The lack of correlation between toxicity and free radical formation of two diaziridinyl benzoquinones.

abstract：:Enhanced aggregation of platelets was observed in platelet-rich plasma, but not in washed platelet suspension (WPS), during acute inflammation in rats. Incubation of WPS with inflammatory plasma increased the aggregatory response to ADP, but the plasma itself did not cause aggregation of platelets. It potentiated the ...

journal_title：Biochemical pharmacology

authors： Srivastava R,Srimal RC

更新日期：1990-07-15 00:00:00

abstract：:The present study aimed to investigate endothelin-1 (ET-1) receptors in human and swine cardiomyocytes with binding studies using ET(A) and ET(B) selective receptor antagonists (BMS-182874 and BQ-788, respectively). Cell distribution of mRNA expression for ET(A) and ET(B) subtypes was investigated by in situ hybridiza...

journal_title：Biochemical pharmacology

authors： Modesti PA,Vanni S,Paniccia R,Perna A,Maccherini M,Lisi G,Sani G,Neri Serneri GG

更新日期：1999-07-15 00:00:00

abstract：:Dravet syndrome (DS) is a catastrophic epileptic encephalopathy characterised by childhood-onset polymorphic seizures, multiple neuropsychiatric comorbidities, and increased risk of sudden death. Heterozygous loss-of-function mutations in one allele of SCN1A, the gene encoding the voltage-gated sodium channel 1.1 (NaV...

journal_title：Biochemical pharmacology

authors： Chow CY,Chin YKY,Ma L,Undheim EAB,Herzig V,King GF

更新日期：2020-11-01 00:00:00

abstract：:Cytidine deaminase, an enzyme found in the supernatant fluid of hepatocytes, granulocytes and tumor cells, and in plasma, degrades the antitumor agents cytosine arabinoside and 5-azacytidine. Uridine and its analogs, 3-deazauridine, 5-bromodeoxyuridine, 5-fluorodeoxyuridine and 6-azauridine, were found to competitivel...

journal_title：Biochemical pharmacology

authors： Drake JC,Hande KR,Fuller RW,Chabner BA

更新日期：1980-03-01 00:00:00

abstract：:The cytochrome P450-dependent metabolism of benzo(a)pyrene and other xenobiotics has been investigated in liver microsomes prepared from a local marine safi fish, Siganus canaliculatus. The safi fish was found to have a well-developed microsomal monooxygenase system consisting of cytochrome P450, cytochrome b5 and NAD...

journal_title：Biochemical pharmacology

authors： Raza H,Otaiba A,Montague W

更新日期：1995-10-26 00:00:00

abstract：:Hepatic expression of multiple cytochrome P450 genes is suppressed in the livers of rats undergoing an inflammatory response. Nitric oxide (NO) released during inflammation has been implicated in the decreased activities and expression of several cytochrome P450 isozymes. We examined the role of cytokine-mediated NO r...

journal_title：Biochemical pharmacology

authors： Sewer MB,Morgan ET

更新日期：1997-09-15 00:00:00

abstract：:Hyperactivated macrophages play a key role in the initiation and perpetuation of mucosal inflammation in Crohn's disease (CD). Increasing evidence suggests that the basic helix-loop-helix (bHLH) repressor Twist1 can suppress activation of nuclear factor-κB (NF-κB) and the subsequent production of TNF-α, which are both...

journal_title：Biochemical pharmacology

authors： Tu T,Yu M,Zhang Y,Shi X,Xu J,Hu J,Gan J,He W,Dong L,Han J,Huang Z,Pan Y,Zhang J

更新日期：2018-09-01 00:00:00

abstract：:Apo 2 ligand/tumor necrosis factor (TNF)-related apoptosis-inducing ligand (Apo2L/TRAIL), is a member of the TNF family of cytokines, which can induce apoptotic cell death in cells expressing at least one of their specific death receptors, DR4 (TRAIL-R1) or DR5 (TRAIL-R2). In the last decade, the Apo2L/TRAIL system of...

journal_title：Biochemical pharmacology

authors： Martinez-Lostao L,Marzo I,Anel A,Naval J

更新日期：2012-06-01 00:00:00

abstract：:BAY X 1005 ((R)-2-[4-(quinolin-2-yl-methoxy)phenyl]-2-cyclopentyl acetic acid) has been demonstrated to be a potent inhibitor of leukotriene B4 (LTB4) and 5-hydroxyeicosatetraenoic acid (5-HETE) synthesis in various in vitro systems. Using mainly human polymorphonuclear leukocytes (PMNL) this study elucidates the mech...

journal_title：Biochemical pharmacology

authors： Hatzelmann A,Fruchtmann R,Mohrs KH,Raddatz S,Müller-Peddinghaus R

更新日期：1993-01-07 00:00:00

abstract：:trans-Resveratrol is a dietary polyphenolic compound present in grapes, which has been shown to exhibit strong anti-inflammatory, antioxidant, and chemopreventive activities. In this study we have compared the in vitro and in vivo effects of resveratrol on the development of various cell-mediated immune responses, inc...

journal_title：Biochemical pharmacology

authors： Gao X,Deeb D,Media J,Divine G,Jiang H,Chapman RA,Gautam SC

更新日期：2003-12-15 00:00:00

abstract：:Partial agonists for G protein-coupled receptors (GPCRs) provide opportunities for novel pharmacotherapies with enhanced on-target safety compared to full agonists. For the human adenosine A1 receptor (hA1AR) this has led to the discovery of capadenoson, which has been in phase IIa clinical trials for heart failure. A...

journal_title：Biochemical pharmacology

authors： Yang X,Dilweg MA,Osemwengie D,Burggraaff L,van der Es D,Heitman LH,IJzerman AP

更新日期：2020-10-01 00:00:00

abstract：:Nucleoside diphosphokinase (NDK) of human platelets has been purified by chromatography on Blue Sepharose CL-6B gel (purification factor of 950) and shown to be free of adenylate kinase, ATPase and adenylate cyclase. The molecular weight was 70,000 with subunits of 17,000. The pH optimum was 8.0 Km values for ATP and ...

journal_title：Biochemical pharmacology

authors： Lam SC,Packham MA

更新日期：1986-12-15 00:00:00

abstract：:Glutathione (GSH) is important in protection of cells against electrophilic drug injury and against reactive oxygen species. Both steady-state concentrations and turnover of GSH are important determinants of susceptibility of the hepatocyte to injury. Chronic ethanol administration is known to enhance susceptibility t...

journal_title：Biochemical pharmacology

authors： Morton S,Mitchell MC

更新日期：1985-05-01 00:00:00

abstract：:A calcium antagonist, verapamil, enhanced the cellular uptake and cytotoxicity of vincristine (VCR) in adriamycin-resistant P388 leukemia (P388/ADM) cells and also enhanced the cellular uptake and cytotoxicity of adriamycin (ADM) in vincristine-resistant P388 leukemia (P388/VCR) and P388/ADM cells. The enhancement of ...

journal_title：Biochemical pharmacology

authors： Tsuruo T,Iida H,Yamashiro M,Tsukagoshi S,Sakurai Y

更新日期：1982-10-01 00:00:00

abstract：:A selected number of 1,3-diaminobenzo[f]quinazolines and 1,3-diamino-5,6-dihydrobenzo[f]quinazolines, which may be viewed as tricyclic analogues of the lipid-soluble antifolates pyrimethamine (PM), metoprine (DDMP), and etoprine (DDEP), were tested as inhibitors of purified dihydrofolate reductase (DHFR) from WI-L2 ly...

journal_title：Biochemical pharmacology

authors： Rosowsky A,Freisheim JH,Hynes JB,Queener SF,Bartlett M,Smith JW,Lazarus H,Modest EJ

更新日期：1989-08-15 00:00:00

abstract：:Neurotoxic esterase (NTE) is a membrane-bound protein found in highest concentration in brain and lymphocytes. The enzyme has no known physiological function, but its organophosphorylation and aging in neural tissue are thought to trigger the pathogenesis of organophosphorus-induced delayed neuropathy (OPIDN). Solubil...

journal_title：Biochemical pharmacology

authors： Davis CS,Richardson RJ

更新日期：1987-05-01 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：:The PI3K/AKT/mTOR signaling pathway regulates cell proliferation, survival and angiogenesis. The mammalian target of rapamycin (mTOR) is a protein kinase ubiquitously expressed within cells that regulates cell growth and survival by integrating nutrient and hormonal signals. mTOR exists in two complexes, mTORC1 and mT...

journal_title：Biochemical pharmacology

authors： Espona-Fiedler M,Soto-Cerrato V,Hosseini A,Lizcano JM,Guallar V,Quesada R,Gao T,Pérez-Tomás R

更新日期：2012-02-15 00:00:00

abstract：:Castanospermine (CS) is a potent but non-selective inhibitor of many glycohydrolases including the intestinal disaccharidases. Several CS-glucosides were synthesized to investigate the effect of an attached glucopyranosyl residue on the potency and selectivity of CS toward inhibition of intestinal disaccharidases. 8 a...

journal_title：Biochemical pharmacology

authors： Rhinehart BL,Robinson KM,King CH,Liu PS

更新日期：1990-05-15 00:00:00

abstract：:LLC-PK(1) is a proximal tubular cell line derived from normal pig kidney which has a structure and function similar to those of renal proximal tubular cells and which expresses baseline levels of P-glycoprotein. We isolated by drug selection a doxorubicin-resistant cell line (LLC-PK(1)/ADR) that exhibited a multidrug-...

journal_title：Biochemical pharmacology

authors： Decorti G,Rosati A,Candussio L,Giraldi T,Bartoli Klugmann F

更新日期：2001-01-01 00:00:00

abstract：:Clonidine, idazoxan, and related imidazoline adrenergic drugs bind to non-adrenergic sites in brain and several peripheral tissues. These sites, termed imidazoline receptors, appear to exist in two major subclasses, I1 sites labeled by clonidine and I2 sites labeled by idazoxan. In this study, we investigated whether ...

journal_title：Biochemical pharmacology

authors： Regunathan S,Nassir Y,Sundaram K,Vaughan ED Jr,Reis DJ,Felsen D

更新日期：1996-02-23 00:00:00

abstract：:Inflammatory bowel disease (IBD) is an incurable disease which affects millions of people in industrialized countries. Anecdotal and scientific evidence suggests that Cannabis use may have a positive impact in IBD patients. Here, we investigated the effect of cannabigerol (CBG), a non-psychotropic Cannabis-derived can...

journal_title：Biochemical pharmacology

authors： Borrelli F,Fasolino I,Romano B,Capasso R,Maiello F,Coppola D,Orlando P,Battista G,Pagano E,Di Marzo V,Izzo AA

更新日期：2013-05-01 00:00:00

abstract：:It has been hypothesized that oxidative modification of low density lipoprotein plays a key role in the pathogenesis of atherosclerosis. In order to elucidate the role of lipid oxidation and its inhibition in vivo, apolipoprotein E and alpha-tocopherol (alphaT) transfer protein double knockout (ApoE(-/-)alpha-TTP(-/-)...

journal_title：Biochemical pharmacology

authors： Yoshida Y,Hayakawa M,Itoh N,Habuchi Y,Inoue R,Chen ZH,Cao J,Cynshi O,Jishage K,Niki E

更新日期：2007-10-01 00:00:00

abstract：:Adult hepatocytes from rat and man were maintained for 2 weeks between two gel layers in a sandwich configuration to study the influence of this culture technique on the preservation of basal activities of xenobiotic-metabolizing phase I and phase II enzymes. The response of these enzyme activities to an enzyme induce...

journal_title：Biochemical pharmacology

authors： Kern A,Bader A,Pichlmayr R,Sewing KF

更新日期：1997-10-01 00:00:00

abstract：:Hepatic stellate cells (HSCs) are the primary source of matrix components in hepatic fibrosis. Ferulic acid (FA) has antifibrotic potential in renal and cardiac disease. However, whether FA comprises inhibitive effects of HSCs activation remains to be clarified. This study aims at evaluating the hypothesis that FA inh...

journal_title：Biochemical pharmacology

authors： Xu T,Pan Z,Dong M,Yu C,Niu Y

更新日期：2015-01-01 00:00:00

abstract：:Heme oxygenase 1 (HO-1) is a stress protein and has been suggested to provide defense mechanisms against agents that may induce oxidative injury. Vitamin E (VE) is considered to function as an important cellular antioxidant. Rats were fed a VE-deficient (0E) or a VE-sufficient (10E) diet for 6 weeks and then were intr...

journal_title：Biochemical pharmacology

authors： Ito K,Yano T,Hagiwara K,Ozasa H,Horikawa S

更新日期：1997-11-15 00:00:00

abstract：:Leydig and Sertoli cells of the rat testes differ with respect to the activities of the enzymes of the heme and hemoprotein degradative pathway and in their responses to Cd2+ treatment. The microsomal heme oxygenase activity in the Leydig cell preparations was nearly 9- to 10-fold greater than in Sertoli cell preparat...

journal_title：Biochemical pharmacology

authors： Maines MD

更新日期：1984-05-01 00:00:00

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

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

更新日期：2006-08-28 00:00:00

abstract：:The chemotherapeutic drug cisplatin is an important treatment for many types of solid tumours, in particular non-small cell lung cancer (NSCLC). Platinum(IV) complexes offer several advantages to cisplatin due to their requirement for reduction to the active platinum(II) form to elicit cytotoxicity. This should minimi...

journal_title：Biochemical pharmacology

authors： Mellor HR,Snelling S,Hall MD,Modok S,Jaffar M,Hambley TW,Callaghan R

更新日期：2005-10-15 00:00:00

abstract：:Disodium cromoglycate and compounds which elevated levels of cyclic AMP in the mast cell variously inhibited cytotoxic histamine release induced by the surface active agents melittin, Tween 20 and Triton X-100. These results are inconsistent with the postulated effects of the drugs on receptor mediated calcium channel...

journal_title：Biochemical pharmacology

authors： Pearce FL,Clements J

更新日期：1982-07-01 00:00:00