abstract：BACKGROUND AND PURPOSE:Baclofen (a GABA(B) receptor agonist) is the most commonly used anti-spasticity agent in clinical practice. While effective when administered spinally or systemically, the development of progressive tolerance represents a serious limitation for its long-term use. The goal of the present study was...

journal_title：British journal of pharmacology

authors： Oshiro M,Hefferan MP,Kakinohana O,Lukacova N,Sugahara K,Yaksh TL,Marsala M

更新日期：2010-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Lithocholic acid (LCA), the most toxic bile acid, induces cholestatic liver injury in rodents. We previously showed that LCA activates the oxidative stress-responsive nuclear factor (erythroid-2 like), factor 2 (Nrf2) in cultured liver cells, triggering adaptive responses that reduce cell injury....

journal_title：British journal of pharmacology

authors： Tan KP,Wood GA,Yang M,Ito S

更新日期：2010-11-01 00:00:00

abstract：:For almost three decades intrathecal baclofen therapy has been the standard treatment for spinal cord injury spasticity when oral medication is ineffective or produces serious side effects. Although intrathecal baclofen therapy has a good clinical benefit-risk ratio for spinal spasticity, tolerance and the life-threat...

journal_title：British journal of pharmacology

authors： Gómez-Soriano J,Goiriena E,Taylor J

更新日期：2010-11-01 00:00:00

abstract：:An increasing number of examples in the literature suggest that the in vivo duration of drug action not only depends on macroscopic pharmacokinetic properties like plasma half-life and the time needed to equilibrate between the plasma and the effect compartments, but is also influenced by long-lasting target binding a...

journal_title：British journal of pharmacology

authors： Vauquelin G,Charlton SJ

更新日期：2010-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:K(v)11.1 channels are involved in regulating cellular excitability in various tissues including brain, heart and smooth muscle. In these tissues, at least two isoforms, K(v)11.1a and K(v)11.1b, with different kinetics, are expressed. K(v)11.1 activators are potential therapeutic agents, but their...

journal_title：British journal of pharmacology

authors： Larsen AP,Bentzen BH,Grunnet M

更新日期：2010-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Quercetin lowers plasma glucose, normalizes glucose tolerance tests and preserves pancreatic β-cell integrity in diabetic rats. However, its mechanism of action has never been explored in insulin-secreting β-cells. Using the INS-1 β-cell line, the effects of quercetin were determined on glucose- ...

journal_title：British journal of pharmacology

authors： Youl E,Bardy G,Magous R,Cros G,Sejalon F,Virsolvy A,Richard S,Quignard JF,Gross R,Petit P,Bataille D,Oiry C

更新日期：2010-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Certain 5-lipoxygenase (5-LO) inhibitors exhibit anti-carcinogenic activities against 5-LO overexpressing tumour types and cultured tumour cells. It has been proposed therefore that 5-LO products significantly contribute to tumour cell proliferation. To date, the relationship between the inhibito...

journal_title：British journal of pharmacology

authors： Fischer AS,Metzner J,Steinbrink SD,Ulrich S,Angioni C,Geisslinger G,Steinhilber D,Maier TJ

更新日期：2010-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Metabolic and cardiovascular abnormalities accompanying metabolic syndrome, such as obesity, insulin resistance and hypertension, are all associated with endothelial dysfunction and are independent risk factors for erectile dysfunction. The purpose of the present study was to investigate the vasc...

journal_title：British journal of pharmacology

authors： Contreras C,Sánchez A,Martínez P,Raposo R,Climent B,García-Sacristán A,Benedito S,Prieto D

更新日期：2010-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Subunit-specific modulators of gamma-aminobutyric acid (GABA) type A (GABA(A)) receptors can help to assess the physiological function of receptors with different subunit composition and also provide the basis for the development of new drugs. Valerenic acid (VA) was recently identified as a beta...

journal_title：British journal of pharmacology

authors： Khom S,Strommer B,Ramharter J,Schwarz T,Schwarzer C,Erker T,Ecker GF,Mulzer J,Hering S

更新日期：2010-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Volume-regulated anion channels (VRACs) play an important role in cell-volume regulation. alpha(1)-Adrenoceptor stimulation by phenylephrine (PE) suppressed the hypotonic activation of VRAC current in mouse ventricular cells and regulatory volume decrease (RVD) was also absent in PE-treated cells...

journal_title：British journal of pharmacology

authors： Ichishima K,Yamamoto S,Iwamoto T,Ehara T

更新日期：2010-09-01 00:00:00

abstract：:British Journal of Pharmacology (BJP) is pleased to publish a new set of guidelines for reporting research involving animals, simultaneously with several other journals; the 'ARRIVE' guidelines (Animals in Research: Reporting In Vivo Experiments). This editorial summarizes the background to the guidelines, gives our v...

journal_title：British journal of pharmacology

authors： McGrath JC,Drummond GB,McLachlan EM,Kilkenny C,Wainwright CL

更新日期：2010-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Dexmedetomidine, an alpha(2)-adrenoceptor agonist, exhibits anti-nociceptive actions at the spinal cord and enhances the effect of local anaesthetics in the peripheral nervous system. Although the latter action may be attributed in part to inhibition of nerve conduction produced by dexmedetomidin...

journal_title：British journal of pharmacology

authors： Kosugi T,Mizuta K,Fujita T,Nakashima M,Kumamoto E

更新日期：2010-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The aim of this study was to determine whether the apelin/APJ system is altered in human cardiovascular disease by investigating whether the expression of apelin or its receptor is altered at the protein level. EXPERIMENTAL APPROACH:Radioligand binding studies were used to determine apelin recep...

journal_title：British journal of pharmacology

authors： Pitkin SL,Maguire JJ,Kuc RE,Davenport AP

更新日期：2010-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Carboxylesterases (CEs) metabolize a wide range of xenobiotic substrates including heroin, cocaine, meperidine and the anticancer agent CPT-11. In this study, we have purified to homogeneity human liver and intestinal CEs and compared their ability with hydrolyse heroin, cocaine and CPT-11. EXPE...

journal_title：British journal of pharmacology

authors： Hatfield MJ,Tsurkan L,Hyatt JL,Yu X,Edwards CC,Hicks LD,Wadkins RM,Potter PM

更新日期：2010-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Excessive production of nitric oxide (NO) by inducible NO synthase (iNOS) is thought to underlie the vascular dysfunction, systemic hypotension and organ failure that characterize endotoxic shock. Plasma levels of atrial natriuretic peptide (ANP), brain natriuretic peptide (BNP) and C-type natriu...

journal_title：British journal of pharmacology

authors： Panayiotou CM,Baliga R,Stidwill R,Taylor V,Singer M,Hobbs AJ

更新日期：2010-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:A functional link between seizure-induced P-glycoprotein overexpression at the blood-brain barrier and therapeutic failure has been suggested by several studies using rodent epilepsy models and human epileptic tissue. Recently, we reported that interference with the mechanisms that up-regulate P-...

journal_title：British journal of pharmacology

authors： Schlichtiger J,Pekcec A,Bartmann H,Winter P,Fuest C,Soerensen J,Potschka H

更新日期：2010-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Tetracyclines were recently found to induce tumour cell death, but the early processes involved in this cytotoxic effect remain unclear. EXPERIMENTAL APPROACH:Viability of human and mouse melanoma cells was determined by MTT assay and flow cytometry. Kinase/protein/caspase activation was measure...

journal_title：British journal of pharmacology

authors： Shieh JM,Huang TF,Hung CF,Chou KH,Tsai YJ,Wu WB

更新日期：2010-07-01 00:00:00

abstract：:In this issue MacMillan and McCarron in 2010 demonstrated that the phospholipase C (PLC) inhibitor U-73122 can potently inhibit Ca(2+) release from isolated smooth muscle cells independent of its effect on PLC. Their data suggest that the PLC inhibitor can block the sarcoplasmic/endoplasmic reticulum calcium ATPase pu...

journal_title：British journal of pharmacology

authors： Hollywood MA,Sergeant GP,Thornbury KD,McHale NG

更新日期：2010-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Montelukast and S-carbocysteine have been used in asthmatic patients as an anti-inflammatory or mucolytic agent respectively. S-carbocysteine also exhibits anti-inflammatory properties. EXPERIMENTAL APPROACH:Ovalbumin (OVA) sensitized BALB/c mice were challenged with OVA for 3 days followed by s...

journal_title：British journal of pharmacology

authors： Takeda K,Shiraishi Y,Matsubara S,Miyahara N,Matsuda H,Okamoto M,Joetham A,Gelfand EW

更新日期：2010-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Although trace amines (TAs) are historically considered 'false neurotransmitters' on the basis of their ability to induce catecholamine release, there is evidence that they directly affect neuronal activity via TA receptors, ligand-gated receptor channels and/or sigma receptors. Here, we have inv...

journal_title：British journal of pharmacology

authors： Ledonne A,Federici M,Giustizieri M,Pessia M,Imbrici P,Millan MJ,Bernardi G,Mercuri NB

更新日期：2010-07-01 00:00:00

abstract：:The endogenous cannabinoid system is involved in numerous physiological and neuropsychological functions. Medications that target this system hold promise for the treatment of a wide variety of disorders. However, as reward is one of the most prominent of these functions, medications that activate this system must be ...

journal_title：British journal of pharmacology

authors： Panlilio LV,Justinova Z,Goldberg SR

更新日期：2010-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Recent studies suggest that the effects of cyclooxygenase-2 (COX-2) inhibition are mediated by cannabinoid receptor activation. However, some non-steroidal anti-inflammatory drugs inhibit the enzyme fatty acid amide hydrolase, which regulates levels of some endocannabinoids. Whether COX-2 directl...

journal_title：British journal of pharmacology

authors： Staniaszek LE,Norris LM,Kendall DA,Barrett DA,Chapman V

更新日期：2010-06-01 00:00:00

abstract：:Psoriasis is a chronic inflammatory disease affecting 1-3% of the general population. Among psoriatic patients, 5-40% are affected by psoriatic arthritis. Due to the chronic nature of the disease, patients suffer from substantial psychological and financial burdens, thus adding to a significantly impaired quality of l...

journal_title：British journal of pharmacology

authors： Weger W

更新日期：2010-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Hydrogen sulphide (H(2)S) is a labile, endogenous metabolite of cysteine, with multiple biological roles. The development of sulphide-based therapies for human diseases will benefit from a reliable method of quantifying H(2)S in blood and tissues. EXPERIMENTAL APPROACH:Concentrations of reactive...

journal_title：British journal of pharmacology

authors： Wintner EA,Deckwerth TL,Langston W,Bengtsson A,Leviten D,Hill P,Insko MA,Dumpit R,VandenEkart E,Toombs CF,Szabo C

更新日期：2010-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Some neurosteroids, notably 3alpha-hydroxysteroids, positively modulate GABA(A) receptors, but sulphated steroids negatively modulate these receptors. Recently, other lipophilic amphiphiles have been suggested to positively modulate GABA receptors. We examined whether there was similarity among t...

journal_title：British journal of pharmacology

authors： Chisari M,Shu HJ,Taylor A,Steinbach JH,Zorumski CF,Mennerick S

更新日期：2010-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:There is increasing evidence that not only the monoaminergic but also the glutamatergic system is involved in the pathophysiology of attention-deficit hyperactivity disorder (ADHD). Hyperactivity of glutamate metabolism might be causally related to a hypoactive state in the dopaminergic system. A...

journal_title：British journal of pharmacology

authors： Ludolph AG,Udvardi PT,Schaz U,Henes C,Adolph O,Weigt HU,Fegert JM,Boeckers TM,Föhr KJ

更新日期：2010-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Due to their potent bronchodilator properties, beta(2)-adrenoceptor agonists are a mainstay of therapy in asthma. However, the effects of beta(2)-adrenoceptor agonists on inflammation are less clear. Accordingly, we have investigated the effects of beta(2)-adrenoceptor agonists on inflammatory me...

journal_title：British journal of pharmacology

authors： Holden NS,Rider CF,Bell MJ,Velayudhan J,King EM,Kaur M,Salmon M,Giembycz MA,Newton R

更新日期：2010-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:beta-Amyloid peptide (Abeta) is implicated in the pathogenesis of Alzheimer's disease by initiating a cascade of events from mitochondrial dysfunction to neuronal death. The metabolic enhancer piracetam has been shown to improve mitochondrial dysfunction following brain aging and experimentally i...

journal_title：British journal of pharmacology

authors： Kurz C,Ungerer I,Lipka U,Kirr S,Schütt T,Eckert A,Leuner K,Müller WE

更新日期：2010-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Recent findings suggest that the noxious gas H(2)S is produced endogenously, and that physiological concentrations of H(2)S are able to modulate pain and inflammation in rodents. This study was undertaken to evaluate the ability of endogenous and exogenous H(2)S to modulate carrageenan-induced sy...

journal_title：British journal of pharmacology

authors： Ekundi-Valentim E,Santos KT,Camargo EA,Denadai-Souza A,Teixeira SA,Zanoni CI,Grant AD,Wallace J,Muscará MN,Costa SK

更新日期：2010-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Gallium (Ga) has been shown to be effective in the treatment of disorders associated with accelerated bone loss, including cancer-related hypercalcemia and Paget's disease. These clinical applications suggest that Ga could reduce bone resorption. However, few studies have studied the effects of G...

journal_title：British journal of pharmacology

authors： Verron E,Masson M,Khoshniat S,Duplomb L,Wittrant Y,Baud'huin M,Badran Z,Bujoli B,Janvier P,Scimeca JC,Bouler JM,Guicheux J

更新日期：2010-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:5-Hydroxytryptamine (5-HT) has been shown to control and modulate many physiological and behavioural functions in insects. In this study, we report the cloning and pharmacological properties of a 5-HT(1) receptor of an insect model for neurobiology, physiology and pharmacology. EXPERIMENTAL APPR...

journal_title：British journal of pharmacology

authors： Troppmann B,Balfanz S,Baumann A,Blenau W

更新日期：2010-04-01 00:00:00

abstract：:S-nitrosothiols have a number of potential clinical applications, among which their use as antithrombotic agents has been emphasized. This is largely because of their well-documented platelet inhibitory effects, which show a degree of platelet selectivity, although the mechanism of this remains undefined. Recent progr...

journal_title：British journal of pharmacology

authors： Gordge MP,Xiao F

更新日期：2010-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Inflammatory response and cytokine activation are markedly stimulated after myocardial infarction, and contribute to cardiac remodelling. Interleukin-6 (IL-6), a pro-inflammatory cytokine, has pleiotropic effects on cardiac remodelling. Adenosine, released by all cell types, binds to a class of G...

journal_title：British journal of pharmacology

authors： Feng W,Song Y,Chen C,Lu ZZ,Zhang Y

更新日期：2010-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Much interest is currently being focused on the anti-nociceptive effects mediated by nicotinic acetylcholine (nACh) receptors, including their location and mechanism of action. The purpose of this study was to elucidate these issues using 5-iodo-3-(2(S)-azetidinylmethoxy)pyridine (5IA), a nACh re...

journal_title：British journal of pharmacology

authors： Ueda M,Iida Y,Tominaga A,Yoneyama T,Ogawa M,Magata Y,Nishimura H,Kuge Y,Saji H

更新日期：2010-03-01 00:00:00

abstract：:G protein-coupled receptors are the largest group of membrane proteins and are the targets for approximately 30% of drugs currently used therapeutically. These 7-transmembrane-spanning proteins continue to provide new opportunities to develop therapeutics based on emerging knowledge of their structure, signalling prop...

journal_title：British journal of pharmacology

authors： Summers RJ

更新日期：2010-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Excitation-transcriptional coupling involves communication between plasma membrane ion channels and gene expression in the nucleus. Calcium influx through L-type Ca(2+) channels induces phosphorylation of the transcription factor, cyclic-AMP response element binding protein (CREB) and downstream ...

journal_title：British journal of pharmacology

authors： Kang M,Ross GR,Akbarali HI

更新日期：2010-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:In humans and non-human primates, the 7TM receptor GPR17 exists in two isoforms differing only by the length of the N-terminus. Of these, only the short isoform has previously been characterized. Hence, we investigated gene expression and ligand-binding profiles of both splice variants and furthe...

journal_title：British journal of pharmacology

authors： Benned-Jensen T,Rosenkilde MM

更新日期：2010-03-01 00:00:00

abstract：:After many years of effort, recent technical breakthroughs have enabled the X-ray crystal structures of three G-protein-coupled receptors (GPCRs) (beta1 and beta2 adrenergic and adenosine A(2a)) to be solved in addition to rhodopsin. GPCRs, like other membrane proteins, have lagged behind soluble drug targets such as ...

journal_title：British journal of pharmacology

authors： Congreve M,Marshall F

更新日期：2010-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:It is well known that adenine-based purines exert multiple effects on pain transmission. However, less attention has been given to the potential effects of guanine-based purines on pain transmission. The aim of this study was to investigate the effects of intraperitoneal (i.p.) and oral (p.o.) ad...

journal_title：British journal of pharmacology

authors： Schmidt AP,Böhmer AE,Schallenberger C,Antunes C,Tavares RG,Wofchuk ST,Elisabetsky E,Souza DO

更新日期：2010-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The aim of the current study was to investigate the role of arachidonic acid (AA) metabolism via cyclooxygenase (COX) in the endothelial dysfunction of penile arteries from pre-diabetic, obese Zucker rats (OZR). EXPERIMENTAL APPROACH:Penile arteries from OZR and from lean Zucker rats (LZR) were ...

journal_title：British journal of pharmacology

authors： Sánchez A,Contreras C,Villalba N,Martínez P,Martínez AC,Bríones A,Salaíces M,García-Sacristán A,Hernández M,Prieto D

更新日期：2010-02-01 00:00:00