abstract：:BACKGROUND AND PURPOSE The transepithelial absorption of Na(+) in the lungs is crucial for the maintenance of the volume and composition of epithelial lining fluid. The regulation of Na(+) transport is essential, because hypo- or hyperabsorption of Na(+) is associated with lung diseases such as pulmonary oedema or cys...

journal_title：British journal of pharmacology

authors： Althaus M,Urness KD,Clauss WG,Baines DL,Fronius M

更新日期：2012-07-01 00:00:00

abstract：:In this issue of the BJP, Green et al. suggest that animal data could not be used to predict the adverse effects of 3,4-methylenedioxymethamphetamine (MDMA) in humans and that MDMA did not produce 5-HT neurotoxicity in the human brain. This proposal was, however, not accompanied by a review of the empirical evidence i...

journal_title：British journal of pharmacology

authors： Parrott AC

更新日期：2012-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The chemokine receptor CXCR3 directs migration of T-cells in response to the ligands CXCL9/Mig, CXCL10/IP-10 and CXCL11/I-TAC. Both ligands and receptors are implicated in the pathogenesis of inflammatory disorders, including atherosclerosis and rheumatoid arthritis. Here, we describe the molecul...

journal_title：British journal of pharmacology

authors： Nedjai B,Li H,Stroke IL,Wise EL,Webb ML,Merritt JR,Henderson I,Klon AE,Cole AG,Horuk R,Vaidehi N,Pease JE

更新日期：2012-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The aggregation of α-synuclein is connected to the pathology of Parkinson's disease and prolyl oligopeptidase (PREP) accelerates the aggregation of α-synuclein in vitro. The aim of this study was to investigate the effects of a PREP inhibitor, KYP-2047, on α-synuclein aggregation in cell lines ov...

journal_title：British journal of pharmacology

authors： Myöhänen TT,Hannula MJ,Van Elzen R,Gerard M,Van Der Veken P,García-Horsman JA,Baekelandt V,Männistö PT,Lambeir AM

更新日期：2012-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Glucocorticoids appear to control Na⁺ absorption in pulmonary epithelial cells via a mechanism dependent upon serum and glucocorticoid-inducible kinase 1 (SGK1), a kinase that allows control over the surface abundance of epithelial Na⁺ channel subunits (α-, β- and γ-ENaC). However, not all data s...

journal_title：British journal of pharmacology

authors： Watt GB,Ismail NA,Caballero AG,Land SC,Wilson SM

更新日期：2012-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Tumour cell-induced platelet aggregation (TCIPA) facilitates cancer cell invasion, angiogenesis and the formation of metastatic foci. TCIPA can be modulated by pharmacological inhibitors of MMP-2 and ADP; however, the COX inhibitor aspirin did not prevent TCIPA. In this study, we have tested the ...

journal_title：British journal of pharmacology

authors： Medina C,Harmon S,Inkielewicz I,Santos-Martinez MJ,Jones M,Cantwell P,Bazou D,Ledwidge M,Radomski MW,Gilmer JF

更新日期：2012-06-01 00:00:00

abstract：BACKGROUNDS AND PURPOSE:Lactic acidosis is a fatal adverse effect of metformin, but the risk factor remains unclear. Multidrug and toxin extrusion 1 (MATE1) is expressed in the luminal membrane of the kidney and liver. MATE1 was revealed to be responsible for the tubular and biliary secretion of metformin. Therefore, s...

journal_title：British journal of pharmacology

authors： Toyama K,Yonezawa A,Masuda S,Osawa R,Hosokawa M,Fujimoto S,Inagaki N,Inui K,Katsura T

更新日期：2012-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The locus coeruleus (LC) is a major source of noradrenergic projections to the dorsal spinal cord, and thereby plays an important role in the modulation of nociceptive information. The LC receives inputs from substance P (SP)-containing fibres from other regions, and expresses the NK(1) tachykin...

journal_title：British journal of pharmacology

authors： Muto Y,Sakai A,Sakamoto A,Suzuki H

更新日期：2012-06-01 00:00:00

abstract：:BACKGROUND AND PURPOSE Selective hyperpolarization activated, cyclic nucleotide-gated channel (HCN) blockers represent an important therapeutic goal due to the wide distribution and multiple functions of these proteins, representing the molecular correlate of f- and h-current (I(f) or I(h) ). Recently, new compounds ...

journal_title：British journal of pharmacology

authors： Del Lungo M,Melchiorre M,Guandalini L,Sartiani L,Mugelli A,Koncz I,Szel T,Varro A,Romanelli MN,Cerbai E

更新日期：2012-05-01 00:00:00

abstract：:Since its discovery over 50 years ago, cAMP has been the archetypal second messenger introducing students to the concept of cell signalling at the simplest level. As explored in this review, however, there are many more facets to cAMP signalling than the path from Gs-coupled receptor to adenylyl cyclase (AC) to cAMP t...

journal_title：British journal of pharmacology

authors： Billington CK,Hall IP

更新日期：2012-05-01 00:00:00

abstract：:The Secretin family of GPCRs are endocrine peptide hormone receptors that share a common genomic organization and are the subject of a wide variety of alternative splicing. All GPCRs contain a central seven transmembrane domain responsible for transducing signals from the outside of the cell as well as extracellular a...

journal_title：British journal of pharmacology

authors： Furness SG,Wootten D,Christopoulos A,Sexton PM

更新日期：2012-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Methylene blue (MB) is commonly employed as a treatment for methaemoglobinaemia, malaria and vasoplegic shock. An increasing number of studies indicate that MB can cause 5-HT toxicity when administered with a 5-HT reuptake inhibitor. MB is a potent inhibitor of monoamine oxidases, but other targe...

journal_title：British journal of pharmacology

authors： Oz M,Isaev D,Lorke DE,Hasan M,Petroianu G,Shippenberg TS

更新日期：2012-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:QT prolongation is commonly used as a surrogate marker for Torsade de Pointes (TdP) risk of non-cardiovascular drugs. However, use of this indirect marker often leads to misinterpretation of the realistic TdP risk, as tested compounds may cause QT prolongation without evoking TdP in humans. A neg...

journal_title：British journal of pharmacology

authors： Guns PJ,Johnson DM,Van Op den Bosch J,Weltens E,Lissens J

更新日期：2012-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Hydrogen sulphide (H(2) S) is gaining acceptance as a gaseous signal molecule. However, mechanisms regarding signal termination are not understood. We used stigmatellin and antimycin A, inhibitors of sulphide quinone reductase (SQR), to test the hypothesis that the catabolism of H(2) S involves S...

journal_title：British journal of pharmacology

authors： Linden DR,Furne J,Stoltz GJ,Abdel-Rehim MS,Levitt MD,Szurszewski JH

更新日期：2012-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:mTOR inhibitors are currently used as immunosuppressants in transplanted patients and as promising anti-cancer agents. However, new-onset diabetes is a frequent complication occurring in patients treated with mTOR inhibitors such as rapamycin (Sirolimus). Here, we investigated the mechanisms asso...

journal_title：British journal of pharmacology

authors： Deblon N,Bourgoin L,Veyrat-Durebex C,Peyrou M,Vinciguerra M,Caillon A,Maeder C,Fournier M,Montet X,Rohner-Jeanrenaud F,Foti M

更新日期：2012-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Activation of cannabinoid receptors decreases emesis, inflammation, gastric acid secretion and intestinal motility. The ability to modulate intestinal permeability in inflammation may be important in therapy aimed at maintaining epithelial barrier integrity. The aim of the present study was to de...

journal_title：British journal of pharmacology

authors： Alhamoruni A,Wright KL,Larvin M,O'Sullivan SE

更新日期：2012-04-01 00:00:00

abstract：:Ischaemia is amongst the leading causes of death. Despite this importance, there are only a few therapeutic approaches to protect from ischaemia-reperfusion injury (IRI). In experimental studies, the amino acid glycine effectively protected from IRI. In the prevention of IRI by glycine in cells and isolated perfused o...

journal_title：British journal of pharmacology

authors： Petrat F,Boengler K,Schulz R,de Groot H

更新日期：2012-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:5-HT receptor agonists have variable nociceptive effects within the spinal cord. While there is some evidence for 5-HT(1A) spinally-mediated analgesia, the role of other 5-HT(1) receptor subtypes remains unclear. In the present study, we examined the spinal actions of a range of 5-HT(1) agonists,...

journal_title：British journal of pharmacology

authors： Jeong HJ,Mitchell VA,Vaughan CW

更新日期：2012-03-01 00:00:00

abstract：:Cyclic nucleotide phosphodiesterases (PDEs) that specifically inactivate the intracellular messengers cAMP and cGMP in a compartmentalized manner represent an important enzyme class constituted by 11 gene-related families of isozymes (PDE1 to PDE11). Downstream receptors, PDEs play a major role in controlling the sign...

journal_title：British journal of pharmacology

authors： Keravis T,Lugnier C

更新日期：2012-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Emesis is a multi-system reflex, which is usually investigated using in vivo models. The aim of the study is to compare the response induced by emetic compounds across species and investigate whether dogs, ferrets and rats are all similarly predictive of humans. EXPERIMENTAL APPROACH:A systemati...

journal_title：British journal of pharmacology

authors： du Sert NP,Holmes AM,Wallis R,Andrews PL

更新日期：2012-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Inhaled corticosteroids (ICS) are the cornerstone of asthma pharmacotherapy and, acting via the glucocorticoid receptor (GR), reduce inflammatory gene expression. While this is often attributed to a direct inhibitory effect of the GR on inflammatory gene transcription, corticosteroids also induce...

journal_title：British journal of pharmacology

authors： Kelly MM,King EM,Rider CF,Gwozd C,Holden NS,Eddleston J,Zuraw B,Leigh R,O'Byrne PM,Newton R

更新日期：2012-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:β-Adrenoceptor stimulation induces glucose uptake in several insulin-sensitive tissues by poorly understood mechanisms. EXPERIMENTAL APPROACH:We used a model system in CHO-K1 cells expressing the human β(2)-adrenoceptor and glucose transporter 4 (GLUT4) to investigate the signalling mechanisms i...

journal_title：British journal of pharmacology

authors： Dehvari N,Hutchinson DS,Nevzorova J,Dallner OS,Sato M,Kocan M,Merlin J,Evans BA,Summers RJ,Bengtsson T

更新日期：2012-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Azithromycin has been reported to modify activation of macrophages towards the M2 phenotype. Here, we have sought to identify the mechanisms underlying this modulatory effect of azithromycin on human monocytes, classically activated in vitro. EXPERIMENTAL APPROACH:Human blood monocytes were prim...

journal_title：British journal of pharmacology

authors： Vrančić M,Banjanac M,Nujić K,Bosnar M,Murati T,Munić V,Stupin Polančec D,Belamarić D,Parnham MJ,Eraković Haber V

更新日期：2012-03-01 00:00:00

abstract：:Gut inflammation occurring in patients with inflammatory bowel diseases (IBD) is associated with an excessive immune response that is directed against constituents of the normal bacterial flora and results in the production of large amounts of inflammatory cytokines. Anti-cytokine compounds, such as the neutralizing T...

journal_title：British journal of pharmacology

authors： Caprioli F,Caruso R,Sarra M,Pallone F,Monteleone G

更新日期：2012-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Insulin resistance is often found to be associated with high blood pressure. We propose that in insulin-resistant hypertension, endothelial dysfunction is the consequence of increased activity of vascular MMP-2. As MMP-2 proteolytically cleaves a number of extracellular matrix proteins, we hypoth...

journal_title：British journal of pharmacology

authors： Nagareddy PR,Rajput PS,Vasudevan H,McClure B,Kumar U,Macleod KM,McNeill JH

更新日期：2012-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Stress is believed to be associated with the development of neuropsychiatric disorders, including Alzheimer's disease (AD). We have studied mechanisms implicated in vulnerability to stress and the relationship with changes in AD-related markers. EXPERIMENTAL APPROACH:Anhedonia induced by a chron...

journal_title：British journal of pharmacology

authors： Briones A,Gagno S,Martisova E,Dobarro M,Aisa B,Solas M,Tordera R,Ramírez M

更新日期：2012-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Partial agonists selective for α4β2 nicotinic ACh receptors have been developed for smoking cessation as they induce weak activation of native α4β2* receptors and inhibit effect of nicotine. However, it is unclear whether at brain functions there is an existence of receptor reserve that allows we...

journal_title：British journal of pharmacology

authors： Chen Y,Broad LM,Phillips KG,Zwart R

更新日期：2012-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:3,4-Methylenedioxymethamphetamine (MDMA or 'Ecstasy') is a worldwide major drug of abuse known to elicit neurotoxic effects. The mechanisms underlying the neurotoxic effects of MDMA are not clear at present, but the metabolism of dopamine and 5-HT by monoamine oxidase (MAO), as well as the hepati...

journal_title：British journal of pharmacology

authors： Barbosa DJ,Capela JP,Oliveira JM,Silva R,Ferreira LM,Siopa F,Branco PS,Fernandes E,Duarte JA,de Lourdes Bastos M,Carvalho F

更新日期：2012-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The glucagon-like peptides GLP-1 and GLP-2 are secreted from enteroendocrine L-cells following nutrient ingestion. Drugs that increase activity of the GLP-1 axis are highly successful therapies for type 2 diabetes, and boosting L-cell secretion is a potential strategy for future diabetes treatmen...

journal_title：British journal of pharmacology

authors： Parker HE,Wallis K,le Roux CW,Wong KY,Reimann F,Gribble FM

更新日期：2012-01-01 00:00:00

abstract：:Along with many other mammalian ATP-binding cassette (ABC) transporters, members of the ABCG group are involved in the regulated transport of hydrophobic compounds across cellular membranes. In humans, five ABCG family members have been identified, encoding proteins ranging from 638 to 678 amino acids in length. All f...

journal_title：British journal of pharmacology

authors： Kerr ID,Haider AJ,Gelissen IC

更新日期：2011-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Inhibitors of phosphodiesterase 5 (PDE5) affect signalling pathways by elevating cGMP, which is a second messenger involved in processes of neuroplasticity. In the present study, the effects of the PDE5 inhibitor, sildenafil, on the pathological features of Alzheimer's disease and on memory-relat...

journal_title：British journal of pharmacology

authors： Cuadrado-Tejedor M,Hervias I,Ricobaraza A,Puerta E,Pérez-Roldán JM,García-Barroso C,Franco R,Aguirre N,García-Osta A

更新日期：2011-12-01 00:00:00

abstract：:Ever since the discovery of prostaglandin E(2)(PGE(2)), this lipid mediator has been the focus of intense research. The diverse biological effects of PGE(2) are due, at least in part, to the existence of four distinct receptors (EP(1-4)). This can complicate the analysis of the biological effects produced by PGE2. Whi...

journal_title：British journal of pharmacology

authors： Birrell MA,Nials AT

更新日期：2011-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Rosiglitazone is an anti-diabetic drug improving insulin sensitivity and glucose uptake in skeletal muscle and adipose tissues. However, several recent clinical trials suggest that rosiglitazone can increase the risk of cardiovascular ischaemia, although other studies failed to show such risks. T...

journal_title：British journal of pharmacology

authors： Yu L,Jin X,Yang Y,Cui N,Jiang C

更新日期：2011-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Depolarization-induced suppression of inhibition (DSI) and excitation (DSE) are two forms of cannabinoid CB(1) receptor-mediated inhibition of synaptic transmission, whose durations are regulated by endocannabinoid (eCB) degradation. We have recently shown that in cultured hippocampal neurons mon...

journal_title：British journal of pharmacology

authors： Straiker A,Wager-Miller J,Hu SS,Blankman JL,Cravatt BF,Mackie K

更新日期：2011-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Adenosine is considered to be an important modulator of intestinal motility. This study was undertaken to investigate the role of adenosine in the modulation of contractility in the mouse duodenum and to characterize the adenosine receptor subtypes involved. EXPERIMENTAL APPROACH:RT-PCR was used...

journal_title：British journal of pharmacology

authors： Zizzo MG,Mastropaolo M,Lentini L,Mulè F,Serio R

更新日期：2011-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Hyperbilirubinaemia and cholestasis are two major forms of liver abnormality. The Chinese herb Yin Chin has been used for thousands of years to treat liver dysfunctions. In mice, this herb and its principal ingredient scoparone were found to accelerate the clearance of bilirubin accompanied by th...

journal_title：British journal of pharmacology

authors： Yang D,Yang J,Shi D,Deng R,Yan B

更新日期：2011-11-01 00:00:00

abstract：:Obsessive-compulsive disorder (OCD) is characterized by obsessions (intrusive thoughts) and compulsions (repetitive ritualistic behaviours) leading to functional impairment. Accumulating evidence links these conditions with underlying dysregulation of fronto-striatal circuitry and monoamine systems. These abnormalitie...

journal_title：British journal of pharmacology

authors： Fineberg NA,Chamberlain SR,Hollander E,Boulougouris V,Robbins TW

更新日期：2011-10-01 00:00:00

abstract：BACKGROUND:Dimebolin (latrepirdine), a compound with multiple potential drug targets, is being evaluated in clinical trials for the treatment of Alzheimer's disease (AD) and preliminary results suggest it can slow the disease process. There is also evidence that dimebolin directly improves aspects of cognition. Here we...

journal_title：British journal of pharmacology

authors： Webster SJ,Wilson CA,Lee CH,Mohler EG,Terry AV Jr,Buccafusco JJ

更新日期：2011-10-01 00:00:00

abstract：:Rodent models of chronic pain may elucidate pathophysiological mechanisms and identify potential drug targets, but whether they predict clinical efficacy of novel compounds is controversial. Several potential analgesics have failed in clinical trials, in spite of strong animal modelling support for efficacy, but there...

journal_title：British journal of pharmacology

authors： Berge OG

更新日期：2011-10-01 00:00:00

abstract：:Two structurally distinct peptides, angiotensin IV and LVV-haemorphin 7, both competitive high-affinity inhibitors of insulin-regulated aminopeptidase (IRAP), were found to enhance aversion-associated and spatial memory in normal rats and to improve performance in a number of memory tasks in rat deficits models. These...

journal_title：British journal of pharmacology

authors： Albiston AL,Diwakarla S,Fernando RN,Mountford SJ,Yeatman HR,Morgan B,Pham V,Holien JK,Parker MW,Thompson PE,Chai SY

更新日期：2011-09-01 00:00:00