abstract：BACKGROUND AND PURPOSE:Atherosclerosis is associated with reduced vascular hydrogen sulfide (H2 S) biosynthesis. GYY4137 is a novel slow-releasing H2 S compound that may effectively mimic the time course of H2 S release in vivo. However, it is not known whether GYY4137 affects atherosclerosis. EXPERIMENTAL APPROACH:RA...

journal_title：British journal of pharmacology

authors： Liu Z,Han Y,Li L,Lu H,Meng G,Li X,Shirhan M,Peh MT,Xie L,Zhou S,Wang X,Chen Q,Dai W,Tan CH,Pan S,Moore PK,Ji Y

更新日期：2013-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Normal pregnancy is associated with decreased vascular resistance and increased release of vasodilators. Endothelin-1 (ET-1) causes vasoconstriction via endothelin receptor type A (ET(A)R), but could activate ET(B)R in the endothelium and release vasodilator substances. However, the roles of ET(B...

journal_title：British journal of pharmacology

authors： Mazzuca MQ,Dang Y,Khalil RA

更新日期：2013-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:PPAR-γ has been reported to be a protective regulator in ischaemia/reperfusion (I/R) injury. The receptor for advanced glycation end-products (RAGE) plays a major role in the innate immune response, and its expression is associated with PPAR-γ activation. Several angiotensin receptor blockers pos...

journal_title：British journal of pharmacology

authors： Koh EJ,Yoon SJ,Lee SM

更新日期：2013-07-01 00:00:00

abstract：:Two-state and operational models of both agonism and allosterism are compared to identify and characterize common pharmacological parameters. To account for the receptor-dependent basal response, constitutive receptor activity is considered in the operational models. By arranging two-state models as the fraction of ac...

journal_title：British journal of pharmacology

authors： Roche D,Gil D,Giraldo J

更新日期：2013-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Small molecule glucokinase activators (GKAs) have been associated with potent antidiabetic efficacy and hepatic steatosis in rodents. This study reports the discovery of S 50131 and S 51434, two novel GKAs with an original scaffold and an atypical pharmacological profile. EXPERIMENTAL APPROACH:A...

journal_title：British journal of pharmacology

authors： De Ceuninck F,Kargar C,Charton Y,Goldstein S,Perron-Sierra F,Ilic C,Caliez A,Rolin JO,Sadlo M,Harley E,Vinson C,Ktorza A

更新日期：2013-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Down's syndrome is a common genetic cause of intellectual disability, for which there are no drug therapies. Mechanistic studies in a model of Down's syndrome [Ts65Dn (TS) mice] demonstrated that impaired cognitive function was due to excessive neuronal inhibitory tone. These deficits were normal...

journal_title：British journal of pharmacology

authors： Colas D,Chuluun B,Warrier D,Blank M,Wetmore DZ,Buckmaster P,Garner CC,Heller HC

更新日期：2013-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Pulmonary arterial hypertension (PAH) is characterized by enhanced pulmonary vascular resistance, right ventricular hypertrophy and increased right ventricular systolic pressure. Here, we investigated the effects of a N-acylhydrazone derivative, 3,4-dimethoxyphenyl-N-methyl-benzoylhydrazide (LASS...

journal_title：British journal of pharmacology

authors： Alencar AK,Pereira SL,Montagnoli TL,Maia RC,Kümmerle AE,Landgraf SS,Caruso-Neves C,Ferraz EB,Tesch R,Nascimento JH,de Sant'Anna CM,Fraga CA,Barreiro EJ,Sudo RT,Zapata-Sudo G

更新日期：2013-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Quercetin is a natural polyphenolic flavonoid that displays anti-diabetic properties in vivo. Its mechanism of action on insulin-secreting beta cells is poorly documented. In this work, we have analysed the effects of quercetin both on insulin secretion and on the intracellular calcium concentrat...

journal_title：British journal of pharmacology

authors： Bardy G,Virsolvy A,Quignard JF,Ravier MA,Bertrand G,Dalle S,Cros G,Magous R,Richard S,Oiry C

更新日期：2013-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:GPR18 is a recently deorphaned lipid receptor that is activated by the endogenous lipid N-arachidonoyl glycine (NAGly) as well the behaviourally inactive atypical cannabinoid, abnormal cannabidiol (Abn-CBD). The presence and/or function of any GPR18-based ocular signalling system remain essential...

journal_title：British journal of pharmacology

authors： Caldwell MD,Hu SS,Viswanathan S,Bradshaw H,Kelly ME,Straiker A

更新日期：2013-06-01 00:00:00

abstract：:Recent advances have improved our understanding of the renin-angiotensin system (RAS). These have included the recognition that angiotensin (Ang)-(1-7) is a biologically active product of the RAS cascade. The identification of the ACE homologue ACE2, which forms Ang-(1-7) from Ang II, and the GPCR Mas as an Ang-(1-7) ...

journal_title：British journal of pharmacology

authors： Simões e Silva AC,Silveira KD,Ferreira AJ,Teixeira MM

更新日期：2013-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:In small arteries, small conductance Ca²⁺-activated K⁺ channels (SK(Ca)) and intermediate conductance Ca²⁺-activated K⁺ channels (IK(Ca)) restricted to the vascular endothelium generate hyperpolarization that underpins the NO- and PGI₂-independent, endothelium-derived hyperpolarizing factor respo...

journal_title：British journal of pharmacology

authors： Yarova PL,Smirnov SV,Dora KA,Garland CJ

更新日期：2013-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Hydrogen sulphide (H2 S) is an endogenous gaseous signalling molecule with putative functions in gastrointestinal motility regulation. Characterization of H2 S effects on colonic motility is crucial to establish its potential use as therapeutic agent in the treatment of colonic disorders. EXPERI...

journal_title：British journal of pharmacology

authors： Gil V,Parsons S,Gallego D,Huizinga J,Jimenez M

更新日期：2013-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Voltage-gated sodium channels (VGSCs) are assembled from two classes of subunits, a pore-bearing α-subunit (NaV 1) and one or two accessory β-subunits (NaV βs). Neurons in mammals can express one or more of seven isoforms of NaV 1 and one or more of four isoforms of NaV β. The peptide μ-conotoxin...

journal_title：British journal of pharmacology

authors： Zhang MM,Wilson MJ,Azam L,Gajewiak J,Rivier JE,Bulaj G,Olivera BM,Yoshikami D

更新日期：2013-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Cigarette smoke is a major cause for chronic obstructive pulmonary disease (COPD). Andrographolide is an active biomolecule isolated from the plant Andrographis paniculata. Andrographolide has been shown to activate nuclear factor erythroid-2-related factor 2 (Nrf2), a redox-sensitive antioxidant...

journal_title：British journal of pharmacology

authors： Guan SP,Tee W,Ng DS,Chan TK,Peh HY,Ho WE,Cheng C,Mak JC,Wong WS

更新日期：2013-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:SU4312, a potent and selective inhibitor of VEGF receptor-2 (VEGFR-2), has been designed to treat cancer. Recent studies have suggested that SU4312 can also be useful in treating neurodegenerative disorders. In this study, we assessed neuroprotection by SU4312 against 1-methyl-4-phenylpyridinium ...

journal_title：British journal of pharmacology

authors： Cui W,Zhang Z,Li W,Hu S,Mak S,Zhang H,Han R,Yuan S,Li S,Sa F,Xu D,Lin Z,Zuo Z,Rong J,Ma ED,Choi TC,Lee SM,Han Y

更新日期：2013-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The effects of 4-O-methylhonokiol (MH), a constituent of Magnolia officinalis, were investigated on human prostate cancer cells and its mechanism of action elucidated. EXPERIMENTAL APPROACH:The anti-cancer effects of MH were examined in prostate cancer and normal cells. The effects were validate...

journal_title：British journal of pharmacology

authors： Lee NJ,Oh JH,Ban JO,Shim JH,Lee HP,Jung JK,Ahn BW,Yoon DY,Han SB,Ham YW,Hong JT

更新日期：2013-03-01 00:00:00

abstract：:The consumption of green tea (Camellia sinensis) has been shown to have many physiological and pharmacological health benefits. In the past two decades several studies have reported that epigallocatechin-3-gallate (EGCG), the main constituent of green tea, has anti-infective properties. Antiviral activities of EGCG wi...

journal_title：British journal of pharmacology

authors： Steinmann J,Buer J,Pietschmann T,Steinmann E

更新日期：2013-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Fibroblast-to-myofibroblast differentiation is associated with scarring, an important issue in corneal surgery. Moxifloxacin (MOX), commonly applied to prevent post-operative infection, would benefit more if it modifies fibroblast-to-myofibroblast differentiation other than antimicrobial activity...

journal_title：British journal of pharmacology

authors： Chen TC,Chang SW,Wang TY

更新日期：2013-03-01 00:00:00

abstract：AIMS:The trace amine-associated receptor (Taar) family displays high species- and subtype-specific pharmacology. Several trace amines such as β-phenylethylamine (β-PEA), p-tyramine and tryptamine are agonists at TA(1) but poorly activate rat and mouse Taar4. PRINCIPAL RESULTS:Using rat TA(1) and Taar4 chimera, we id...

journal_title：British journal of pharmacology

authors： Stäubert C,Bohnekamp J,Schöneberg T

更新日期：2013-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Evidence suggests that phosphorylation of TRPV1 is an important component underlying its aberrant activation in pathological pain states. To date, the detailed pharmacology of diverse TRPV1 receptor agonists and antagonists has yet to be reported for native TRPV1 under phosphorylating conditions....

journal_title：British journal of pharmacology

authors： Mogg AJ,Mill CE,Folly EA,Beattie RE,Blanco MJ,Beck JP,Broad LM

更新日期：2013-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Kinins are pro-inflammatory peptides that are released during tissue injury, including that caused by inflammatory bowel disease. Herein, we assessed the role and underlying mechanisms through which the absence of kinin B(1) receptors exacerbates the development of dextran sulfate sodium (DSS)-i...

journal_title：British journal of pharmacology

authors： Marcon R,Claudino RF,Dutra RC,Bento AF,Schmidt EC,Bouzon ZL,Sordi R,Morais RL,Pesquero JB,Calixto JB

更新日期：2013-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Recombinant human erythropoietin (rHuEPO) is currently the mainstay of renal anaemia treatment. Recently, rHuEPO has been shown to provide pleiotrophic tissue protection in various pathological conditions. However, the benefits of rHuEPO beyond anaemia treatment are limited because it increases r...

journal_title：British journal of pharmacology

authors： Chattong S,Tanamai J,Kiatsomchai P,Nakatsu M,Sereemaspun A,Pimpha N,Praditpornsilpa K,Rojanathanes R,Sethpakadee A,Tungsanga K,Eiam-Ong S,Manotham K

更新日期：2013-01-01 00:00:00

abstract：:Translational sciences increasingly emphasize the measurement of functions in native human tissues. However, such studies must confront variations in patient age, gender, genetic background and disease. Here, these are discussed with reference to neuromuscular and neurosecretory functions of the human gastrointestinal...

journal_title：British journal of pharmacology

authors： Sanger GJ,Broad J,Kung V,Knowles CH

更新日期：2013-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Ca(2+)-dependent Cl(-) secretion (CaCC) in airways and other tissues is due to activation of the Cl(-) channel TMEM16A (anoctamin 1). Earlier studies suggested that Ca(2+) -activated Cl(-) channels are regulated by membrane lipid inositol phosphates, and that 1-O-octyl-2-O-butyryl-myo-inositol 3,...

journal_title：British journal of pharmacology

authors： Tian Y,Schreiber R,Wanitchakool P,Kongsuphol P,Sousa M,Uliyakina I,Palma M,Faria D,Traynor-Kaplan AE,Fragata JI,Amaral MD,Kunzelmann K

更新日期：2013-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The passage of drugs across the blood-brain barrier (BBB) limits the efficacy of chemotherapy in brain tumours. For instance, the anticancer drug doxorubicin, which is effective against glioblastoma in vitro, has poor efficacy in vivo, because it is extruded by P-glycoprotein (Pgp/ABCB1), multidr...

journal_title：British journal of pharmacology

authors： Pinzón-Daza M,Garzón R,Couraud P,Romero Ia,Weksler B,Ghigo D,Bosia A,Riganti C

更新日期：2012-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:There is growing evidence that inflammation plays a major role in the pathogenesis of neural damage caused by deposition of amyloid β (Aβ) in the brain. Nimodipine has received attention as a drug that might improve learning and reduce cognitive deficits in Alzheimer's disease, but the mechanism ...

journal_title：British journal of pharmacology

authors： Sanz JM,Chiozzi P,Colaianna M,Zotti M,Ferrari D,Trabace L,Zuliani G,Di Virgilio F

更新日期：2012-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Calcitonin gene-related peptide (CGRP) is a potent vasodilator, implicated in the pathogenesis of migraine. CGRP activates a receptor complex comprising, calcitonin receptor-like receptor (CLR) and receptor activity-modifying protein 1 (RAMP1). In vitro studies indicate recycling of CLR●RAMP1 is ...

journal_title：British journal of pharmacology

authors： McNeish AJ,Roux BT,Aylett SB,Van Den Brink AM,Cottrell GS

更新日期：2012-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The cannabinoid receptor-mediated analgesic effects of 2-arachidonoylglycerol (2-AG) are limited by monoacylglycerol lipase (MAGL). 4-nitrophenyl 4-[bis (1,3-benzodioxol-5-yl) (hydroxy) methyl] piperidine-1-carboxylate (JZL184) is a potent inhibitor of MAGL in the mouse, though potency is reporte...

journal_title：British journal of pharmacology

authors： Woodhams SG,Wong A,Barrett DA,Bennett AJ,Chapman V,Alexander SP

更新日期：2012-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Pyrazole derivatives have recently been suggested as selective blockers of transient receptor potential cation (TRPC) channels but their ability to distinguish between the TRPC and Orai pore complexes is ill-defined. This study was designed to characterize a series of pyrazole derivatives in term...

journal_title：British journal of pharmacology

authors： Schleifer H,Doleschal B,Lichtenegger M,Oppenrieder R,Derler I,Frischauf I,Glasnov TN,Kappe CO,Romanin C,Groschner K

更新日期：2012-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Inhalation of the superantigen,staphylococcal enterotoxin B (SEB), leads to the activation of the host T and invariant natural killer (iNK) T cells, thereby resulting in acute lung inflammation and respiratory failure but the underlying mechanism(s) of disease remain elusive, with limited treatme...

journal_title：British journal of pharmacology

authors： Rieder SA,Nagarkatti P,Nagarkatti M

更新日期：2012-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:N-arachidonoyl 5-HT (NA-5HT) has anti-nociceptive effects reported to be mediated by inhibitory actions at the transient receptor potential vanilloid receptor 1 (TRPV1) and fatty acid amide hydrolase (FAAH). Anandamide and N-arachidonoyl dopamine (NA-DA), endocannabinoids that activate TRPV1 or a...

journal_title：British journal of pharmacology

authors： Gilmore AJ,Heblinski M,Reynolds A,Kassiou M,Connor M

更新日期：2012-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Pituitary adenylate cyclase-activating polypeptide (PACAP) is an excitatory neuropeptide with central and peripheral cardiovascular actions. Intrathecal PACAP increases splanchnic sympathetic nerve activity and heart rate, but not mean arterial pressure (MAP). We hypothesize that the three PACAP ...

journal_title：British journal of pharmacology

authors： Inglott MA,Lerner EA,Pilowsky PM,Farnham MM

更新日期：2012-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The use of tubulin-binding compounds, which act in part by inhibiting tumour angiogenesis, has become an integral strategy of tumour therapy. Recently, tubulysins were identified as a novel class of natural compounds of myxobacterial origin, which inhibit tubulin polymerization. As these compound...

journal_title：British journal of pharmacology

authors： Rath S,Liebl J,Fürst R,Ullrich A,Burkhart JL,Kazmaier U,Herrmann J,Müller R,Günther M,Schreiner L,Wagner E,Vollmar AM,Zahler S

更新日期：2012-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:In mammalian cells, the anti-parasitic drug ivermectin is known as a positive allosteric modulator of the ATP-activated ion channel P2X4 and is used to discriminate between P2X4- and P2X7-mediated cellular responses. In this paper we provide evidence that the reported isoform selectivity of iverm...

journal_title：British journal of pharmacology

authors： Nörenberg W,Sobottka H,Hempel C,Plötz T,Fischer W,Schmalzing G,Schaefer M

更新日期：2012-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Positive allosteric modulation of α4β2 nicotinic acetylcholine (nACh) receptors could add a new dimension to the pharmacology and therapeutic approach to these receptors. The novel modulator NS9283 was therefore tested extensively. EXPERIMENTAL APPROACH:Effects of NS9283 were evaluated in vitro ...

journal_title：British journal of pharmacology

authors： Timmermann DB,Sandager-Nielsen K,Dyhring T,Smith M,Jacobsen AM,Nielsen EØ,Grunnet M,Christensen JK,Peters D,Kohlhaas K,Olsen GM,Ahring PK

更新日期：2012-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Here, we have compared the neurochemical profile of three new cathinones, butylone, mephedrone and methylone, in terms of their potential to inhibit plasmalemmal and vesicular monoamine transporters. Their interaction with 5-HT and dopamine receptors and their psychostimulant effect was also stud...

journal_title：British journal of pharmacology

authors： López-Arnau R,Martínez-Clemente J,Pubill D,Escubedo E,Camarasa J

更新日期：2012-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Airway remodelling is a consequence of long-term inflammation and MAPKs are key signalling molecules that drive pro-inflammatory pathways. The endogenous MAPK deactivator--MAPK phosphatase 1 (MKP-1)--is a critical negative regulator of the myriad pro-inflammatory pathways activated by MAPKs in th...

journal_title：British journal of pharmacology

authors： Manetsch M,Ramsay EE,King EM,Seidel P,Che W,Ge Q,Hibbs DE,Newton R,Ammit AJ

更新日期：2012-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The sarcoplasmic reticulum Ca²⁺-ATPase (SERCA) plays a role in thermogenesis. The exogenous compound capsaicin increased SERCA-mediated ATP hydrolysis not coupled to Ca²⁺ transport. Here, we have sought to identify endogenous compounds that may function as SERCA uncoupling agents. EXPERIMENTAL A...

journal_title：British journal of pharmacology

authors： Mahmmoud YA,Gaster M

更新日期：2012-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Exposure to an acute stress inhibits gastric emptying and stimulates colonic transit via central neuropeptide Y (NPY) pathways; however, peripheral involvement is uncertain. The anxiogenic phenotype of NPY(-/-) mice is gender-dependent, raising the possibility that stress-induced gastrointestinal...

journal_title：British journal of pharmacology

authors： Forbes S,Herzog H,Cox HM

更新日期：2012-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:JNJ-Q2, a novel broad-spectrum fluoroquinolone with anti-methicillin-resistant Staphylococcus aureus activity, was evaluated in a comprehensive set of non-clinical and clinical cardiovascular safety studies. The effect of JNJ-Q2 on different cardiovascular parameters was compared with that of mox...

journal_title：British journal of pharmacology

authors： Eichenbaum G,Pugsley MK,Gallacher DJ,Towart R,McIntyre G,Shukla U,Davenport JM,Lu HR,Rohrbacher J,Hillsamer V

更新日期：2012-07-01 00:00:00