Receptor-independent G protein activation may account for the stimulatory effects of first-generation H1-receptor antagonists in HL-60 cells, basophils, and mast cells.

abstract：:In the combat against inflammation, glucocorticoids (GCs) are a widespread therapeutic. These ligands of the glucocorticoid receptor (GR) inhibit the transactivation of various transcription factors, including nuclear factor-kappaB (NF-kappaB), and alter the composition of the pro-inflammatory enhanceosome, culminatin...

journal_title：Biochemical pharmacology

authors： Beck IM,Vanden Berghe W,Gerlo S,Bougarne N,Vermeulen L,De Bosscher K,Haegeman G

更新日期：2009-04-01 00:00:00

abstract：:We have investigated the effects of fatty acids on the Na+-H+ exchanger and other carrier-mediated transport systems in intestinal brush-border membrane vesicles. The Na+-H+ exchanger (i.e. H+ gradient-dependent, dimethylamiloride-sensitive Na+ uptake) was strongly inhibited by fatty acids and the inhibition was conce...

journal_title：Biochemical pharmacology

authors： Tiruppathi C,Miyamoto Y,Ganapathy V,Leibach FH

更新日期：1988-04-01 00:00:00

abstract：:When HL-60 cells were stimulated with histamine, a significant differentiation of the cells toward neutrophils was elicited. Histamine increased phagocytic activity, but it reduced myeloperoxidase activity of HL-60 cells. Histamine-induced differentiation in HL-60 cells was inhibited not only by H2 antagonists, such a...

journal_title：Biochemical pharmacology

authors： Nonaka T,Mio M,Doi M,Tasaka K

更新日期：1992-09-25 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：: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

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

更新日期：1996-10-11 00:00:00

abstract：:Recent experiments from our laboratory have indicated that the inhibitory effect of 3'-azido-3'-deoxythymidine (AZT) on oxidative phosphorylation may occur directly, in addition to being brought about by its inhibition of mtDNA replication. We report here studies on the effect of AZT on adenylate kinase, an enzyme cru...

journal_title：Biochemical pharmacology

authors： Barile M,Valenti D,Hobbs GA,Abruzzese MF,Keilbaugh SA,Passarella S,Quagliariello E,Simpson MV

更新日期：1994-10-07 00:00:00

abstract：:Isolated liver from phenobarbital-induced male mice was perfused using infusions of cytochrome c pulses as quality control of the system. Livers spontaneously evolved 1.1 pmoles ethane g-1 liver min-1, exogenous pentane disappeared with 0.6 pmoles g-1 min-1. Infusion of 0.26 mmoles/l. FeCl2 led to immediate ethane pro...

journal_title：Biochemical pharmacology

authors： Thelen M,Wendel A

更新日期：1983-06-01 00:00:00

abstract：:Escape from the proper control of the cell cycle by up-regulation of cyclins or aberrant activation of cyclin-dependent kinases (CDKs) as well as by inactivation of cellular inhibitors of CDKs (CKI) leads to malignant transformation. Loss of cellular CKIs in cancers provided a rationale for development of pharmacologi...

journal_title：Biochemical pharmacology

authors： Wesierska-Gadek J,Hajek SB,Sarg B,Wandl S,Walzi E,Lindner H

更新日期：2008-12-01 00:00:00

abstract：:Nephrotoxicity due to renal proximal tubule accumulation of aminoglycoside (AG) antibiotics, such as gentamicin, represents a major clinical problem. Receptor-mediated endocytosis via the multi-ligand receptor megalin is thought to be a key mechanism in the cellular uptake of AGs and nephrotoxicity. This process can b...

journal_title：Biochemical pharmacology

authors： Antoine DJ,Srivastava A,Pirmohamed M,Park BK

更新日期：2010-02-15 00:00:00

abstract：:The stimulated uptake of 45Ca2+ into incubated cerebrocortical synaptosomes caused by veratrine (75 microM) was blocked by low concentrations of verapamil (0.5-30 microM) which did not prevent or reduce depolarization as judged by efflux of potassium (K+). However, verapamil did not prevent amino acid neutrotransmitte...

journal_title：Biochemical pharmacology

authors： Norris DK,Bradford HF

更新日期：1985-06-01 00:00:00

abstract：:The proinflammatory cytokine interleukin (IL)-18 appears to be involved in the pathogenesis of diseases associated with immunoactivation and inflammation. Consequently, blockage of IL-18 bioactivity by use of IL-18 binding protein (IL-18 BP) is likely a promising therapeutic concept. In the present study, we investiga...

journal_title：Biochemical pharmacology

authors： Nold M,Hauser IA,Höfler S,Goede A,Eberhardt W,Ditting T,Geiger H,Pfeilschifter J,Mühl H

更新日期：2003-08-01 00:00:00

abstract：:The beta-adrenoceptor blocking properties of vaninolol ((+/-)4-[4'-(2-hydroxy-3-tert-butyl-aminopropoxy)-3'-methoxyphenyl]- 3-buten-2-one), derived from vanillin, were first investigated under in vivo and in vitro conditions. Vaninolol (0.1, 0.5, 1.0 mg/kg, i.v.), as well as propranolol, produced a dose-dependent brad...

journal_title：Biochemical pharmacology

authors： Wu BN,Hwang TL,Liao CF,Chen IJ

更新日期：1994-07-05 00:00:00

abstract：:A series of nitrogen mustard derivatives was tested for neurotoxic effects on cholinergic and GABAergic markers at three rat brain regions: hippocampus, striatum and cortex. All compounds were administered intracerebroventricularly, and the enzymatic activities were measured 7 days after treatment. The effects of synt...

journal_title：Biochemical pharmacology

authors： Maysinger D,Tagari PC,Cuello C

更新日期：1986-10-15 00:00:00

abstract：:Aberrant activation of Jak/Stat signaling causes a number of hematopoietic disorders and oncogenesis, and therefore the effective inhibitors of the Jak/Stat signaling pathway may be therapeutically useful. TEL-Jak2 gene fusion, which has been identified in human leukemia, encodes a chimeric protein endowed with consti...

journal_title：Biochemical pharmacology

authors： Funakoshi-Tago M,Tago K,Nishizawa C,Takahashi K,Mashino T,Iwata S,Inoue H,Sonoda Y,Kasahara T

更新日期：2008-12-15 00:00:00

abstract：:The inhibitory effects of quinolone antimicrobial agents and nonsteroidal anti-inflammatory drugs on purified mouse liver mitochondrial medium chain acyl-CoA synthetase catalyzing the first reaction of glycine conjugation were examined, using hexanoic acid as a substrate. Enoxacin, ofloxacin, nalidixic acid, diflunisa...

journal_title：Biochemical pharmacology

authors： Kasuya F,Hiasa M,Kawai Y,Igarashi K,Fukui M

更新日期：2001-08-01 00:00:00

abstract：:The inhibitory effects of anion channel blockers were evaluated on aggregation, intracellular Ca2+ rises, and the production of arachidonic acid metabolites in human platelets. Inhibitors included five anion channel blockers: phloretin, probenecid, pyridoxal phosphate, 4,4'-diisothiocyano-2,2'-disulfonic acid stilbene...

journal_title：Biochemical pharmacology

authors： Ozaki Y,Matsumoto Y,Yatomi Y,Higashihara M,Kariya T,Shoji K

更新日期：1989-07-01 00:00:00

abstract：:The effects of 3-monoalkyl- and 3,5-dialkyl-substitution on the cytotoxicity of paracetamol (PAR) in rat hepatocytes was studied. PAR is known to be bioactivated by the hepatic microsomal cytochrome P-450 containing a mixed-function oxidase system presumably to N-acetyl-para-benzoquinone imine (NAPQI), a reactive meta...

journal_title：Biochemical pharmacology

authors： Van De Straat R,De Vries J,Kulkens T,Debets AJ,Vermeulen NP

更新日期：1986-11-01 00:00:00

abstract：:Neurofibromatosis type 1 (NF1) is the most common cancer predisposition syndrome. NF1 patients present with a constellation of clinical manifestations and have an increased risk of developing certain benign and malignant tumors. This disease results from mutation within the gene encoding neurofibromin, a GTPase activa...

journal_title：Biochemical pharmacology

authors： Dilworth JT,Kraniak JM,Wojtkowiak JW,Gibbs RA,Borch RF,Tainsky MA,Reiners JJ Jr,Mattingly RR

更新日期：2006-11-30 00:00:00

abstract：:Site-specific DNA cleavage in the presence of Cu(II) complexes of podophyllotoxin derivatives was investigated with a modified Sanger sequencing method. Cu(II) complexes of 4'-demethylepipodophyllotoxin (DEPD) and syringic acid (SA) cleaved M13mp18 single-strand DNA site-specifically at both cytosine (C) and guanine (...

journal_title：Biochemical pharmacology

authors： Yamashita A,Tawa R,Imakura Y,Lee KH,Sakurai H

更新日期：1994-05-18 00:00:00

abstract：:Mercaptomethylimidazole (MMI), a potent antithyroid drug of the thionamide group, induces both acid and pepsinogen secretion independently in control and pylorus ligated mice. The effect is dose dependent and the drug is more effective than histamine, carbachol or isoproterenol when administered by an intraperitoneal ...

journal_title：Biochemical pharmacology

authors： Bhattacharjee M,Chakraborty T,Banerjee RK

更新日期：1990-09-01 00:00:00

abstract：:Phospho-tyrosol-indomethacin (PTI; MPI 621), a novel anti-cancer agent, is more potent and safer than conventional indomethacin. Here, we show that PTI was extensively metabolized in vitro and in vivo. PTI was rapidly hydrolyzed by carboxylesterases to generate indomethacin as its major metabolite in the liver microso...

journal_title：Biochemical pharmacology

authors： Xie G,Zhou D,Cheng KW,Wong CC,Rigas B

更新日期：2013-04-15 00:00:00

abstract：:The effects of two recently developed alpha 2-adrenergic antagonists, RX 781094 and WY 26703, on the synthesis of norepinephrine (NE), dopamine (DA) and serotonin (5-HT) in rat brain were compared to those of yohimbine, its diastereoisomer rauwolscine, and mianserin. Intraperitoneal administration of these compounds i...

journal_title：Biochemical pharmacology

authors： Pettibone DJ,Pfleuger AB,Totaro JA

更新日期：1985-04-01 00:00:00

abstract：:The long-term effects of incubating freshly isolated, elicited guinea-pig peritoneal macrophages with the beta-adrenoceptor agonist isoprenaline and the selective inhibitor of phosphodiesterase (PDE) IV rolipram, on adenosine-3',5'-cyclic phosphate (cAMP)-specific PDE IV activity have been investigated. The level of c...

journal_title：Biochemical pharmacology

authors： Kochetkova M,Burns FM,Souness JE

更新日期：1995-12-22 00:00:00

abstract：:Compounds of the mevalonate pathway containing a terminal di- or triphosphate (mev-PP or mev-PPP) were tested as substrates of several enzyme ligases (T4 RNA ligase, T4 DNA ligase, firefly luciferase and other ligases) for the synthesis of ATP derivatives of the mev-pppA or mev-ppppA type. T4 RNA ligase, in the presen...

journal_title：Biochemical pharmacology

authors： Sillero MA,de Diego A,Tavares JE,Silva JA,Pérez-Zúñiga FJ,Sillero A

更新日期：2009-08-15 00:00:00

abstract：:Prodrug activation gene therapy for cancer involves expressing prodrug-activating enzymes in tumour cells, so they can be selectively killed by systemically administered prodrug. For example, Escherichia colinfsB nitroreductase (E.C. 1.6.99.7)(NTR), sensitises cells to the prodrug CB1954 (5-[aziridin-1-yl]-2,4-dinitro...

journal_title：Biochemical pharmacology

authors： Jaberipour M,Vass SO,Guise CP,Grove JI,Knox RJ,Hu L,Hyde EI,Searle PF

更新日期：2010-01-15 00:00:00

abstract：:Local anaesthetics and opioid drugs function synergistically to provide analgesia. In the present study, the nature of this synergy has been investigated using in vitro radioligand binding to determine whether the local anaesthetics bupivacaine and tetracaine modulate the binding of two kappa-opioid receptor ligands, ...

journal_title：Biochemical pharmacology

authors： Fraser GL,Fowler CJ

更新日期：1995-03-30 00:00:00

abstract：:Phenylbutyrate has been shown recently to induce fetal hemoglobin (HbF) production in patients with sickle cell anemia and beta thalassemia. We have now examined related aromatic fatty acids in order to define the range of active structures and identify plausible mechanisms of action. Structure-function analysis revea...

journal_title：Biochemical pharmacology

authors： Hudgins WR,Fibach E,Safaya S,Rieder RF,Miller AC,Samid D

更新日期：1996-10-25 00:00:00

abstract：:The peroxisome proliferator-activated receptors (PPARs) are ligand-dependent transcription factors involved in lipid metabolism and glucose utilization, in cell growth, differentiation and apoptosis, and in the regulation of pro-inflammatory genes expression such as cyclooxygenase-2 (COX-2). PPARγ is the main isoform ...

journal_title：Biochemical pharmacology

authors： Casali CI,Weber K,Faggionato D,Gómez EM,Tome MC

更新日期：2014-08-15 00:00:00

abstract：:In this review, I summarize the sequence of events involved in characterizing the functional role of GABA(B) receptors in the CNS and their involvement in synaptic transmission. The story was launched with the realization that baclofen was a selective agonist of GABA(B) receptors. This lead to the discovery in the CNS...

journal_title：Biochemical pharmacology

authors： Nicoll RA

更新日期：2004-10-15 00:00:00

abstract：:There is increasing evidence that human arylamine N-acetyltransferase type 1 (NAT1, EC 2.3.1.5), although first identified as a homologue of a drug-metabolising enzyme, appears to be a marker in human oestrogen receptor positive breast cancer. Mouse Nat2 is the mouse equivalent of human NAT1. The development of mouse ...

journal_title：Biochemical pharmacology

authors： Kawamura A,Westwood I,Wakefield L,Long H,Zhang N,Walters K,Redfield C,Sim E

更新日期：2008-04-01 00:00:00