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British Journal of Pharmacology

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https://www.readbyqxmd.com/read/28728214/p2x-receptor-channels-in-chronic-pain-pathways
#1
REVIEW
Louis-Philippe Bernier, Ariel R Ase, Philippe Séguéla
Chronic pain is a highly prevalent debilitating condition for which treatment options remain limited for many patients. Ionotropic ATP signaling through excitatory and calcium-permeable P2X receptor-channels is now rightfully considered as a critical player in pathological pain generation and maintenance, therefore their selective targeting represents a therapeutic opportunity with promising yet untapped potential. Recent advances in the structural, functional and pharmacological characterization of rodent and human ATP-gated P2X receptor-channels have shed brighter light on the role of specific subtypes in the pathophysiology of chronic inflammatory, neuropathic or cancer pain...
July 20, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28726253/%C3%AE-9-and-%C3%AE-7-containing-receptors-mediate-the-pro-proliferative-effects-of-nicotine-in-the-a549-adenocarcinoma-cell-line
#2
Vanessa Mucchietto, Francesca Fasoli, Susanna Pucci, Milena Moretti, Roberta Benfante, Annalisa Maroli, Simona Di Lascio, Cristiano Bolchi, Marco Pallavicini, Cheryl Dowell, Michael McIntosh, Francesco Clementi, Cecilia Gotti
BACKGROUND AND PURPOSE: Tobacco smoke contains many classes of carcinogens and although nicotine is unable to initiate tumorigenesis in humans and rodents, it promotes tumour growth and metastasis in lung tumours by acting on neuronal nicotinic acetylcholine receptors (nAChRs). The aim of this study was to identify molecularly, biochemically and pharmacologically which nAChR subtypes are expressed and functionally activated by nicotine in lung cancer cell lines. EXPERIMENTAL APPROACH: We used A549 and H1975 adenocarcinoma cell lines derived from lung tumour to test the in vitro effects of nicotine, and nAChR subtype-specific peptides and compounds...
July 20, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28726252/central-amygdala-relaxin-3-rxfp3-signalling-modulates-alcohol-seeking-in-rats
#3
Leigh C Walker, Hanna E Kastman, Elena Krstew, Andrew L Gundlach, Andrew J Lawrence
BACKGROUND AND PURPOSE: Alcohol use disorders are a leading cause of preventable deaths worldwide and stress is a major trigger of relapse. The neuropeptide relaxin-3 and its cognate receptor, relaxin family peptide receptor 3 (RXFP3), modulate stress-induced relapse to alcohol seeking in rats and while the bed nucleus of the stria terminalis has been implicated in this regard, the central nucleus of the amygdala (CeA) also receives a relaxin-3 innervation and CeA neurons densely express RXFP3 mRNA...
July 20, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28718892/methoxetamine-affects-brain-processing-involved-in-emotional-response-in-rats
#4
M T Zanda, P Fadda, S Antinori, M di Chio, W Fratta, C Chiamulera, L Fattore
BACKGROUND AND PURPOSE: Methoxetamine (MXE) is a novel psychoactive substance that is emerging on the Internet and induces dissociative effects and acute toxicity. Yet, its pharmacological effects are still poorly investigated. EXPERIMENTAL APPROACH: We examined a range of behavioural effects induced by acute intraperitoneal administration of MXE (0.5-5 mg/kg) in rats, and whether it causes rapid neuroadaptive molecular changes. KEY RESULTS: MXE (0...
July 18, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28718891/mk-reduces-inhaled-chlorine-triggered-ahr-and-airway-inflammation-in-the-mouse
#5
Yoichiro Hamamoto, Satoshi Ano, Benoit Allard, Michael O'Sullivan, Toby K McGovern, James G Martin
BACKGROUND AND PURPOSE: Cysteinyl leukotrienes (CysLTs) are pro-inflammatory lipid mediators that exacerbate disease state in several asthma phenotypes including asthma induced by allergen, virus and exercise. However, the role of CysLTs in irritant-induced airway disease is not well characterized. The purpose of the current study was to investigate the effect of montelukast (MK), a CysLT1R antagonist, on parameters of irritant-induced asthma (IIA) induced by inhalation of chlorine (Cl2 ) in the mouse...
July 18, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28710789/atr-101-inhibits-cholesterol-efflux-and-cortisol-secretion-by-abc-transporters-causing-cytotoxic-cholesterol-accumulation-in-adrenocortical-carcinoma-cells
#6
Veronica Elizabeth Burns, Tom Klaus Kerppola
BACKGROUND AND PURPOSE: To further the development of new agents for the treatment of adrenocortical carcinoma (ACC), we characterized the molecular and cellular mechanisms of cytotoxicity by the adrenalytic compound ATR-101 (PD132301-02). EXPERIMENTAL APPROACH: We compared the effects of ATR-101, PD129337, and ABC transporter inhibitors, on cholesterol accumulation and efflux, on cortisol secretion, on ATP levels, and on caspase activation in ACC-derived cell lines...
July 14, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28707298/melatonin-receptors-molecular-pharmacology-and-signaling-in-the-context-of-system-bias
#7
REVIEW
Erika Cecon, Atsuro Oishi, Ralf Jockers
Melatonin, N-acetyl-5-methoxytryptamine, an evolutionally old molecule, is produced by the pineal gland in vertebrates and it binds with high affinity to melatonin receptors, which are members of the G protein-coupled receptor family. Among the multiple effects attributed to melatonin we will focus here on those that are dependent on the activation of the two mammalian MT1 and MT2 melatonin receptors. We briefly summarize the latest developments on synthetic melatonin receptor ligands, including multi-target-directed ligands, and the characterization of signaling-biased ligands...
July 13, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28703283/wnt-signaling-pathways-in-chronic-lymphocytic-leukemia-and-b-cell-lymphomas
#8
REVIEW
Pavlína Janovská, Vítězslav Bryja
In this review, we discuss the intricate roles of the WNT signaling network in the development and progression of mature B cell-derived hematological malignancies, with a focus on chronic lymphocytic leukemia (CLL) and related B cell lymphomas. We review the current literature and highlight the differences between the β-catenin-dependent and independent branches of WNT signaling. Special attention is paid to the role of the non-canonical WNT/Planar cell polarity (PCP) pathway, mediated by the WNT5-ROR1-Dishevelled (DVL) signaling axis in CLL...
July 12, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28703274/pterostilbene-reduces-oxidative-stress-prevents-hypertrophy-and-preserves-systolic-function-of-right-ventricle-in-cor-pulmonale-model
#9
Denise Dos Santos Lacerda, Patrick Türck, Bruna Gazzi de Lima-Seolin, Rafael Colombo, Vanessa Duarte Ortiz, Jéssica Hellen Poletto Bonetto, Cristina Campos-Carraro, Sara Elis Bianchi, Adriane Belló-Klein, Valquiria LinckBassani, Alex Sander da Rosa Araujo
BACKGROUND AND PURPOSE: In cor pulmonale, the increased afterload imposed on the right ventricle (RV) generates a maladaptive response, impairing the contractile cardiac function. Oxidative mechanisms play an important role in the pathophysiology and progression of this disease. The administration of pterostilbene (PTS), a phyto-phenol with antioxidant potential, may represent a therapeutic alternative. In the present study, the objective was to evaluate the effect of PTS complexed with hydroxypropyl-β-cyclodextrin (HPβCD) on hypertrophy, contractile function and oxidative parameters in the RV of rats with pulmonary hypertension induced by monocrotaline administration...
July 12, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28691737/evaluating-the-antifibrotic-potency-of-galunisertib-in-a-human-ex-vivo-model-of-liver-fibrosis
#10
Theerut Luangmonkong, Su Suriguga, Emilia Bigaeva, Miriam Boersema, Dorenda Oosterhuis, Koert P de Jong, Detlef Schuppan, Henricus A M Mutsaers, Peter Olinga
BACKGROUND AND PURPOSE: Liver fibrosis is a major cause of liver-related mortality. Yet, to date, no effective antifibrotic drug is available. Galunisertib, a TGF-β receptor type I kinase inhibitor, is a potential candidate for the treatment of liver fibrosis. Here, we evaluated the potency of galunisertib in a human ex vivo model of liver fibrosis. EXPERIMENTAL APPROACH: Antifibrotic potency and associated mechanisms were studied ex vivo, using both healthy and cirrhotic human precision-cut liver slices...
July 10, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28691227/changes-in-the-plasma-membrane-in-metabolic-disease-impact-of-the-membrane-environment-on-g-protein-coupled-receptor-structure-and-function
#11
REVIEW
Aditya J Desai, Laurence J Miller
Drug development targeting G protein-coupled receptors (GPCRs) often utilizes model heterologous cell expression systems, reflecting an implicit assumption that the membrane environment has little functional impact on these receptors or on their responsiveness to drugs. However, much recent data illustrates important functional impact that membrane components can have on intrinsic membrane proteins. This review is directed toward gaining a better understanding of the structure of the plasma membrane in health and disease, and how this organelle can influence GPCR structure, function, and regulation...
July 10, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28688167/inhibition-of-hyaluronan-synthesis-attenuates-pulmonary-hypertension-associated-with-lung-fibrosis
#12
Scott D Collum, Ning-Yuan Chen, Adriana M Hernandez, Ankit Hanmandlu, Heather Sweeney, Tinne C J Mertens, Tingting Weng, Fayong Luo, Jose G Molina, Jonathan Davies, Ian P Horan, Nick W Morrell, Javier Amione-Guerra, Odeaa Al-Jabbari, Keith Youker, Wenchao Sun, Jayakumar Rajadas, Paul L Bollyky, Bindu H Akkanti, Soma Jyothula, Neeraj Sinha, Ashrith Guha, Harry Karmouty-Quintana
BACKGROUND AND PURPOSE: Group III Pulmonary hypertension (PH) is a highly lethal and widespread lung disorder that is a common complication in idiopathic pulmonary fibrosis (IPF) where it is considered to be the single most significant predictor of mortality. While increased levels of hyaluronan have been observed in IPF patients, hyaluronan-mediated vascular remodelling and the hyaluronan-mediated mechanisms promoting PH associated with IPF are not fully understood. EXPERIMENTAL APPROACH: Explanted lung tissue from patients with IPF with and without a diagnosis of PH was used to identify increased levels of hyaluronan...
July 8, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28688145/therapeutic-concentrations-of-digitoxin-inhibit-endothelial-focal-adhesion-kinase-and-angiogenesis-induced-by-diverse-growth-factors
#13
Annalisa Trenti, Elisabetta Zulato, Lorenza Pasqualini, Stefano Indraccolo, Chiara Bolego, Lucia Trevisi
BACKGROUND AND PURPOSE: Cardiac glycosides are Na(+) /K(+) -ATPases inhibitors used to treat congestive heart failure and cardiac arrhythmias. Epidemiological studies indicate that patients on digitalis therapy are more protected from cancer. Evidence of a selective cytotoxicity against cancer cells has suggested their potential use as anticancer drugs. The effect on angiogenesis of clinically used cardiac glycosides has not been extensively explored. EXPERIMENTAL APPROACH: We studied the effect of digoxin, digitoxin and ouabain on early events of the angiogenic process in human umbilical vein endothelial cells (HUVEC)...
July 8, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28688122/diminazene-aceturate-prevents-type-1-diabetic-nephropathy-through-increasing-glomerular-ace2-and-at2-receptor-expression
#14
Santosh Kumar Goru, Almesh Kadakol, Vajir Malek, Anuradha Pandey, Nisha Sharma, Anil Bhanudas Gaikwad
BACKGROUND AND PURPOSE: Angiotensin converting enzyme 2 (ACE2) shows its protective actions through degrading Ang II. ACE2 activity and its expression was found to be reduced in glomeruli of diabetic patients as well as in animal models of diabetes. Several recent studies have also showed the potential role of recombinant ACE2 administration in preventing diabetic nephropathy (DN). Hence, we hypothesized that ACE2 activator, diminazene aceturate (DIZE) may be beneficial in preventing DN...
July 8, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28685814/drug-repurposing-screens-and-synergistic-drug-combinations-for-infectious-diseases
#15
REVIEW
Wei Zheng, Wei Sun, Anton Simeonov
Infectious diseases account for nearly one fifth of the worldwide death toll every year. Continuous increase of drug-resistant pathogens is a big challenge for treatment of infectious diseases. In addition, emerging outbreaks of infections and new pathogens are potential threats to public health. Lack of effective treatments for drug-resistant bacteria and recent outbreaks of Ebola and Zika viral infections have become a global public health concern. The number of newly approved antibiotics has decreased significantly in the last two decades compared to previous decades...
July 7, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28681507/correlation-between-herg-channel-inhibition-and-action-potential-prolongation
#16
P Saxena, M P Hortigon-Vinagre, S Beyl, I Baburin, S Andranovits, S M Iqbal, A Costa, A P IJzerman, P Kügler, E Timin, G L Smith, S Hering
BACKGROUND AND PURPOSE: hERG (Kv11.1) channel inhibition is a widely accepted predictor of cardiac arrhythmia. hERG channel inhibition alone is often insufficient to predict pro-arrhythmic drug effects. This study used a library of dofetilide derivatives to investigate the relationship between standard measures of hERG current block in an expression system and changes in action potential duration (APD) in hiPSC-CMs. The interference from accompanying block of Cav1.2 and Nav1.5 channels was investigated along with an in-silico action potential (AP) model...
July 6, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28677901/big-conductance-calcium-activated-potassium-channel-openers-control-spasticity-without-sedation
#17
David Baker, Gareth Pryce, Cristina Visintin, Sofia Sisay, Alexander I Bondarenko, W S Vanessa Ho, Samuel J Jackson, Thomas E Williams, Sarah Al-Izki, Ioanna Sevastou, Masahiro Okuyama, Wolfgang F Graier, Lesley A Stevenson, Carolyn Tanner, Ruth Ross, Roger G Pertwee, Christopher M Henstridge, Andrew J Irving, Jesse Schulman, Keith Powell, Mark D Baker, Gavin Giovannoni, David L Selwood
BACKGROUND & PURPOSE: The initial aim was to generate cannabinoid agents that control spasticity, occurring as a consequence of multiple sclerosis, whilst avoiding the sedative, side-effect-potential associated with cannabis. (R,Z)-3-(6-(dimethylamino)-6-oxohex-1-enyl)-N-(1-hydroxypropan-2-yl)benzamide (VSN16R) was synthesized as an anandamide (endocannabinoid) analogue in an anti-metabolite approach to identify drug-like agents to target spasticity. EXPERIMENTAL APPROACH: Following the initial chemistry, a variety of biochemical, pharmacological and electrophysiological approaches, using isolated cells, tissue-based assays and in vivo animal models, were used to demonstrate: activity, efficacy, pharmacokinetics and mechanism of action of the molecule...
July 5, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28675470/brain-serotoninergic-nervous-system-is-involved-in-bombesin-induced-frequent-urination-through-brain-5-ht7-receptors-in-rats
#18
Takahiro Shimizu, Shogo Shimizu, Naoki Wada, Shun Takai, Nobutaka Shimizu, Youichirou Higashi, Katsumi Kadekawa, Tsuyoshi Majima, Motoaki Saito, Naoki Yoshimura
BACKGROUND AND PURPOSE: Psychological stress exacerbates symptoms of urinary bladder dysfunction; however, underlying brain mechanisms are unclear. We reported that centrally administered bombesin, a stress-related neuropeptide, facilitates the rat micturition reflex. Brain bombesin-like peptides modulate the serotoninergic nervous system activity under stress conditions; therefore, we examined whether brain serotonin is involved in bombesin-induced frequent urination in urethane-anesthetized (0...
July 4, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28675448/mpges-1-inhibitor-reduces-human-vascular-tone-by-increasing-pgi2-a-safer-alternative-to-coxibs
#19
Gulsev Ozen, Ingrid Gomez, Armond Daci, Catherine Deschildre, Lilia Boubaya, Onder Teskin, B Sonmez Uydeş-Doğan, Per-Johan Jakobsson, Dan Longrois, Gokce Topal, Xavier Norel
BACKGROUND AND PURPOSE: The side effects of cyclooxygenase-2 (COX-2) inhibitors (COXIBs) on the cardiovascular system could be associated with a reduced prostaglandin (PG) I2 synthesis. Microsomal prostaglandin E synthase-1 (mPGES-1) catalyzes the formation of PGE2 from COX-derived PGH2 . This enzyme is induced under inflammatory conditions and constitutes an attractive target for novel anti-inflammatory drugs. However, it is not known whether mPGES-1 inhibitors could be devoid of cardiovascular side effects...
July 3, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28675424/predicting-qrs-and-pr-interval-prolongations-in-humans-using-nonclinical-data
#20
L Bergenholm, J Parkinson, J Mettetal, N D Evans, M J Chappell, T Collins
BACKGROUND AND PURPOSE: Risk of cardiac conduction slowing (QRS/PR prolongations) is assessed prior to clinical trials using in vitro and in vivo studies. Understanding the quantitative translation of these studies to the clinical situation enables improved risk assessment in the nonclinical phase. EXPERIMENTAL APPROACH: Four compounds that prolong QRS and/or PR (AZD1305, flecainide, quinidine and verapamil) were characterised using in vitro (sodium/calcium channels), in vivo (guinea pigs/dogs) and clinical data...
July 3, 2017: British Journal of Pharmacology
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