abstract：BACKGROUND AND PURPOSE:Allosteric modulators of ionotropic receptors and GPCRs might constitute valuable therapeutic tools for intervention in several diseases, including Parkinson's disease (PD). However, the possibility that some of these compounds could alter neurotransmission in health and disease has not been thor...

journal_title：British journal of pharmacology

authors： Zhang X,Feng ZJ,Chergui K

更新日期：2014-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Varenicline, a neuronal nicotinic acetylcholine receptor (nAChR) modulator, decreases ethanol consumption in rodents and humans. The proposed mechanism of action for varenicline to reduce ethanol consumption has been through modulation of dopamine (DA) release in the nucleus accumbens (NAc) via α...

journal_title：British journal of pharmacology

authors： Feduccia AA,Simms JA,Mill D,Yi HY,Bartlett SE

更新日期：2014-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Suramin is a clinically prescribed drug for treatment of human African trypanosomiasis, cancer and infection. It is also a well-known pharmacological antagonist of P2 purinoceptors. Despite its clinical use and use in research, the biological actions of this molecule are still incompletely unders...

journal_title：British journal of pharmacology

authors： Chi Y,Gao K,Zhang H,Takeda M,Yao J

更新日期：2014-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Idiopathic pulmonary fibrosis (IPF) is a progressive fibro-proliferative disorder refractory to current therapy commonly complicated by the development of pulmonary hypertension (PH); the associated morbidity and mortality are substantial. Natriuretic peptides possess vasodilator and anti-fibroti...

journal_title：British journal of pharmacology

authors： Baliga RS,Scotton CJ,Trinder SL,Chambers RC,MacAllister RJ,Hobbs AJ

更新日期：2014-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Cerebrovascular remodelling is one of the important risk factors of stroke. The underlying mechanisms are unclear. Integrin β3 and volume-regulated ClC-3 Cl(-) channels have recently been implicated as important contributors to vascular cell proliferation. Therefore, we investigated the role of i...

journal_title：British journal of pharmacology

authors： Zeng JW,Wang XG,Ma MM,Lv XF,Liu J,Zhou JG,Guan YY

更新日期：2014-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Dysfunction and injury of endothelial cells in the pulmonary artery play critical roles in the hypertension induced by chronic hypoxia. One consequence of hypoxia is increased activity of 15-hydroxyprostaglandin dehydrogenase (PGDH). Here, we have explored, in detail, the effects of hypoxia on th...

journal_title：British journal of pharmacology

authors： Ma C,Liu Y,Wang Y,Zhang C,Yao H,Ma J,Zhang L,Zhang D,Shen T,Zhu D

更新日期：2014-07-01 00:00:00

abstract：:Diabetes mellitus belongs to the most rapidly increasing diseases worldwide. Approximately 90-95% of these patients suffer from type 2 diabetes mellitus, which is characterized by peripheral insulin resistance and the progressive loss of beta-cell function and mass. Considering the complications of this chronic diseas...

journal_title：British journal of pharmacology

authors： Kaiser D,Oetjen E

更新日期：2014-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:We determined the effects of treatment with LR-90, an inhibitor of advanced glycation end products, on the mechanical properties of the arterial system in streptozotocin (STZ)-induced diabetic Sprague Dawley rats, using aortic impedance analysis, and further investigated the effects of LR-90 on t...

journal_title：British journal of pharmacology

authors： Satheesan S,Figarola JL,Dabbs T,Rahbar S,Ermel R

更新日期：2014-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Marijuana smoking is widespread in many countries, and the use of smoked synthetic cannabinoids is increasing. Smoking a marijuana joint leads to bronchodilation in both healthy subjects and asthmatics. The effects of Δ(9) -tetrahydrocannabinol and synthetic cannabinoids on human bronchus reactiv...

journal_title：British journal of pharmacology

authors： Grassin-Delyle S,Naline E,Buenestado A,Faisy C,Alvarez JC,Salvator H,Abrial C,Advenier C,Zemoura L,Devillier P

更新日期：2014-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Intestinal mucositis is a common side-effect of irinotecan-based cancer chemotherapy regimens. This mucositis is associated with cytokine activation and NO synthesis. Production of IL-18 is up-regulated in patients suffering from inflammatory bowel disease. Therefore, we have investigated the rol...

journal_title：British journal of pharmacology

authors： Lima-Júnior RC,Freitas HC,Wong DV,Wanderley CW,Nunes LG,Leite LL,Miranda SP,Souza MH,Brito GA,Magalhães PJ,Teixeira MM,Cunha FQ,Ribeiro RA

更新日期：2014-05-01 00:00:00

abstract：:Until recently, hydrogen sulfide (H2 S) was exclusively viewed a toxic gas and an environmental hazard, with its toxicity primarily attributed to the inhibition of mitochondrial Complex IV, resulting in a shutdown of mitochondrial electron transport and cellular ATP generation. Work over the last decade established mu...

journal_title：British journal of pharmacology

authors： Szabo C,Ransy C,Módis K,Andriamihaja M,Murghes B,Coletta C,Olah G,Yanagi K,Bouillaud F

更新日期：2014-04-01 00:00:00

abstract：:Amyotrophic lateral sclerosis (ALS) is an adult-onset neurodegenerative disease characterized by the selective death of upper and lower motor neurons which ultimately leads to paralysis and ultimately death. Pathological changes in ALS are closely associated with pronounced and progressive changes in mitochondrial mor...

journal_title：British journal of pharmacology

authors： Muyderman H,Chen T

更新日期：2014-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:(R,S)-ketamine produces rapid and significant antidepressant effects in approximately 65% of patients suffering from treatment-resistant bipolar depression (BD). The genetic, pharmacological and biochemical differences between ketamine responders and non-responders have not been identified. The p...

journal_title：British journal of pharmacology

authors： Villaseñor A,Ramamoorthy A,Silva dos Santos M,Lorenzo MP,Laje G,Zarate C Jr,Barbas C,Wainer IW

更新日期：2014-04-01 00:00:00

abstract：:The phenanthrene-derivative 9-phenanthrol is a recently identified inhibitor of the transient receptor potential melastatin (TRPM) 4 channel, a Ca(2+) -activated non-selective cation channel whose mechanism of action remains to be determined. Subsequent studies performed on other ion channels confirm the specificity o...

journal_title：British journal of pharmacology

authors： Guinamard R,Hof T,Del Negro CA

更新日期：2014-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Fatty acid amide hydrolase inhibitors show promise as a treatment for anxiety, depression and pain. Here we investigated whether perinatal exposure to URB597, a fatty acid amide hydrolase inhibitor, alters brain development and affects behaviour in adult mice. EXPERIMENTAL APPROACH:Mouse dams we...

journal_title：British journal of pharmacology

authors： Wu CS,Morgan D,Jew CP,Haskins C,Andrews MJ,Leishman E,Spencer CM,Czyzyk T,Bradshaw H,Mackie K,Lu HC

更新日期：2014-03-01 00:00:00

abstract：UNLABELLED:During life, new neurons are continually added to hippocampal circuitry, with evidence suggesting that these adult-born neurons are functionally linked to cognition and emotion. The mammalian brain contains actively dividing neural stem cells in discrete regions, including the subventricular zone of the late...

journal_title：British journal of pharmacology

authors： Downer EJ

更新日期：2014-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Melanin-concentrating hormone receptor 1 (MCH1 receptor) antagonists are being considered as anti-obesity agents. The present study reports a new class of MCH1 receptor antagonists with an 8-methylquinoline scaffold. The molecular mechanism of MCH1 receptor blockade by these antagonists was exami...

journal_title：British journal of pharmacology

authors： Sakurai T,Ogawa K,Ishihara Y,Kasai S,Nakayama M

更新日期：2014-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Retinoids, through their activation of retinoic acid receptors (RARs) and retinoid X receptors, regulate diverse cellular processes, and pharmacological intervention in their actions has been successful in the treatment of skin disorders and cancers. Despite the many beneficial effects, administr...

journal_title：British journal of pharmacology

authors： Yin S,Luo J,Qian A,Yu W,Hu H

更新日期：2014-03-01 00:00:00

abstract：:Tyrosine sulfation is a post-translational modification of secreted and transmembrane proteins, including many GPCRs such as chemokine receptors. Most chemokine receptors contain several potentially sulfated tyrosine residues in their extracellular N-terminal regions, the initial binding site for chemokine ligands. Su...

journal_title：British journal of pharmacology

authors： Ludeman JP,Stone MJ

更新日期：2014-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Although the stoichiometry of the major synaptic αβγ subunit-containing GABAA receptors has consensus support for 2α:2β:1γ, a clear view of the stoichiometry of extrasynaptic receptors containing δ subunits has remained elusive. Here we examine the subunit stoichiometry of recombinant α4β3δ recep...

journal_title：British journal of pharmacology

authors： Patel B,Mortensen M,Smart TG

更新日期：2014-02-01 00:00:00

abstract：:Pulmonary arterial hypertension (PAH) is a complex disease characterized by elevated pulmonary arterial pressure, pulmonary vascular remodelling and occlusive pulmonary vascular lesions, leading to right heart failure. Evidence from recent epidemiological studies suggests the influence of gender on the development of ...

journal_title：British journal of pharmacology

authors： Mair KM,Johansen AK,Wright AF,Wallace E,MacLean MR

更新日期：2014-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Many dementia patients exhibit behavioural and psychological symptoms (BPSD) that include psychosis, aggressivity, depression and anxiety. Antipsychotic drugs are frequently prescribed but fail to significantly attenuate mood deficits, may interfere with cognitive function and are associated with...

journal_title：British journal of pharmacology

authors： Kołaczkowski M,Mierzejewski P,Bieńkowski P,Wesołowska A,Newman-Tancredi A

更新日期：2014-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Transient receptor potential melastatin 3 (TRPM3) proteins form non-selective but calcium-permeable membrane channels, rapidly activated by extracellular application of the steroid pregnenolone sulphate and the dihydropyridine nifedipine. Our aim was to characterize the steroid binding site by an...

journal_title：British journal of pharmacology

authors： Drews A,Mohr F,Rizun O,Wagner TF,Dembla S,Rudolph S,Lambert S,Konrad M,Philipp SE,Behrendt M,Marchais-Oberwinkler S,Covey DF,Oberwinkler J

更新日期：2014-02-01 00:00:00

abstract：UNLABELLED:Midkine (MK) is a heparin-binding growth factor or cytokine and forms a small protein family, the other member of which is pleiotrophin. MK enhances survival, migration, cytokine expression, differentiation and other activities of target cells. MK is involved in various physiological processes, such as devel...

journal_title：British journal of pharmacology

authors： Muramatsu T

更新日期：2014-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:While selective, bitter tasting, TAS2R agonists can relax agonist-contracted airway smooth muscle (ASM), their mechanism of action is unclear. However, ASM contraction is regulated by Ca²⁺ signalling and Ca²⁺ sensitivity. We have therefore investigated how the TAS2R10 agonists chloroquine, quinin...

journal_title：British journal of pharmacology

authors： Tan X,Sanderson MJ

更新日期：2014-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The electromechanical window (EMW), the interval between the end of the T-wave and the end of the left ventricular pressure (LVP) curve, has recently been proposed as a predictor of risk of Torsade de Pointes (TdP) in healthy animals, whereby a negative EMW (mechanical relaxation earlier than rep...

journal_title：British journal of pharmacology

authors： Stams TR,Bourgonje VJ,Beekman HD,Schoenmakers M,van der Nagel R,Oosterhoff P,van Opstal JM,Vos MA

更新日期：2014-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Antiretroviral (ARV) drugs activate pregnane X receptors and constitutive androstane receptors, increasing the risk of drug interactions due to altered drug metabolism and disposition. The closely related liver X receptors (LXRα/β), oestrogen receptors (ERα/β) and glucocorticoid receptor (GR) reg...

journal_title：British journal of pharmacology

authors： Svärd J,Blanco F,Nevin D,Fayne D,Mulcahy F,Hennessy M,Spiers JP

更新日期：2014-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Saponins isolated from Panax notoginseng (Burk.) F.H. Chen have been shown to relieve thrombogenesis and facilitate haemostasis. However, it is not known which saponin accounts for this haemostatic effect. Hence, in the present study we aimed to identify which saponins contribute to its haemostat...

journal_title：British journal of pharmacology

authors： Gao B,Huang L,Liu H,Wu H,Zhang E,Yang L,Wu X,Wang Z

更新日期：2014-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Hypoxia in tumours is known to cause resistance to conventional chemotherapeutic drugs. In contrast, little is known about the effects of hypoxia on targeted anti-cancer drugs. This study evaluated the effect of hypoxia on a series of clinically approved tyrosine kinase inhibitors (TKIs). EXPERI...

journal_title：British journal of pharmacology

authors： Ahmadi M,Ahmadihosseini Z,Allison SJ,Begum S,Rockley K,Sadiq M,Chintamaneni S,Lokwani R,Hughes N,Phillips RM

更新日期：2014-01-01 00:00:00

abstract：:The Concise Guide to PHARMACOLOGY 2013/14 provides concise overviews of the key properties of over 2000 human drug targets with their pharmacology, plus links to an open access knowledgebase of drug targets and their ligands (www.guidetopharmacology.org), which provides more detailed views of target and ligand propert...

journal_title：British journal of pharmacology

authors： Alexander SP,Benson HE,Faccenda E,Pawson AJ,Sharman JL,Spedding M,Peters JA,Harmar AJ,CGTP Collaborators.

更新日期：2013-12-01 00:00:00

abstract：UNLABELLED:Sensory neurons play important roles in many disorders, including inflammatory diseases, such as sepsis. Sepsis is a potentially lethal systemic inflammatory reaction to a local bacterial infection, affecting thousands of patients annually. Although associated with a high mortality rate, sepsis outcome depen...

journal_title：British journal of pharmacology

authors： Bodkin JV,Fernandes ES

更新日期：2013-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:4-[3,5-Bis(2-chlorobenzylidene)-4-oxo-piperidine-1-yl]-4-oxo-2-butenoic acid CLEFMA is a new anti-cancer molecule. Here, we investigated changes in apoptosis and inflammatory markers during CLEFMA-induced tumour suppression. EXPERIMENTAL APPROACH:Lung adenocarcinoma H441 and A549, and normal lun...

journal_title：British journal of pharmacology

authors： Yadav VR,Sahoo K,Awasthi V

更新日期：2013-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Bleomycin (BLM), one of the most common sclerosants, is often used to treat venous malformations (VMs). The present study was designed to investigate whether endothelial mesenchymal transition (EndoMT) contributes to the therapeutic effects of BLM. EXPERIMENTAL APPROACH:Endothelial and mesenchym...

journal_title：British journal of pharmacology

authors： Zhang W,Chen G,Ren JG,Zhao YF

更新日期：2013-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:In addition to typical GPCR kinase (GRK)-/β-arrestin-dependent internalization, dopamine D3 receptor employed an additional GRK-independent sequestration pathway. In this study, we investigated the molecular mechanism of this novel sequestration pathway. EXPERIMENTAL APPROACH:Radioligand binding...

journal_title：British journal of pharmacology

authors： Min C,Zheng M,Zhang X,Caron MG,Kim KM

更新日期：2013-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Sublesional osteoporosis predisposes individuals with spinal cord injury (SCI) to an increased risk of low-trauma fracture. The aim of the present work was to investigate the effect of treatment with resveratrol (RES) on sublesional bone loss in spinal cord-injured rats. EXPERIMENTAL APPROACH:Co...

journal_title：British journal of pharmacology

authors： Wang HD,Shi YM,Li L,Guo JD,Zhang YP,Hou SX

更新日期：2013-10-01 00:00:00

abstract：UNLABELLED:Sarcoplasmic reticular (SR) Ca(2+) -ATPase (SERCA2a) is central to cardiac electrophysiological and mechanical function. It ensures full diastolic relaxation minimizing delayed after-potentials that would otherwise compromise membrane electrophysiological stability, and optimizes SR Ca(2+) refilling and syst...

journal_title：British journal of pharmacology

authors： Huang CL

更新日期：2013-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The presence of the histamine H₄ receptor (H₄R) was previously reported in benign and malignant lesions and cell lines derived from the human mammary gland. The aim of this work was to evaluate the effects of H₄R ligands on the survival, tumour growth rate and metastatic capacity of breast cancer...

journal_title：British journal of pharmacology

authors： Martinel Lamas DJ,Croci M,Carabajal E,Crescenti EJ,Sambuco L,Massari NA,Bergoc RM,Rivera ES,Medina VA

更新日期：2013-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Nitric oxide (NO) is known to activate NO-sensitive guanylyl cyclase (NO-GC) and to elicit cGMP production. However, NO has also been proposed to induce cGMP-independent effects. It is accepted practice to use specific NO-GC inhibitors, such as ODQ or NS2028, to assess cGMP-dependent NO effects. ...

journal_title：British journal of pharmacology

authors： Lies B,Groneberg D,Gambaryan S,Friebe A

更新日期：2013-09-01 00:00:00

abstract：:Biological nitrogen oxide signalling and stress is an area of extreme clinical, pharmacological, toxicological, biochemical and chemical research interest. The utility of nitric oxide and derived species as signalling agents is due to their novel and vast chemical interactions with a variety of biological targets. Her...

journal_title：British journal of pharmacology

authors： Heinrich TA,da Silva RS,Miranda KM,Switzer CH,Wink DA,Fukuto JM

更新日期：2013-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The homeostatic control of arterial BP is well understood with changes in BP resulting from changes in cardiac output (CO) and/or total peripheral resistance (TPR). A mechanism-based and quantitative analysis of drug effects on this interrelationship could provide a basis for the prediction of dr...

journal_title：British journal of pharmacology

authors： Snelder N,Ploeger BA,Luttringer O,Rigel DF,Webb RL,Feldman D,Fu F,Beil M,Jin L,Stanski DR,Danhof M

更新日期：2013-08-01 00:00:00