Effects of suramin on increases in cytosolic calcium and on inhibition of adenylate cyclase induced by adenosine 5'-diphosphate in human platelets.


:The effects of the P2-purinoceptor antagonist, suramin, on ADP-induced increases in human platelet cytosolic calcium concentration ([Ca2+]i) and inhibition of prostaglandin E1 (PGE1)-stimulated adenylate cyclase activity were investigated. Suramin (50-200 microM) acted as an antagonist of ADP-induced increases in [Ca2+]i, causing parallel, rightward shifts of the log concentration-response curve to ADP with no apparent depression of the maximal response. However, the slope of the Schild plot was 2.3 +/- 0.3, similar to that obtained in previous studies on aggregation, indicating that the antagonism was not simply competitive. The apparent pA2 for suramin, taken from the Schild plot, was 4.63, similar to that for suramin's inhibition of aggregation, which suggests that these two effects are closely related. Suramin was not specific for the ADP receptor, however, as it was also able to inhibit, non-competitively, increases in [Ca2+]i induced by 5-hydroxytryptamine. Suramin (50-400 microM) also inhibited the effect of ADP on PGE1-stimulated accumulation of cyclic AMP, causing parallel shifts of the log concentration-response curve to ADP, with a Schild plot slope of 1.00 +/- 0.10, suggesting competitive antagonism, and a pA2 value of 5.09. Suramin (400 microM) did not reduce the inhibition of cyclic AMP accumulation by adrenaline, although it was able to inhibit the accumulation of cyclic AMP caused by PGE1, again showing that suramin has some non-specific effects. These data suggest that suramin is an antagonist at the platelet ADP receptor mediating increases in [Ca2+]i and inhibition of adenylate cyclase, but that it also shows non-specific effects and can depress platelet responses to other agonists. In addition, the similar pA2 value of suramin for the two effects of ADP does not support suggestion that they are mediated by two different receptors on human platelets.


Biochem Pharmacol


Biochemical pharmacology


Hall DA,Hourani SM




Has Abstract


1994-03-15 00:00:00














  • The effects of inhibiting choline dehydrogenase on choline metabolism in mice.

    abstract::3,3-Dimethylbutanol (Dimbunol), a competitive inhibitor of choline dehydrogenase (CDH), and ethylcholine mustard aziridinium (ECMA), an effective irreversible inhibitor of both CDH and choline transport, were investigated for their effects upon the uptake and metabolism of [3H]choline in mice. Thirty minutes after Dim...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Barlow P,Marchbanks RM

    更新日期:1985-09-01 00:00:00

  • Eg5 targeting agents: From new anti-mitotic based inhibitor discovery to cancer therapy and resistance.

    abstract::Eg5, the product of Kif11 gene, also known as kinesin spindle protein, is a motor protein involved in the proper establishment of a bipolar mitotic spindle. Eg5 is one of the 45 different kinesins coded in the human genome of the kinesin motor protein superfamily. Over the last three decades Eg5 has attracted great in...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审


    authors: Garcia-Saez I,Skoufias DA

    更新日期:2020-12-11 00:00:00

  • Studies on the mechanism of histamine-induced release of noradrenaline and 5-hydroxytryptamine from slices of rat cerebral cortex.

    abstract::The effect of histamine on the release of endogenous noradrenaline and 5-hydroxytryptamine (5-HT) has been examined in slices of rat cerebral cortex. Histamine was found to produce a marked release of both amines from rat cerebral cortex at concentrations between 0.1 and 1 mM. This response to histamine was relatively...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Young CS,Mason R,Hill SJ

    更新日期:1988-07-15 00:00:00

  • Effect of 3'-deoxythymidin-2'-ene (d4T) on nucleoside metabolism in H9 cells.

    abstract::The effect of 3'-deoxythymidin-2'-ene (d4T) on the metabolism of exogenously supplied radiolabeled nucleosides was investigated. Following a 24-hr exposure to 250 microM d4T, we observed no significant effect on the incorporation of [3H]thymidine or [3H]deoxycytidine into DNA. In contrast, the amounts of [3H]uridine, ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Marongiu ME,August EM,Prusoff WH

    更新日期:1990-05-15 00:00:00

  • Inhibition of indoleamine 2,3-dioxygenase activity in IFN-gamma stimulated astroglioma cells decreases intracellular NAD levels.

    abstract::Astroglia provide essential metabolic and neurotropic support to cells within the CNS and participate in the cellular immune response with microglia/macrophages following activation by the pro-inflammatory cytokine IFN-gamma. Activation of glial cells results in local oxidative stress and induction of a number of prot...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Grant R,Kapoor V

    更新日期:2003-09-15 00:00:00

  • Contribution of non-ADH pathways to ethanol oxidation in hepatocytes from fed and hyperthyroid rats. Effect of fructose and xylitol.

    abstract::The metabolism of (1R)[1-3H]ethanol, [2-3H]lactate or [2-3H]xylitol was studied in hepatocytes from fed or T3-treated rats in the presence or absence of fructose or xylitol. The yields of tritium in ethanol, lactate, water, glycerol and glucose were determined. A simple model, describing the metabolic fate of tritium ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Vind C,Grunnet N

    更新日期:1985-03-01 00:00:00

  • Organic copper complexes as a new class of proteasome inhibitors and apoptosis inducers in human cancer cells.

    abstract::Here we report that organic copper complexes can potently and selectively inhibit the chymotrypsin-like activity of the proteasome in vitro and in vivo. Several copper compounds, such as NCI-109268 and bis-8-hydroxyquinoline copper(II) [Cu(8-OHQ)(2)], can inhibit the chymotrypsin-like activity of purified 20S proteaso...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Daniel KG,Gupta P,Harbach RH,Guida WC,Dou QP

    更新日期:2004-03-15 00:00:00

  • Hydroxylamine and phenol-induced formation of methemoglobin and free radical intermediates in erythrocytes.

    abstract::As previously shown with isolated oxyhemoglobin, methemoglobin formation can also be induced in intact erythrocytes by hydroxylamine compounds and substituted phenols such as butylated hydroxyanisole (BHA). Electron spin resonance investigations revealed that, accordingly, free radical intermediates were formed in ery...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Stolze K,Dadak A,Liu Y,Nohl H

    更新日期:1996-12-24 00:00:00

  • Antagonistic effect of the cardioprotector (+)-1,2-bis(3,5-dioxopiperazinyl-1-yl)propane (ICRF-187) on DNA breaks and cytotoxicity induced by the topoisomerase II directed drugs daunorubicin and etoposide (VP-16).

    abstract::The effect of the bisdioxopiperazine cardioprotector ICRF-187 (ADR-529, dexrazoxan) on drug-induced DNA damage and cytotoxicity was studied. Using alkaline elution assays, ICRF-187 in a dose-dependent manner inhibited the formation of DNA single strand breaks (SSBs) as well as DNA-protein cross-links induced by drugs ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Sehested M,Jensen PB,Sørensen BS,Holm B,Friche E,Demant EJ

    更新日期:1993-08-03 00:00:00

  • Interaction of permanently charged analogs of dopamine with the D-2 dopaminergic receptor.

    abstract::Dopamine can exist in both charged and uncharged forms at physiological pH. At present it is unclear which of these forms is responsible for dopaminergic agonist activity. The purpose of this study was to determine whether permanently charged structural analogs of dopamine containing either a nitrogen, sulfur, or sele...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Wallace RA,Farooqui T,Wallace L,Ares J,Chang YA,Miller D,Uretsky N

    更新日期:1987-11-15 00:00:00

  • Antitumor 1-nitroacridine derivative C-1748, induces apoptosis, necrosis or senescence in human colon carcinoma HCT8 and HT29 cells.

    abstract::C-1748 is a DNA-binding agent with potent antitumor activity, especially towards prostate and colon carcinoma xenografts in mice. Here, we elucidated the nature of cellular response of human colon carcinoma HCT8 and HT29 cells to C-1748 treatment, at biologically relevant concentrations (EC(90) and their multiplicity)...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Augustin E,Moś-Rompa A,Nowak-Ziatyk D,Konopa J

    更新日期:2010-05-01 00:00:00

  • Enhancement of paclitaxel-induced microtubule stabilization, mitotic arrest, and apoptosis by the microtubule-targeting agent EM012.

    abstract::EM012, a semisynthetic phthalideisoquinoline alkaloid, has been recently found to target microtubules and possess anti-cancer activity. In this study, we evaluated the effects of EM012 in combination with the classic microtubule-targeting agent paclitaxel. Our results demonstrated that EM012 enhanced the anti-prolifer...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Zhou J,Liu M,Aneja R,Chandra R,Joshi HC

    更新日期:2004-12-15 00:00:00

  • Hepatic protein tyrosine phosphatase 1B (PTP1B) deficiency protects against obesity-induced endothelial dysfunction.

    abstract::Growing evidence suggests that hepatic-insulin resistance is sufficient to promote progression to cardiovascular disease. We have shown previously that liver-specific protein-tyrosine-phosphatase 1B (PTP1B) deficiency improves hepatic-insulin sensitivity and whole-body glucose homeostasis. The aim of this study was to...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Agouni A,Tual-Chalot S,Chalopin M,Duluc L,Mody N,Martinez MC,Andriantsitohaina R,Delibegović M

    更新日期:2014-12-15 00:00:00

  • Inhibition of gastric tumor growth by a novel Hsp90 inhibitor.

    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

    pub_type: 杂志文章


    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

  • Metabolic profiling of praziquantel enantiomers.

    abstract::Praziquantel (PZQ), prescribed as a racemic mixture, is the most readily available drug to treat schistosomiasis. In the present study, ultra-performance liquid chromatography coupled with electrospray ionization quadrupole time-of-flight mass spectrometry (UPLC-ESI-QTOFMS) based metabolomics was employed to decipher ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Wang H,Fang ZZ,Zheng Y,Zhou K,Hu C,Krausz KW,Sun D,Idle JR,Gonzalez FJ

    更新日期:2014-07-15 00:00:00

  • MZF1 possesses a repressively regulatory function in ERCC1 expression.

    abstract::ERCC1 is a critical gene within the nucleotide excision repair pathway. Overexpression of ERCC1 through promoter-mediating transcriptional regulation is associated with repair of cisplatin-induced DNA damage and clinical resistance to platinum-chemotherapy. Several transcriptional repressors and activators within the ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Yan QW,Reed E,Zhong XS,Thornton K,Guo Y,Yu JJ

    更新日期:2006-03-14 00:00:00

  • The effect of metformin in EML4-ALK+ lung cancer alone and in combination with crizotinib in cell and rodent models.

    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

    pub_type: 杂志文章


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

    更新日期:2021-01-01 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

  • Sulphate conjugation of minoxidil in rat skin.

    abstract::Minoxidil sulphotransferase (MST) activity was determined in the cytosolic fraction of rat skin and liver. MST of rat skin is similar to the P (phenol)-form of phenosulphotransferase (PST) of human tissues with respect to thermostability and inhibition by 2,6-dichloro-4-nitrophenol (DCNP). p-Nitrophenol, a prototype s...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Wong KO,Tan AY,Lim BG,Wong KP

    更新日期:1993-03-09 00:00:00

  • A novel approach for stress-induced gastritis based on paradoxical anti-oxidative and anti-inflammatory action of exogenous 8-hydroxydeoxyguanosine.

    abstract::Reactive oxygen species (ROS) attack guanine bases in DNA and form 8-hydroxydeoxyguanosine (8-OHdG), which has been regarded simply as an oxidative mutagenic by-product. On the other hand, our previous report showed paradoxically ROS attenuating action of generated 8-OHdG. In the current study, both in vitro and in vi...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Ock CY,Hong KS,Choi KS,Chung MH,Kim Ys,Kim JH,Hahm KB

    更新日期:2011-01-01 00:00:00

  • Effects of the novel vascular targeting agent MDS-11P on tumor vascularity and its antitumor activity.

    abstract::Vascular disrupting agents show selective effects on tumor established vasculature, and achieve encouraging results in both pre-clinical and clinical experiments. In the present study, we investigated the effects of a new CA4 derivative MDS-11 and its prodrug MDS-11P on vascular disrupting activity in vitro and in viv...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Deng ZT,Feng T,Wang P,Qi X,Chen XH,Li YX,Song CL,Geng MY,Li J

    更新日期:2011-12-15 00:00:00

  • Reduced hepatic expression of CYP7A1 and CYP2C13 in rats with spontaneous hyperlipidaemia.

    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

    pub_type: 杂志文章


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

    更新日期:1998-07-15 00:00:00

  • Effect of methylated bepridil on slow action potentials in cardiac muscle and vascular smooth muscle.

    abstract::The anti-anginal agent bepridil blocks slow Ca2+ channels in a variety of tissues. Since bepridil accumulates inside cells, the possibility exists that bepridil acts, at least partially, from inside the cell. To test this possibility, we examined the effects of a quaternary ammonium analog of bepridil, methylated bepr...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Wahler GM,Doane JD,Ousterhout JM,Sperelakis N,Lamar JC,Busch N,Biswas JC,Rogers TB

    更新日期:1986-07-15 00:00:00

  • Heterogeneity of rabbit hepatocytes for bile secretion after acinar zone 3 damage induced by bromobenzene. Effect of bilirubin and bile salt infusions.

    abstract::Anaesthetized rabbits were used to study the effect of bromobenzene-induced hepatic damage to the acinar zone 3 on bile flow, bile salt, sodium secretion as well as bilirubin transport in basal conditions or with infusion of sodium glycodeoxycholate. The bromobenzene-pretreated animals exhibited in basal conditions a ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: González J,Esteller A

    更新日期:1985-02-15 00:00:00

  • Inducibility of P450Coh by pyrazole and its derivatives.

    abstract::Pyrazole and several of its derivatives increase the hepatic microsomal coumarin 7-hydroxylase to a variable extent. The strongest inducers are pyrazole itself and those derivatives which have a hydroxy group or a halogen at the 4-position of the molecule. The increase in coumarin 7-hydroxylase is due to an increase i...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Kojo A,Heiskanen R,Rytkönen AL,Honkakoski P,Juvonen R,Lang M

    更新日期:1991-10-09 00:00:00

  • Affinity, potency, efficacy, selectivity, and molecular modeling of substituted fentanyls at opioid receptors.

    abstract::Substituted fentanyls are abused and cause rapid fatal overdose. As their pharmacology is not well characterized, we examined in vitro pharmacology and structure-activity relationships of 22 substituted fentanyls with modifications of the fentanyl propyl group, and conducted in silico receptor/ligand modeling. Affinit...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Eshleman AJ,Nagarajan S,Wolfrum KM,Reed JF,Nilsen A,Torralva R,Janowsky A

    更新日期:2020-12-01 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

  • Enhanced DNA excision repair in CCRF-CEM cells resistant to 1,3-bis(2-chloroethyl)-1-nitrosourea, quantitated using the single cell gel electrophoresis (Comet) assay.

    abstract::Enhanced DNA repair activity is important for the development of cellular resistance to alkylating agents. Here, we quantitated the kinetics of DNA excision repairs initiated by 1,3-bis(2-chloroethyl)-1-nitrosourea (BCNU) in human leukemia CCRF-CEM cells. CEM cells that had been established resistant to BCNU (CEM-R) w...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Yamauchi T,Kawai Y,Ueda T

    更新日期:2003-09-15 00:00:00

  • Deoxyelephantopin inhibits cancer cell proliferation and functions as a selective partial agonist against PPARgamma.

    abstract::Deoxyelephantopin (ESD) was reported to potentiate apoptosis, inhibit invasion and abolish osteoclastogenesis but no target protein was disclosed. Here, we discovered that ESD could significantly inhibit the proliferation of different cancer cells and induce apoptosis and cell cycle arrest at G(2)/M phase in HeLa cell...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Zou G,Gao Z,Wang J,Zhang Y,Ding H,Huang J,Chen L,Guo Y,Jiang H,Shen X

    更新日期:2008-03-15 00:00:00

  • Effects of ticlopidine, a new platelet antiaggregating agent, and its analogues on mitochondrial metabolism. Oxidative phosphorylation, protein synthesis and DNA polymerase activity.

    abstract::The effects of ticlopidine and six of its analogues on mitochondrial functions were studied in isolated rat liver mitochondria. The influence of ticlopidine and each of the following analogues: PCR 5325, PCR 4099, PCR 3787, PCR 2362, PCR 4499 and PCR 0665 was evaluated by determining their interaction with three major...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Abou-Khalil WH,Lim LO,Yunis AA,Abou-Khalil S

    更新日期:1984-12-01 00:00:00