Cardiac sensitivity to the inhibitory effects of chlorpromazine, imipramine and amitriptyline upon formation of flavins.

Abstract:

:Chlorpromazine, imipramine and amitriptyline, drugs structurally related to riboflavin, each inhibited the formation in vivo of flavin adenine dinucleotide (FAD) from riboflavin in rat heart at 2-5 mg/kg body weight, doses comparable on a weight basis to those used clinically. All three drugs inhibited FAD formation in heart within 5 hr after a single dose of 25 mg/kg. Chlorpromazine under these conditions also inhibited FAD formation in liver, cerebrum and cerebellum. A series of psychoactive agents structurally unrelated to riboflavin did not inhibit flavin formation in the organs tested. These findings indicate that the inhibitory effects of the drugs studied have organ specificity with respect to FAD formation.

journal_name

Biochem Pharmacol

journal_title

Biochemical pharmacology

authors

Pinto J,Huang YP,Pelliccione N,Rivlin RS

doi

10.1016/0006-2952(82)90632-3

subject

Has Abstract

pub_date

1982-11-01 00:00:00

pages

3495-9

issue

21

eissn

0006-2952

issn

1873-2968

pii

0006-2952(82)90632-3

journal_volume

31

pub_type

杂志文章
  • A sensitive new method for clinically monitoring cytarabine concentrations at the DNA level in leukemic cells.

    abstract::Cytarabine (ara-C), a major antileukemic agent, is phosphorylated in the cell to cytarabine triphosphate (ara-CTP), which is then partly incorporated into DNA. The drug incorporation into DNA poisons the extending primer against further incorporation of deoxyribonucleotides including dCTP, ultimately inhibiting DNA sy...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2005.03.013

    authors: Yamauchi T,Ueda T

    更新日期:2005-06-15 00:00:00

  • Human adenosine A(3) receptor leads to intracellular Ca(2+) mobilization but is insufficient to activate the signaling pathway via phosphoinositide 3-kinase gamma in mice.

    abstract::Selective antagonists for the adenosine A(3) receptor (A3AR), a member of the G protein-coupled receptors, have been indicated as potential drugs for anti-asthma or anti-inflammation. However, potent antagonists for the rodent A3AR have not been identified. To evaluate the pharmacological effects of human A3AR antagon...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2005.08.003

    authors: Yamano K,Inoue M,Masaki S,Saki M,Ichimura M,Satoh M

    更新日期:2005-11-15 00:00:00

  • Effects of a new triazinoaminopiperidine derivative on adriamycin accumulation and retention in cells displaying P-glycoprotein-mediated multidrug resistance.

    abstract::A new triazinoaminopiperidine derivative, Servier 9788 (S9788), was investigated for its ability to increase Adriamycin (ADR) accumulation and retention in two rodent (P388/ADR and DC-3F/AD) and three human (KB-A1, K562/R and COLO 320DM) cell lines displaying the P-glycoprotein (P-gp)-mediated multidrug resistance (MD...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(92)90063-o

    authors: Léonce S,Pierré A,Anstett M,Pérez V,Genton A,Bizzari JP,Atassi G

    更新日期:1992-11-03 00:00:00

  • A checkerboard method to evaluate interactions between drugs.

    abstract::A method to evaluate interactions between biologically active agents is presented. Synergism, zero interaction, and antagonism were easily detected with the three-dimensional approach proposed herein. This method is compatible with a checkerboard design to diagnose the interaction between agents and obviate the need t...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0006-2952(95)02230-9

    authors: Martinez-Irujo JJ,Villahermosa ML,Alberdi E,Santiago E

    更新日期:1996-03-08 00:00:00

  • Reduction of intracellular pH by inhibitors of natural killer cell activity, nicardipine, methyl 2-(N-benzyl-N-methylamino)ethyl-2,6-dimethyl-4-(2-isopropyl-pyrazolo[1, 5-a]pyridine-3-yl)-1,4-dihydro-pyridine-3,5-dicarboxylate (AHC-52), and 4,4'-diisothio

    abstract::Our previous study showed that nicardipine and its structural analog, methyl 2-(N-benzyl-N-methylamino)ethyl-2,6-dimethyl-4-(2-isopropyl-pyrazolo[1,5 -a]pyridine-3-yl)-1,4-dihydro-pyridine-3,5-dicarboxylate (AHC-52), which is devoid of calcium channel blocking activity, were equally effective in inhibiting natural kil...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0006-2952(97)00160-3

    authors: Yamashiro T,Watanabe N,Kobayashi Y

    更新日期:1997-07-01 00:00:00

  • Reactive oxygen species derived from xanthine oxidase interrupt dimerization of breast cancer resistance protein, resulting in suppression of uric acid excretion to the intestinal lumen.

    abstract::The prevalence of hyperuricemia/gout increases with aging. However, the effect of aging on function for excretion of uric acid to out of the body has not been clarified. We found that ileal uric acid clearance in middle-aged rats (11-12 months) was decreased compared with that in young rats (2 months). In middle-aged ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2015.06.021

    authors: Ogura J,Kuwayama K,Sasaki S,Kaneko C,Koizumi T,Yabe K,Tsujimoto T,Takeno R,Takaya A,Kobayashi M,Yamaguchi H,Iseki K

    更新日期:2015-09-01 00:00:00

  • Inhibitory effect of ionized free intracellular calcium enhanced by ruthenium red and m-chloro-carbonylcyanide phenyl hydrazon on the evoked release of acetylcholine.

    abstract::In order to understand the relationship between the free ionized calcium concentration in the axon terminals and the transmitter release we have investigated the effect of ruthenium red (RuR) and m-chloro-carbonylcyanide phenyl hydrazon (CCCP), mitochondrial uncoupler agents on the liberation of acetylcholine from mye...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(87)90020-7

    authors: Bernath S,Vizi ES

    更新日期:1987-11-01 00:00:00

  • Thioredoxin reductase 1 knockdown enhances selenazolidine cytotoxicity in human lung cancer cells via mitochondrial dysfunction.

    abstract::Thioredoxin reductase (TR1) is a selenoprotein that is involved in cellular redox status control and deoxyribonucleotide biosynthesis. Many cancers, including lung, overexpress TR1, making it a potential cancer therapy target. Previous work has shown that TR1 knockdown enhances the sensitivity of cancer cells to antic...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2010.09.024

    authors: Poerschke RL,Moos PJ

    更新日期:2011-01-15 00:00:00

  • 86Rb+ efflux mediated by alpha4beta2*-nicotinic acetylcholine receptors with high and low-sensitivity to stimulation by acetylcholine display similar agonist-induced desensitization.

    abstract::The nicotinic acetylcholine receptors (nAChR) assembled from alpha4 and beta2 subunits are the most densely expressed subtype in the brain. Concentration-effect curves for agonist activation of alpha4beta2*-nAChR are biphasic. This biphasic agonist sensitivity is ascribed to differences in subunit stoichiometry. The s...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2010.06.040

    authors: Marks MJ,Meinerz NM,Brown RW,Collins AC

    更新日期:2010-10-15 00:00:00

  • Down-regulation of cytochrome P450 proteins and its activities by Shiga-like toxin II from Escherichia coli O157:H7.

    abstract::Escherichia coli O157:H7 infection frequently induces clinical complications such as hemolytic uremic syndromes and intestinal dysfunctions. These changes could alter the disposition of drugs, consequently changing their efficacy. However, the possible changes of drug-metabolizing activities by E. coli O157:H7 infecti...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2003.12.009

    authors: Kitaichi K,Nakayama H,Ueyama J,Nadai M,Baba K,Takagi K,Takagi K,Ohta M,Hasegawa T

    更新日期:2004-04-15 00:00:00

  • Inhibition of mammalian tumour thymidylate synthetase by 5-alkylated 2'-deoxyuridine 5'-phosphates.

    abstract::Improved syntheses, based on Lewis acid-catalyzed nucleosidation, are described for the preparation of 5-alkyl-2'-deoxyuridines. These were converted to their 5'-phosphates with the use of wheat shoot phosphotransferase. The dUMP analogues, 5-ethyl-dUMP and 5-propyl-dUMP, were competitive vs dUMP inhibitors of thymidy...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(84)90683-x

    authors: Rode W,Kulikowski T,Kedzierska B,Jastreboff M,Shugar D

    更新日期:1984-09-01 00:00:00

  • The angiogenic process as a therapeutic target in cancer.

    abstract::Angiogenesis has emerged as a critical process for tumour progression. Identifying key pathways involved in the regulation and promotion of angiogenesis has resulted in the development of numerous approaches targeting pro-angiogenic signalling pathways. The most prominent and characterised pro-angiogenic pathway is th...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.bcp.2011.02.016

    authors: Bridges EM,Harris AL

    更新日期:2011-05-15 00:00:00

  • Histamine H1 receptor-induced Ca2+ mobilization and prostaglandin E2 release in human gingival fibroblasts. Possible role of receptor-operated Ca2+ influx.

    abstract::Stimulation of human gingival fibroblasts with histamine elicited an increase in the intracellular concentration of free calcium ([Ca2+]i) and the formation of inositol 1,4,5-trisphosphate (InsP3) in a concentration- and time-dependent manner. The histamine-induced increase in [Ca2+]i was attenuated completely by chlo...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(96)00417-0

    authors: Niisato N,Ogata Y,Furuyama S,Sugiya H

    更新日期:1996-10-11 00:00:00

  • Hepatic metabolism and pulmonary toxicity of monocrotaline using isolated perfused liver and lung.

    abstract::Monocrotaline is a pyrrolizidine alkaloid obtained from the seeds of Crotalaria spectabilis. When perfused through an isolated liver, monocrotaline is metabolized to Ehrlich reactive (E+) metabolites. Metabolism of monocrotaline was faster in livers from male rats than female rats, was inducible with phenobarbital pre...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(84)90721-4

    authors: Lafranconi WM,Huxtable RJ

    更新日期:1984-08-01 00:00:00

  • Inhibition of G1/S transition potentiates oxaliplatin-induced cell death in colon cancer cell lines.

    abstract::In a series of colorectal cancer cell lines, both necrosis and apoptosis were induced upon exposure to oxaliplatin, and enhanced by co-administration of the Hsp90 inhibitor 17-AAG. We analyzed the effects of these interventions on the cell cycle, and found that oxaliplatin treatment caused G1 and G2 arrest in HCT116 c...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2007.01.037

    authors: Rakitina TV,Vasilevskaya IA,O'Dwyer PJ

    更新日期:2007-06-01 00:00:00

  • Dimethylsphingosine increases cytosolic calcium and intracellular pH in human T lymphocytes.

    abstract::N,N-Dimethyl-D-erythro-sphingosine (DMS) is the N-methyl derivative of sphingosine; both are activators of sphingosine-dependent protein kinases. The aim of this work was to study the effect of DMS on cytosolic calcium and intracellular pH (pHi) in human T lymphocytes. The variations of calcium and pH were determined ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0006-2952(02)01519-8

    authors: Alfonso A,De la Rosa LA,Vieytes MR,Botana LM

    更新日期:2003-02-01 00:00:00

  • Stem cell toxicity of oxazaphosphorine metabolites in comparison to their antileukemic activity.

    abstract::The oxazaphosphorine agent cyclophosphamide (CP) is an alkylating agent with a relative low stem cell toxicity. The aim of this study was to further evaluate the stem cell toxicity of the active metabolites of CP and its structural analogue ifosfamide (IFO) in comparison to their antileukemic efficacy. Cells of differ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0006-2952(02)00868-7

    authors: Brueggemann SK,Schlenke P,Klich S,Deeken M,Peters SO,Wagner T

    更新日期:2002-04-01 00:00:00

  • Heat shock protein 70 protects against bleomycin-induced pulmonary fibrosis in mice.

    abstract::Idiopathic pulmonary fibrosis (IPF) involves infiltration of leucocytes, pulmonary injury, fibrosis and resulting pulmonary dysfunction. Myofibroblasts and transforming growth factor (TGF)-beta1 have been suggested to play a major role in the pathology and the myofibroblasts are derived from both lung epithelial cells...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2010.05.025

    authors: Tanaka K,Tanaka Y,Namba T,Azuma A,Mizushima T

    更新日期:2010-09-15 00:00:00

  • Suppression of beta-catenin signaling by liver X receptor ligands.

    abstract::The nuclear receptors liver X receptor (LXR) alpha and LXRbeta serve as oxysterol receptors and play an important role in the regulation of lipid metabolism. We investigated the potential effects of LXRs on pathways of colon carcinogenesis and found that LXR activation suppresses the transactivation activity of beta-c...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2008.10.007

    authors: Uno S,Endo K,Jeong Y,Kawana K,Miyachi H,Hashimoto Y,Makishima M

    更新日期:2009-01-15 00:00:00

  • Fas/CD95-mediated apoptosis in human glioblastoma cells: a target for sensitisation to topoisomerase I inhibitors.

    abstract::The expression of the death receptor Fas/CD95 is cell type-specific and can be modulated by different cytotoxic treatments. In spite of a frequent expression of Fas/CD95 in high-grade gliomas, these tumours are typically refractory to conventional therapy. Using a human glioblastoma cell line (GBM), we explored the po...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0006-2952(01)00837-1

    authors: Ciusani E,Perego P,Carenini N,Corna E,Facchinetti F,Boiardi A,Salmaggi A,Zunino F

    更新日期:2002-03-01 00:00:00

  • Molecular and functional characterization of flavin-containing monooxygenases in cynomolgus macaque.

    abstract::Flavin-containing monooxygenases (FMOs), drug-metabolizing enzymes essential for the metabolism of endogenous biochemicals and foreign compounds, have been characterized in human (including FMO1-5 and FMO6P), but remain to be investigated in cynomolgus macaque. In this study, cDNAs of cynomolgus FMO1-5 and FMO6 were i...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2013.04.012

    authors: Uno Y,Shimizu M,Yamazaki H

    更新日期:2013-06-15 00:00:00

  • Evaluation of in vitro PXR-based assays and in silico modeling approaches for understanding the binding of a structurally diverse set of drugs to PXR.

    abstract::The pregnane X-receptor (PXR) is a promiscuous nuclear receptor primarily responsible for the induction of genes from the cytochrome P450 3A family. In this study, we used a previously described PXR/SRC tethered protein to establish two in vitro assays for identifying PXR ligands: automated ligand identification syste...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2010.12.003

    authors: Xiao L,Nickbarg E,Wang W,Thomas A,Ziebell M,Prosise WW,Lesburg CA,Taremi SS,Gerlach VL,Le HV,Cheng KC

    更新日期:2011-03-01 00:00:00

  • 13-cis retinoic acid and isomerisation in paediatric oncology--is changing shape the key to success?

    abstract::Retinoic acid isomers have been used with some success as chemotherapeutic agents, most recently with 13-cis retinoic acid showing impressive clinical efficacy in the paediatric malignancy neuroblastoma. The aim of this commentary is to review the evidence that 13-cis retinoic acid is a pro-drug, and consider the impl...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.bcp.2005.02.003

    authors: Armstrong JL,Redfern CP,Veal GJ

    更新日期:2005-05-01 00:00:00

  • A novel steroidal inhibitor of estrogen-related receptor alpha (ERR alpha).

    abstract::The orphan nuclear receptor estrogen-related receptor alpha (ERRalpha) has been implicated in the development of various human malignancies, including breast, prostate, ovary, and colon cancer. ERRalpha, bound to a co-activator protein (e.g., peroxisome proliferator receptor gamma co-activator-1alpha, PGC-1alpha), reg...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2010.05.024

    authors: Duellman SJ,Calaoagan JM,Sato BG,Fine R,Klebansky B,Chao WR,Hobbs P,Collins N,Sambucetti L,Laderoute KR

    更新日期:2010-09-15 00:00:00

  • Binding of indapamide to serum proteins and erythrocytes.

    abstract::The binding of indapamide to isolated serum proteins and erythrocytes was studied in order to understand its blood distribution. In serum, indapamide was mainly bound to alpha 1-acid glycoprotein with a high affinity (K = 73.4/mM), and to albumin and lipoproteins. Indapamide was bound to erythrocytes via a saturable p...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(88)90282-1

    authors: Urien S,Riant P,Renouard A,Coulomb B,Rocher I,Tillement JP

    更新日期:1988-08-01 00:00:00

  • Inhibition of hepatic carnitine palmitoyl-transferase I (CPT IA) by valproyl-CoA as a possible mechanism of valproate-induced steatosis.

    abstract:BACKGROUND/AIMS:Carnitine palmitoyl-transferase I (CPT I) catalyses the synthesis of long-chain (LC)-acylcarnitines from LC-acyl-CoA esters. It is the rate-limiting enzyme of mitochondrial fatty acid beta-oxidation (FAO) pathway and its activity is regulated by malonyl-CoA. The antiepileptic drug valproic acid (VPA) is...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2009.10.011

    authors: Aires CC,Ijlst L,Stet F,Prip-Buus C,de Almeida IT,Duran M,Wanders RJ,Silva MF

    更新日期:2010-03-01 00:00:00

  • Activation mechanism of the heterodimeric GABA(B) receptor.

    abstract::The GABA(B) receptor was the first heteromeric G-protein coupled receptor (GPCR) identified. Indeed, both GABA(B1) and GABA(B2) subunits appear necessary to get a functional GABA(B) receptor. Soon after the cloning of both subunits, it was demonstrated that GABA(B2) was required for GABA(B1) to reach the cell surface....

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2004.06.035

    authors: Pin JP,Kniazeff J,Binet V,Liu J,Maurel D,Galvez T,Duthey B,Havlickova M,Blahos J,Prézeau L,Rondard P

    更新日期:2004-10-15 00:00:00

  • Cadmium induces apoptotic cell death in WI 38 cells via caspase-dependent Bid cleavage and calpain-mediated mitochondrial Bax cleavage by Bcl-2-independent pathway.

    abstract::Previous reports have demonstrated that cadmium (Cd) may induce cell death via apoptosis, but the mechanism responsible for cellular death is not clear. In this study, we investigated the signaling pathways implicated in Cd-induced apoptosis in lung epithelial fibroblast (WI 38) cells. Apoptotic features were observed...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2004.06.021

    authors: Oh SH,Lee BH,Lim SC

    更新日期:2004-11-01 00:00:00

  • Inverse gene expression patterns for macrophage activating hepatotoxicants and peroxisome proliferators in rat liver.

    abstract::Macrophage activation contributes to adverse effects produced by a number of hepatotoxic compounds. Transcriptional profiles elicited by two macrophage activators, LPS and zymosan A, were compared to those produced by 100 paradigm compounds (mostly hepatotoxicants) using cDNA microarrays. Several hepatotoxicants previ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2004.01.029

    authors: McMillian M,Nie AY,Parker JB,Leone A,Kemmerer M,Bryant S,Herlich J,Yieh L,Bittner A,Liu X,Wan J,Johnson MD

    更新日期:2004-06-01 00:00:00

  • The measurement of polyglutamate metabolites of the thymidylate synthase inhibitor, ICI D1694, in mouse and human cultured cells.

    abstract::A method is described for the measurement of the polyglutamates of the quinazoline thymidylate synthase inhibitor, N-(5-[N-(3,4-dihydro-2-methyl-4-oxoquinazolin- 6-ylmethyl)-N-methylamino]-2-theonyl)-L-glutamic acid (ICI D1694). This involved incubation of cells with [5-3H]ICI D1694, extraction of the polyglutamates a...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(93)90170-2

    authors: Gibson W,Bisset GM,Marsham PR,Kelland LR,Judson IR,Jackman AL

    更新日期:1993-02-24 00:00:00