were found in the present study to secrete GSH into the mucosal solution at the rate of about 0.25 nmol/min/g tissue.


Biochem Pharmacol


Biochemical pharmacology


Fujisaki H,Shibata H,Oketani K,Murakami M,Fujimoto M,Wakabayashi T,Yamatsu I,Yamaguchi M,Sakai H,Takeguchi N




Has Abstract


1991-07-05 00:00:00














  • Alkannin induces cytotoxic autophagy and apoptosis by promoting ROS-mediated mitochondrial dysfunction and activation of JNK pathway.

    abstract::Naphthoquinone derivatives and metabolites are widely dispersed molecules in nature. Alkannin, a natural naphthoquinone compound, induces excellent cytotoxicity in cancer cells. However, the detailed mechanism by which alkannin inhibits cancer cell survival remains unclear. In the present study, we isolated alkannin f...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Zheng Q,Li Q,Zhao G,Zhang J,Yuan H,Gong D,Guo Y,Liu X,Li K,Lin P

    更新日期:2020-10-01 00:00:00

  • Induction of functional beta-adrenergic receptors in rat aortic smooth muscle cells by sodium butyrate.

    abstract::Rat aortic smooth muscle cells in culture (A-10; ATCC CRL 1476) exhibited low levels of beta-adrenergic receptors as determined by specific binding of [125I]cyanopindolol ([125I]CYP) and marginal stimulation of adenylate cyclase in plasma membranes by (-)isoproterenol. When these cells were exposed to 5 mM sodium buty...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Nambi P,Whitman MH,Schmidt DB,Heckman GD,Stassen FL,Crooke ST

    更新日期:1986-11-01 00:00:00

  • Regulation of adenylate cyclase by cannabinoid drugs. Insights based on thermodynamic studies.

    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

    pub_type: 杂志文章


    authors: Howlett AC,Scott DK,Wilken GH

    更新日期:1989-10-01 00:00:00

  • SP1-regulated p27/Kip1 gene expression is involved in terbinafine-induced human A431 cancer cell differentiation: an in vitro and in vivo study.

    abstract::In this study, the differentiation-promoting effects of terbinafine (Lamisil), TB) were investigated in human epithelioid squamous carcinoma (A431) cells. The polyhydroxyethylmethacrylate (poly-HEMA)- and type-I collagen-coated culture plate models were adapted to harvest the TB-induced differentiated cells by agitati...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Huang CS,Ho WL,Lee WS,Sheu MT,Wang YJ,Tu SH,Chen RJ,Chu JS,Chen LC,Lee CH,Tseng H,Ho YS,Wu CH

    更新日期:2008-05-01 00:00:00

  • The food colorant erythrosine is a promiscuous protein-protein interaction inhibitor.

    abstract::Following our observation that erythrosine B (FD&C Red No. 3) is a relatively potent inhibitor of the TNF-R-TNFα and CD40-CD154 protein-protein interactions, we investigated whether this inhibitory activity extends to any other protein-protein interactions (PPI) as well as whether any other approved food colors posses...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Ganesan L,Margolles-Clark E,Song Y,Buchwald P

    更新日期:2011-03-15 00:00:00

  • Alteration of mast cell responsiveness to adenosine by pertussis toxin.

    abstract::Adenosine potentiates mouse bone marrow-derived mast cell mediator release by a mechanism that appears to involve cell surface adenosine receptors. In an attempt to explore possible interactions between G proteins and adenosine receptors, mast cells were incubated with activated pertussis toxin, an agent that ADP-ribo...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Marquardt DL,Walker LL

    更新日期:1988-10-15 00:00:00

  • Effect of staurosporine on transcription factor NF-kappaB in human keratinocytes.

    abstract::Activation of the transcription factor NF-kappaB is known to be important in the regulated expression of a large number of pro-inflammatory genes including interleukin-8 (IL-8). Previously, we showed that the protein kinase inhibitor staurosporine potentiates IL-1-stimulated IL-8 production in human keratinocytes. Mor...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Chabot-Fletcher M,Breton JJ

    更新日期:1998-07-01 00:00:00

  • Inhibition of tumour-induced lipolysis in vitro and cachexia and tumour growth in vivo by eicosapentaenoic acid.

    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

    pub_type: 杂志文章


    authors: Tisdale MJ,Beck SA

    更新日期:1991-01-01 00:00:00

  • Differential inhibition of cellular glutathione reductase activity by isocyanates generated from the antitumor prodrugs Cloretazine and BCNU.

    abstract::The antitumor, DNA-alkylating agent 1,3-bis[2-chloroethyl]-2-nitrosourea (BCNU; Carmustine), which generates 2-chloroethyl isocyanate upon decomposition in situ, inhibits cellular glutathione reductase (GR; EC activity by up to 90% at pharmacological doses. GR is susceptible to attack from exogenous electroph...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Rice KP,Penketh PG,Shyam K,Sartorelli AC

    更新日期:2005-05-15 00:00:00

  • Autophagy exacerbates caspase-dependent apoptotic cell death after short times of starvation.

    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

    pub_type: 杂志文章


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

    更新日期:2015-12-15 00:00:00

  • Isolation and characterization of metallothionein dimers.

    abstract::The dimeric forms of metallothionein were isolated from livers of rabbits which accumulated cadmium in large quantities. The dimers were separated into three isoproteins, both on a DEAE Sephadex A-25 column and on a gel permeation column. Reduction of each dimer with mercaptoethanol yielded monomeric metallothionein-I...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Suzuki KT,Yamamura M

    更新日期:1980-03-01 00:00:00

  • Influence of delta 9-tetrahydrocannabinol on expression of histone and ribosomal genes in normal and transformed human cells.

    abstract::The influence of delta 9-tetrahydrocannabinol (delta 9-THC) on the cellular levels of histone mRNAs and ribosomal RNAs was examined in several normal and transformed human cell lines--HeLa S3 cells, WI-38 human diploid fibroblasts, SV40-transformed WI-38 cells, and A549 lung carcinoma cells. RNA sequences were quantit...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Green LG,Stein JL,Stein GS

    更新日期:1984-04-01 00:00:00

  • Flow linear dichroism supports an accordion model for the salt-induced condensation of chromatin.

    abstract::The salt-induced condensation of chromatin has been studied with flow-linear dichroism technique using an intercalative dye (methylene blue) to selectively monitor the linker orientation. At low ionic strength both linkers and chromatosomes (with their flat faces) are oriented preferentially parallel to the chromatin ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Kubista M,Nielsen PE,Nordén B

    更新日期:1988-05-01 00:00:00

  • Inhibition of phosphatidylcholine secretion by stilbene disulfonates in alveolar type II cells.

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    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Chander A,Sen N

    更新日期:1993-05-05 00:00:00

  • Quilamine HQ1-44, an iron chelator vectorized toward tumor cells by the polyamine transport system, inhibits HCT116 tumor growth without adverse effect.

    abstract::Tumor cell growth requires large iron quantities and the deprivation of this metal induced by synthetic metal chelators is therefore an attractive method for limiting the cancer cell proliferation. The antiproliferative effect of the Quilamine HQ1-44, a new iron chelator vectorized toward tumor cells by a polyamine ch...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Renaud S,Corcé V,Cannie I,Ropert M,Lepage S,Loréal O,Deniaud D,Gaboriau F

    更新日期:2015-08-01 00:00:00

  • Role of sulfhydryl compounds in the bactericidal effect of metronidazole.

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    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Yeung TC,Goldman P

    更新日期:1983-11-01 00:00:00

  • Repression of inducible nitric oxide synthase and cyclooxygenase-2 by prostaglandin E2 and other cyclic AMP stimulants in J774 macrophages.

    abstract::The enhanced nitric oxide (NO) and prostaglandin (PG) generation of activated macrophages is controlled by glucocorticoid-sensitive inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2), respectively. Negative feedback regulation of iNOS expression by the products of both pathways has been suggested, but...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Pang L,Hoult JR

    更新日期:1997-02-21 00:00:00

  • Effect of culture conditions on the expression and function of Bsep, Mrp2, and Mdr1a/b in sandwich-cultured rat hepatocytes.

    abstract::Rat hepatocytes cultured in a sandwich configuration form functional canalicular networks. The influence of extracellular matrix configuration, medium composition, and confluency on the expression and function of Bsep, Mrp2, and Mdr1a/b in sandwich-cultured (SC) rat hepatocytes was examined. Primary rat hepatocytes we...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Turncliff RZ,Tian X,Brouwer KL

    更新日期:2006-05-14 00:00:00

  • Correlation [corrected] of salinity with flavin-containing monooxygenase activity but not cytochrome P450 activity in the euryhaline fish (Platichthys flesus)

    abstract::To test the association between flavin-containing monooxygenases (FMOs) and osmoregulation, saltwater-adapted euryhaline flounder (Platichthys flesus) were statically exposed to 34 (ambient), 25, and 15 parts per thousand (/1000) salinity for 1 or 2 weeks. FMO activity (thiourea S-oxidase) was assayed in gill and live...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Schlenk D,Peters LD,Livingstone DR

    更新日期:1996-09-13 00:00:00

  • Characterization of alpha 1- and alpha 2-adrenoceptors directly associated with basolateral membranes from rat kidney proximal tubules.

    abstract::We have used 2-(beta-(3-125iodo-4-hydroxyphenyl)-ethylaminoethyl)-tetr alo ne ([125I]HEAT or BE2254), an alpha 1-selective antagonist, and [3H]yohimbine, an alpha 2-selective antagonist, to demonstrate and characterize binding sites in basolateral membranes from rat kidney cortex. Parathyroid hormone (PTH) stimulated ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Matsushima Y,Akabane S,Ito K

    更新日期:1986-08-01 00:00:00

  • Effects of propranolol and a number of its analogues on sodium channels.

    abstract::To assess the relative contributions that the sodium channel blocking activity of propranolol may play in a variety of its therapeutic applications, its effects were examined in vitro with a sodium channel specific 22Na+ uptake system, using rat brain membranes. Propranolol inhibited 22Na+ uptake in the rat brain memb...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Matthews JC,Baker JK

    更新日期:1982-05-01 00:00:00

  • Clotrimazole inhibits and modulates heterologous association of the key glycolytic enzyme 6-phosphofructo-1-kinase.

    abstract::Clotrimazole is an antifungal azole derivative recently recognized as a calmodulin antagonist with promising anticancer effects. This property has been correlated with the ability of the drug to decrease the viability of tumor cells by inhibiting their glycolytic flux and consequently decreasing the intracellular conc...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Zancan P,Rosas AO,Marcondes MC,Marinho-Carvalho MM,Sola-Penna M

    更新日期:2007-05-15 00:00:00

  • A novel biologically active seleno-organic compound--I. Glutathione peroxidase-like activity in vitro and antioxidant capacity of PZ 51 (Ebselen).

    abstract::a synthetic seleno-organic compound, 2-phenyl-1,2-benzoisoselenazol-3(2H)-one (PZ 51), exhibits GSH peroxidase-like activity in vitro, in contrast to its sulfur analog, PZ 25. In addition, PZ 51 behaves as an antioxidant shown by a temporary protection of rat liver microsomes against ascorbate/ADP-Fe-induced lipid per...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Müller A,Cadenas E,Graf P,Sies H

    更新日期:1984-10-15 00:00:00

  • Relationship between alpha-naphthylisothiocyanate-induced liver injury and elevations in hepatic non-protein sulfhydryl content.

    abstract::Acute administration of alpha-naphthylisothiocyanate (ANIT) to rats has been used as a model of intrahepatic cholestasis. The mechanism of toxicity of ANIT is unknown, although recent evidence suggests a causal or permissive role for glutathione (GSH) (Dahm LJ and Roth RA, Biochem Pharmacol 42: 1181-1188, 1991). In th...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Dahm LJ,Bailie MB,Roth RA

    更新日期:1991-08-22 00:00:00

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    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Lyles GA,Callingham BA

    更新日期:1982-04-01 00:00:00

  • Innovative treatment programs against cancer: II. Nuclear factor-kappaB (NF-kappaB) as a molecular target.

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    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审


    authors: Waddick KG,Uckun FM

    更新日期:1999-01-01 00:00:00

  • Poly (ADP-ribose) polymerases inhibitor, Zj6413, as a potential therapeutic agent against breast cancer.

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    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    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

  • Rat CYP24A1 acts on 20-hydroxyvitamin D(3) producing hydroxylated products with increased biological activity.

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    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Tieu EW,Tang EK,Chen J,Li W,Nguyen MN,Janjetovic Z,Slominski A,Tuckey RC

    更新日期:2012-12-15 00:00:00

  • Effect of human serum albumin on transplacental transfer of glyburide.

    abstract::Glyburide is a second-generation sulfonylurea hypoglycemic drug used for the treatment of select women with pregestational and gestational diabetes mellitus (GDM). In vitro and in vivo investigations demonstrated its very low transplacental transfer to the fetal circulation. However, the factors influencing its low tr...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Nanovskaya TN,Nekhayeva I,Hankins GD,Ahmed MS

    更新日期:2006-08-28 00:00:00

  • Differential regulation of a fibroblast growth factor-binding protein by receptor-selective analogs of retinoic acid.

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    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Boyle BJ,Harris VK,Liaudet-Coopman ED,Riegel AT,Wellstein A

    更新日期:2000-12-01 00:00:00