abstract：BACKGROUND AND PURPOSE:Tolerance induced by morphine and other opiates remains a major unresolved problem in the clinical management of pain. There is now good evidence for the importance of MAPKs in morphine-induced antinociceptive tolerance. A member of the MAPK kinase kinase family, TGF-β activated kinase 1 (TAK1) i...

journal_title：British journal of pharmacology

authors： Xu H,Xu T,Ma X,Jiang W

更新日期：2015-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Lysophosphatidylinositol (LPI), a lipid signalling molecule, activates GPR55 and elevates intracellular Ca(2+). Here, we examine the actions of LPI in the rat resistance mesenteric artery and Ca(2+) responses in endothelial cells isolated from the artery. EXPERIMENTAL APPROACH:Vascular responses...

journal_title：British journal of pharmacology

authors： AlSuleimani YM,Hiley CR

更新日期：2015-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Two of the most relevant unmet needs in epilepsy are represented by the development of disease-modifying drugs able to affect epileptogenesis and/or the study of related neuropsychiatric comorbidities. No systematic study has investigated the effects of chronic treatment with antipsychotics or an...

journal_title：British journal of pharmacology

authors： Citraro R,Leo A,De Fazio P,De Sarro G,Russo E

更新日期：2015-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Toll-like receptor 4 (TLR4) signalling contributes to inflammatory cardiovascular diseases, but its role in hypertension and the associated vascular damage is not known. We investigated whether TLR4 activation contributed to angiotensin II (AngII)-induced hypertension and the associated vascular ...

journal_title：British journal of pharmacology

authors： Hernanz R,Martínez-Revelles S,Palacios R,Martín A,Cachofeiro V,Aguado A,García-Redondo L,Barrús MT,de Batista PR,Briones AM,Salaices M,Alonso MJ

更新日期：2015-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:GoSlo-SR compounds are efficacious BK (KCa 1.1) channel openers, but little is known about their mechanism of action or effect on bladder contractility. We examined the effects of two closely related compounds on BK currents and bladder contractions. EXPERIMENTAL APPROACH:A combination of electr...

journal_title：British journal of pharmacology

authors： Large RJ,Kshatri A,Webb TI,Roy S,Akande A,Bradley E,Sergeant GP,Thornbury KD,McHale NG,Hollywood MA

更新日期：2015-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Inhaled glucocorticoid (ICS)/long-acting β2 -adrenoceptor agonist (LABA) combination therapy is a recommended treatment option for patients with moderate/severe asthma in whom adequate control cannot be achieved by an ICS alone. Previously, we discovered that LABAs can augment dexamethasone-induc...

journal_title：British journal of pharmacology

authors： Joshi T,Johnson M,Newton R,Giembycz MA

更新日期：2015-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Pulmonary hypertension (PH) is a devastating disease characterized by increased pulmonary arterial pressure, which progressively leads to right-heart failure and death. A dys-regulated renin angiotensin system (RAS) has been implicated in the development and progression of PH. However, the role o...

journal_title：British journal of pharmacology

authors： Bruce E,Shenoy V,Rathinasabapathy A,Espejo A,Horowitz A,Oswalt A,Francis J,Nair A,Unger T,Raizada MK,Steckelings UM,Sumners C,Katovich MJ

更新日期：2015-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Recently, we demonstrated that the nucleus accumbens (NAC) is required for the acquisition and expression of relief memory. The purpose of this study was to investigate the role of NMDA receptors within the NAC in relief learning. EXPERIMENTAL APPROACH:The NMDA receptor antagonist 2-amino-5-phos...

journal_title：British journal of pharmacology

authors： Mohammadi M,Fendt M

更新日期：2015-05-01 00:00:00

abstract：:This article discusses the background to the need for change in the reporting of experiments involving animals, including a report of a consensus meeting organised by the Basel Declaration Society and Understanding Animal Research UK that sought to Internationalise guidelines for reporting experiments involving animal...

journal_title：British journal of pharmacology

authors： McGrath JC,McLachlan EM,Zeller R

更新日期：2015-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Hypoxia/reoxygenation induces synthesis of reactive oxygen species (ROS) which can attack macromolecules and cause brain injury. The transcription factor, nuclear factor (erythroid-derived 2)-like 2, (Nrf2), ia potent activator of genes with an antioxidant responsive element and Nrf2 can countera...

journal_title：British journal of pharmacology

authors： Cao S,Chao D,Zhou H,Balboni G,Xia Y

更新日期：2015-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Sphingosine-1-phosphate (S1P) has been shown to be involved in the asthmatic disease as well in preclinical mouse experimental models of this disease. The aim of this study was to understand the mechanism(s) underlying S1P effects on the lung. EXPERIMENTAL APPROACH:BALB/c, mast cell-deficient an...

journal_title：British journal of pharmacology

authors： Roviezzo F,Sorrentino R,Bertolino A,De Gruttola L,Terlizzi M,Pinto A,Napolitano M,Castello G,D'Agostino B,Ianaro A,Sorrentino R,Cirino G

更新日期：2015-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The non-nucleoside analogue reverse transcriptase inhibitor efavirenz is associated with hepatic toxicity and metabolic disturbances. Although the mechanisms involved are not clear, recent evidence has pinpointed a specific mitochondrial action of efavirenz accompanied by the induction of an endo...

journal_title：British journal of pharmacology

authors： Polo M,Alegre F,Funes HA,Blas-Garcia A,Victor VM,Esplugues JV,Apostolova N

更新日期：2015-04-01 00:00:00

abstract：:Annexin A2 (AnxA2) was originally identified as a substrate of the pp60v-src oncoprotein in transformed chicken embryonic fibroblasts. It is an abundant protein that associates with biological membranes as well as the actin cytoskeleton, and has been implicated in intracellular vesicle fusion, the organization of memb...

journal_title：British journal of pharmacology

authors： Liu Y,Myrvang HK,Dekker LV

更新日期：2015-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The chemokine receptor CXCR3 is implicated in a variety of clinically important diseases, notably rheumatoid arthritis and atherosclerosis. Consequently, antagonists of CXCR3 are of therapeutic interest. In this study, we set out to characterize binding sites of the specific low MW CXCR3 antagoni...

journal_title：British journal of pharmacology

authors： Nedjai B,Viney JM,Li H,Hull C,Anderson CA,Horie T,Horuk R,Vaidehi N,Pease JE

更新日期：2015-04-01 00:00:00

abstract：:Mitochondrial permeability transition pore (mPTP) opening plays a critical role in cardiac reperfusion injury and its prevention is cardioprotective. Tumour cell mitochondria usually have high levels of hexokinase isoform 2 (HK2) bound to their outer mitochondrial membranes (OMM) and HK2 binding to heart mitochondria ...

journal_title：British journal of pharmacology

authors： Halestrap AP,Pereira GC,Pasdois P

更新日期：2015-04-01 00:00:00

abstract：:Carbon monoxide (CO) is firmly established as an important, physiological signalling molecule as well as a potent toxin. Through its ability to bind metal-containing proteins, it is known to interfere with a number of intracellular signalling pathways, and such actions can account for its physiological and pathologica...

journal_title：British journal of pharmacology

authors： Peers C,Boyle JP,Scragg JL,Dallas ML,Al-Owais MM,Hettiarachichi NT,Elies J,Johnson E,Gamper N,Steele DS

更新日期：2015-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Treatment with selective oestrogen receptor modulators (SERMs) reduces low-density lipoprotein (LDL) cholesterol levels. We assessed the effect of tamoxifen, raloxifene and toremifene and their combinations with lovastatin on LDL receptor activity in lymphocytes from normolipidaemic and familial ...

journal_title：British journal of pharmacology

authors： Cerrato F,Fernández-Suárez ME,Alonso R,Alonso M,Vázquez C,Pastor O,Mata P,Lasunción MA,Gómez-Coronado D

更新日期：2015-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:MLN4924 prevents the formation of active cullin-RING ubiquitin ligase complexes and thus inhibits NF-κB signalling. Here, we evaluated the effects of this compound on monocytes and dendritic cells (DCs). EXPERIMENTAL APPROACH:Monocytes and DCs were challenged with TNF or LPS in the presence and ...

journal_title：British journal of pharmacology

authors： El-Mesery M,Seher A,Stühmer T,Siegmund D,Wajant H

更新日期：2015-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Memantine and ketamine are clinically used, open-channel blockers of NMDA receptors exhibiting remarkable pharmacodynamic similarities despite strikingly different clinical profiles. Although NMDA channel gating constitutes an important difference between memantine and ketamine, it is unclear how...

journal_title：British journal of pharmacology

authors： Emnett CM,Eisenman LN,Mohan J,Taylor AA,Doherty JJ,Paul SM,Zorumski CF,Mennerick S

更新日期：2015-03-01 00:00:00

abstract：:It is well documented that metabolic syndrome (i.e. a group of risk factors, such as abdominal obesity, elevated blood pressure, elevated fasting plasma glucose, high serum triglycerides and low cholesterol level in high-density lipoprotein), which raises the risk for heart disease and diabetes, is associated with inc...

journal_title：British journal of pharmacology

authors： Pechánová O,Varga ZV,Cebová M,Giricz Z,Pacher P,Ferdinandy P

更新日期：2015-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Histone deacetylase 6 (HDAC6) and silent information regulator 2 (SIRT2) control the dynamics of the microtubule network via their deacetylase activities. Tubulin polymerization promoting protein (TPPP/p25) enhances microtubule acetylation by its direct binding to HDAC6. Our objective was to char...

journal_title：British journal of pharmacology

authors： Mangas-Sanjuan V,Oláh J,Gonzalez-Alvarez I,Lehotzky A,Tőkési N,Bermejo M,Ovádi J

更新日期：2015-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Post-operative ileus (POI) is induced by intestinal inflammation. Here, we aimed to clarify the effects of 5-HT3 receptor antagonists against POI. EXPERIMENTAL APPROACH:We administered three 5-HT3 receptor antagonists, ondansetron, tropisetron and palonosetron, to a mouse model of POI induced by...

journal_title：British journal of pharmacology

authors： Maehara T,Matsumoto K,Horiguchi K,Kondo M,Iino S,Horie S,Murata T,Tsubone H,Shimada S,Ozaki H,Hori M

更新日期：2015-02-01 00:00:00

abstract：:PPARδ is a ligand-activated receptor that dimerizes with another nuclear receptor of the retinoic acid receptor family. The dimers interact with other co-activator proteins and form active complexes that bind to PPAR response elements and promote transcription of genes involved in lipid metabolism. It appears that var...

journal_title：British journal of pharmacology

authors： Kahremany S,Livne A,Gruzman A,Senderowitz H,Sasson S

更新日期：2015-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Acute activation of κ opioid (KOP) receptors results in anticocaine-like effects, but adverse effects, such as dysphoria, aversion, sedation and depression, limit their clinical development. Salvinorin A, isolated from the plant Salvia divinorum, and its semi-synthetic analogues have been shown t...

journal_title：British journal of pharmacology

authors： Simonson B,Morani AS,Ewald AW,Walker L,Kumar N,Simpson D,Miller JH,Prisinzano TE,Kivell BM

更新日期：2015-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Pancreatic cancer is characterized by alterations in several key signalling proteins, including increased expression and activity of the Src tyrosine kinase and focal adhesion kinase (FAK), which have been linked to its chemoresistance. Sustained Src inhibition reactivates survival pathways regul...

journal_title：British journal of pharmacology

authors： Pathania D,Kuang Y,Sechi M,Neamati N

更新日期：2015-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:N-docosahexaenoylethanolamine (DHEA) is the ethanolamine conjugate of the long-chain polyunsaturated n-3 fatty acid docosahexaenoic (DHA; 22: 6n-3). Its concentration in animal tissues and human plasma increases when diets rich in fish or krill oil are consumed. DHEA displays anti-inflammatory pr...

journal_title：British journal of pharmacology

authors： Meijerink J,Poland M,Balvers MG,Plastina P,Lute C,Dwarkasing J,van Norren K,Witkamp RF

更新日期：2015-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Insulin stimulates the transport of glucose in target tissues by triggering the translocation of glucose transporter 4 (GLUT4) to the plasma membrane. Resistance to insulin, the major abnormality in type 2 diabetes, results in a decreased GLUT4 translocation efficiency. Thus, special attention is...

journal_title：British journal of pharmacology

authors： Lanzerstorfer P,Stadlbauer V,Chtcheglova LA,Haselgrübler R,Borgmann D,Wruss J,Hinterdorfer P,Schröder K,Winkler SM,Höglinger O,Weghuber J

更新日期：2014-12-01 00:00:00

abstract：UNLABELLED:Reorganization of the actin cytoskeleton is essential for cell motility and chemotaxis. Actin-binding proteins (ABPs) and membrane lipids, especially phosphoinositides PI(4,5)P2 and PI(3,4,5)P3 are involved in the regulation of this reorganization. At least 15 ABPs have been reported to interact with, or reg...

journal_title：British journal of pharmacology

authors： Wu CY,Lin MW,Wu DC,Huang YB,Huang HT,Chen CL

更新日期：2014-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Impaired function of spinal strychnine-sensitive glycine receptors gives rise to chronic pain states and movement disorders. Therefore, increased activity of glycine receptors should help to treat such disorders. Although compounds targeting glycine receptors with a high selectivity are lacking, ...

journal_title：British journal of pharmacology

authors： Eckle VS,Grasshoff C,Mirakaj V,O'Neill PM,Berry NG,Leuwer M,Antkowiak B

更新日期：2014-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Endogenous cannabinoids (endocannabinoids) in the periaqueductal grey (PAG) play a vital role in mediating stress-induced analgesia. This analgesic effect of endocannabinoids is enhanced by pharmacological inhibition of their degradative enzymes. However, the specific effects of endocannabinoids ...

journal_title：British journal of pharmacology

authors： Lau BK,Drew GM,Mitchell VA,Vaughan CW

更新日期：2014-12-01 00:00:00

abstract：UNLABELLED:Cell movement is a fundamental process of normal cellular physiology and pathophysiology. Abnormal regulation of cell migration is a common denominator of many medical disorders, including cancer metastasis, autoimmune disease and inflammation. Increased interest in the targeting of cell migration and invasi...

journal_title：British journal of pharmacology

authors： Detchokul S,Frauman AG

更新日期：2014-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Caffeine is one of the most commonly used psychoactive substances. Circadian rhythms consist of the main suprachiasmatic nucleus (SCN) clocks and peripheral clocks. Although caffeine lengthens circadian rhythms and modifies phase changes in SCN-operated rhythms, the effects on caffeine on the pha...

journal_title：British journal of pharmacology

authors： Narishige S,Kuwahara M,Shinozaki A,Okada S,Ikeda Y,Kamagata M,Tahara Y,Shibata S

更新日期：2014-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Combretastatin A-4 3-O-phosphate (CA4P) is in clinical trial as a tumour vascular disrupting agent (VDA) but the cause of blood flow disruption is unclear. We tested the hypothesis that activation of Rho/Rho kinase (ROCK) is fundamental to the effects of this drug in vivo. EXPERIMENTAL APPROACH:...

journal_title：British journal of pharmacology

authors： Williams LJ,Mukherjee D,Fisher M,Reyes-Aldasoro CC,Akerman S,Kanthou C,Tozer GM

更新日期：2014-11-01 00:00:00

abstract：:In recent years there has been a growing recognition of the influence of sex on brain structure and function, and in relation, on the susceptibility, prevalence and response to treatment of psychiatric disorders. Most theories and descriptions of the effects of sex on the brain are dominated by an analogy to the curre...

journal_title：British journal of pharmacology

authors： Joel D,Yankelevitch-Yahav R

更新日期：2014-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Orexins have been demonstrated to play important roles in many physiological processes. However, it is not known how orexin A affects the activity of the hypoglossal motoneuron (HMN) and genioglossus (GG) muscle. EXPERIMENTAL APPROACH:GG muscle electromyograms (GG-EMG) were recorded in anaesthet...

journal_title：British journal of pharmacology

authors： Zhang GH,Liu ZL,Zhang BJ,Geng WY,Song NN,Zhou W,Cao YX,Li SQ,Huang ZL,Shen LL

更新日期：2014-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:An innovative chemical approach, named peptide welding technology (PWT), allows the synthesis of multibranched peptides with extraordinary high yield, purity and reproducibility. With this approach, three different tetrabranched derivatives of nociceptin/orphanin FQ (N/OFQ) have been synthesized ...

journal_title：British journal of pharmacology

authors： Rizzi A,Malfacini D,Cerlesi MC,Ruzza C,Marzola E,Bird MF,Rowbotham DJ,Salvadori S,Guerrini R,Lambert DG,Calo G

更新日期：2014-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Ischaemia compromises mitochondrial respiration. Consequently, the mitochondrial F1 Fo-ATPsynthase reverses and acts as a proton-pumping ATPase, so maintaining the mitochondrial membrane potential (ΔΨm ), while accelerating ATP depletion and cell death. Here we have looked for a molecule that can...

journal_title：British journal of pharmacology

authors： Ivanes F,Faccenda D,Gatliff J,Ahmed AA,Cocco S,Cheng CH,Allan E,Russell C,Duchen MR,Campanella M

更新日期：2014-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Proteinase activated receptor 2 (PAR2) is a GPCR associated with inflammation, metabolism and disease. Clues to understanding how to block PAR2 signalling associated with disease without inhibiting PAR2 activation in normal physiology could be provided by studies of biased signalling. EXPERIMENT...

journal_title：British journal of pharmacology

authors： Suen JY,Cotterell A,Lohman RJ,Lim J,Han A,Yau MK,Liu L,Cooper MA,Vesey DA,Fairlie DP

更新日期：2014-09-01 00:00:00

abstract：:GPCRs can interact with each other to form homomers or heteromers. Homomers involve interactions with the same receptor type while heteromers involve interactions between two different GPCRs. These receptor-receptor interactions modulate not only the binding but also the signalling and trafficking properties of indivi...

journal_title：British journal of pharmacology

authors： Fujita W,Gomes I,Devi LA

更新日期：2014-09-01 00:00:00

abstract：:Multiple myeloma is a neoplastic disorder of plasma cells characterized by clonal proliferation within the bone marrow. One of the major clinical features of multiple myeloma is the destructive osteolytic bone disease that occurs in the majority of patients. Myeloma bone disease is associated with increased osteoclast...

journal_title：British journal of pharmacology

authors： Webb SL,Edwards CM

更新日期：2014-08-01 00:00:00