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British Journal of Pharmacology

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https://www.readbyqxmd.com/read/28812311/nad-replenishment-with-nicotinamide-mononucleotide-protects-blood-brain-barrier-integrity-and-attenuates-delayed-tpa-induced-haemorrhagic-transformation-after-cerebral-ischemia
#1
Chun-Chun Wei, Yuan-Yuan Kong, Xia-Hua, Guo-Qiang Li, Si-Li Zheng, Ming-He Cheng, Pei Wang, Chao-Yu Miao
BACKGROUND AND PURPOSE: Tissue plasminogen activator (tPA) is the only approved pharmacological therapy for acute brain ischemia; however, a major limitation of tPA is the haemorrhagic transformation followed by tPA treatment. Here, we determine whether nicotinamide mononucleotide (NMN), a key intermediate of nicotinamide adenine dinucleotide biosynthesis, would affect tPA-induced haemorrhagic transformation. EXPERIMENTAL APPROACH: Middle cerebral artery occlusion (MCAO) was achieved in CD1 mice by introducing a filament to the left MCA for 5 hours...
August 15, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28810065/olodaterol-shows-anti-fibrotic-efficacy-in-in-vitro-and-in-vivo-models-of-pulmonary-fibrosis
#2
Franziska Elena Herrmann, Lutz Wollin, Johannes Wirth, Florian Gantner, Bärbel Lämmle, Eva Wex
BACKGROUND AND PURPOSE: Idiopathic pulmonary fibrosis (IPF) is a fatal respiratory disease characterized by excessive fibroblast activation ultimately leading to scarring of the lungs. Although, the activation of β2 -adrenergic receptors (β2 -AR) has been shown to inhibit pro-fibrotic events primarily in cell lines, the role of β2 -AR agonism has not yet been fully characterized. The aim of our study was to explore the anti-fibrotic activity of the long-acting β2 -AR-agonist olodaterol in primary human lung fibroblasts, and in murine models of pulmonary fibrosis...
August 15, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28806493/olaparib-a-clinically-used-poly-adp-ribose-polymerase-inhibitor-protects-against-oxidant-induced-cardiac-myocyte-death-in-vitro-and-improves-cardiac-contractility-during-early-phase-after-heart-transplantation-in-a-rat-model-in-vivo
#3
Sevil Korkmaz-Icöz, Bartosz Szczesny, Michela Marcatti, Shiliang Li, Mihály Ruppert, Felix Lasitschka, Sivakkanan Loganathan, Csaba Szabo, Gábor Szabó
BACKGROUND AND PURPOSE: Olaparib, rucaparib and niraparib, potent inhibitors of poly(ADP-ribose) polymerase (PARP) have recently been approved for human use for oncological indications. Considering the previously demonstrated role of PARP in various forms of acute and chronic myocardial injury, we tested the effect of olaparib in in-vitro models of oxidative stress in cardiomyocytes, and in an in-vivo model of cardiac transplantation. EXPERIMENTAL APPROACH: H9c2-embryonic rat heart-derived myoblasts pretreated with vehicle or olaparib (10μM) were challenged with either hydrogen-peroxide (H2 O2 ) or with glucose-oxidase (GOx, which generates H2 O2 in the tissue culture medium)...
August 14, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28806488/serotonergic-5-ht2b-receptors-in-mitral-valvulopathy-bone-marrow-mobilization-of-endothelial-progenitors
#4
Estelle Ayme-Dietrich, Roland Lawson, Francine Côté, Claudia de Tapia, Sylvia Da Silva, Claudine Ebel, Béatrice Hechler, Christian Gachet, Jérome Guyonnet, Hélène Rouillard, Jordane Stoltz, Emily Quentin, Sophie Banas, François Daubeuf, Nelly Frossard, Bernard Gasser, Jean-Philippe Mazzucotelli, Olivier Hermine, Luc Maroteaux, Laurent Monassier
BACKGROUND: Valvular heart disease is highly prevalent in industrialized countries. Chronic use of anorexigens, amphetamine or ergot derivatives targeting the serotonin system has been associated with valvular heart disease. PURPOSE AND EXPERIMENTAL APPROACH: Here, we investigated the contribution of serotonin receptors in a mouse model of valve degeneration induced by nordexfenfluramine, the main metabolite of the anorexigens dexfenfluramine and benfluorex. KEY RESULTS: Chronically activated 5-HT2B receptors by nordexfenfluramine in mice mimicked early steps of mitral valve remodelling attested by increased valve thickness, and cell density in a thick extracellular matrix...
August 14, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28805944/suppression-of-acute-and-anticipatory-nausea-by-peripherally-restricted-faah-inhibitor-in-animal-models-role-of-ppar%C3%AE-and-cb1-receptors
#5
Erin M Rock, Guillermo Moreno-Sanz, Cheryl L Limebeer, Gavin N Petrie, Roberto Angelini, Daniele Piomelli, Linda A Parker
To evaluate the ability of the peripherally restricted fatty acid amide hydrolase (FAAH) inhibitor, URB937 (cyclohexylcarbamic acid 3'-carbamoyl-6-hydroxybiphenyl-3-yl ester) to suppress acute and anticipatory nausea in rats, and to examine the pharmacological mechanism of such an effect. EXPERIMENTAL APPROACH: We investigated the potential of URB937 to reduce the establishment of lithium chloride (LiCl)-induced conditioned gaping (a model of acute nausea) and to reduce the expression of contextually elicited conditioned gaping (a model of anticipatory nausea) in rats...
August 14, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28800680/pharmacological-inhibition-of-fsgs-related-trpc6-gain-of-function-mutants-by-semisynthetic-larixol-derived-compounds
#6
Nicole Urban, Sonja Neuser, Anika Hentschel, Sebastian Köhling, Jörg Rademann, Michael Schaefer
BACKGROUND AND PURPOSE: Gain of function mutations in TRPC6 can cause autosomal dominant forms of focal segmental glomerulosclerosis (FSGS). Validated inhibitors of TRPC6 that are biologically active on FSGS-related TRPC6 mutants are eagerly sought. EXPERIMENTAL APPROACH: We synthesized new TRPC6-inhibiting modulators from larixol, a resiniferous constituent of Larix decidua, and tested the potency and selectivity in cell lines stably expressing various TRP channel isoforms...
August 11, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28800679/the-short-chain-fatty-acid-sodium-butyrate-exerts-protective-effects-through-ameliorating-blood-milk-barrier-disruption-and-modulating-inflammatory-response-in-lipopolysaccharide-induced-mastitis-model
#7
Jing-Jing Wang, Zheng-Kai Wei, Xu Zhang, Ya-Nan Wang, Yun-He Fu, Zheng-Tao Yang
BACKGROUND AND PURPOSE: Short-chain fatty acids (SCFAs) are fermentation end products produced by the gut bacteria,which have been shown to ameliorate inflammatory bowel diseases (IBD) and allergic asthma. However, the mechanism involved remains largely unknown. Here, we investigate the protective effects and mechanisms of sodium butyrate (SB) on lipopolysaccharide (LPS)-induced mastitis model. EXPERIMENTAL APPROACH: Effects of increasing doses of SB on blood-milk barrier function and inflammation are studied in LPS-induced mastitis...
August 11, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28800677/levothyroxine-enhances-glucose-clearance-and-blunts-the-onset-of-experimental-type-1-diabetes-mellitus-in-mice
#8
Livia López-Noriega, Nadia Cobo-Vuilleumier, Álvaro Jesús Narbona-Pérez, Juan Luis Araujo-Garrido, Petra Isabel Lorenzo, José Manuel Mellado-Gil, José Carlos Moreno, Benoit R Gauthier, Alejandro Martín-Montalvo
BACKGROUND AND PURPOSE: Thyroid hormones induce several changes in whole body metabolism that are known to improve metabolic homeostasis. However, adverse side effects have prevented its use in the clinic. In view of the promising effects of thyroid hormones, we investigated the effects of levothyroxine supplementation in glucose. EXPERIMENTAL APPROACH: C57BL/6 mice were treated with levothyroxine from birth to 24 weeks of age, when mice were euthanized. The effects of levothyroxine supplementation on metabolic health were determined...
August 11, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28800675/discovery-and-pharmacological-characterisation-of-a-novel-series-of-highly-selective-inhibitors-of-cyclin-dependent-kinases-4-and-6-as-anticancer-agents
#9
Solomon Tadesse, Laychiluh Bantie, Khamis Tomusange, Mingfeng Yu, Saiful Islam, Nataliya Bykovska, Benjamin Noll, Ge Zhu, Peng Li, Frankie Lam, Malika Kumarasiri, Robert Milne, Shudong Wang
BACKGROUND AND PURPOSE: Cyclin D dependent kinases 4 and 6 (CDK4/6) are crucial regulators of the G1 to S phase transition of the cell cycle, and are actively pursued as therapeutic targets in cancer targets. We sought to discover a novel series of orally bioavailable, and highly selective small molecule inhibitors of CDK4/6. EXPERIMENTAL APPROACH: The discovery of pharmacological inhibitors and optimisation for potency, selectivity and drug properties were achieved by iterative chemical synthesis, biochemical screening against a panel of kinases, cell-based assays measuring cellular viability, cell cycle distribution, induction of apoptosis, and the level of retinoblastoma tumour suppressor protein (Rb) phosphorylation and E2 factor (E2F) regulated gene expression, and in vitro biopharmaceutical and in vivo pharmacokinetic profiling...
August 11, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28800673/m-type-k-channels-in-peripheral-nociceptive-pathways
#10
REVIEW
Xiaona Du, Haixia Gao, David Jaffe, Hailin Zhang, Nikita Gamper
Pathological pain is a hyperexcitability disorder. Since the excitability of a neuron is set and controlled by a complement of ion channels it expresses, in order to understand and treat pain we need to develop a mechanistic insight into the key ion channels controlling excitability within the mammalian pain pathways, and how these ion channels are regulated and modulated in various physiological and pathophysiological settings. In this review we will discuss the emerging data on the expression in pain pathways, functional role and modulation of a family of voltage-gated K(+) channels called 'M channels' (KCNQ, Kv7)...
August 11, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28800377/antidote-to-cannabinoid-intoxication-inverse-cannabinoid-receptor-one-cb1-agonism-by-n-piperidin-1-yl-5-4-iodophenyl-1-2-4-dichlorophenyl-4-methyl-1h-pyrazole-3-carboxamidse-am251-reverses-the-hypothermic-effects-of-cannabinoid-receptor-one-agonism-by-1-naphthalenyl
#11
Gareth Pryce, David Baker
BACKGROUND & PURPOSE: Cannabis is a recreational drug leading to intoxication, due to cannabinoid receptor one (CB1 ) stimulation. However, more recently herbs mixed with synthetic cannabinoids sometimes known as "Spice" and "Black Mamba" have been increasing used and their high CB1 receptor affinity means not only marked intoxication, but life-threatening complications and an increasing number of deaths. Whilst many studies have indicated that prophylactic CB1 receptor antagonism can block cannabimimetic effects in animals and humans...
August 11, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28782244/using-the-affective-bias-test-to-predict-drug-induced-negative-affect-implications-for-drug-safety
#12
S A Stuart, C M Wood, E S J Robinson
BACKGROUND AND PURPOSE: Predicting the risk of drug-induced adverse psychiatric effects is important but currently not possible in non-human species. This study has investigated whether the affective bias test (ABT) could provide a preclinical method with translational and predictive validity. EXPERIMENTAL APPROACH: The ABT is a bowl-digging task which quantifies biases associated with learning and memory. Rats encounter independent learning experiences, on separate days, under either acute manipulations (e...
August 7, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28771708/metabolic-profiling-of-murine-plasma-reveals-eicosapentaenoic-acid-metabolites-protecting-against-endothelial-activation-and-atherosclerosis
#13
Yajin Liu, Xuan Fang, Xu Zhang, Jing Huang, Jinlong He, Liyuan Peng, Chenji Ye, Yingmei Wang, Fengxia Xue, Ding Ai, Dan Li, Yi Zhu
BACKGROUND AND PURPOSE: Atherosclerosis results from a maladaptive inflammatory response initiated by the intramural retention of LDL in susceptible areas of the arterial vasculature. ω-3 polyunsaturated fatty acids (ω-3) have protective effects in atherosclerosis; however, the molecular mechanism is still largely unknown. The present study used a metabolomic approach to reveal the atheroprotective metabolites of ω-3 and investigate the underlying mechanisms. EXPERIMENTAL APPROACH: We evaluated the development of atherosclerosis in LDL-receptor-deficient mice (LDLR(-/-) ) fed a Western-type diet (WTD) plus ω-3 and also LDLR(-/-) and fat-1 transgenic (LDLR(-/-) -fat-1(tg) ) mice fed a WTD...
August 3, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28771697/effects-of-centrally-administered-endocannabinoids-and-opioids-on-orofacial-pain-perception-in-rats
#14
Marek Zubrzycki, Anna Janecka, Andreas Liebold, Mechthild Ziegler, Maria Zubrzycka
BACKGROUND AND PURPOSE: Endocannabinoids and opioids play a vital role in mediating pain-induced analgesia. The specific effects of these compounds within orofacial region are largely unknown. In this study we tried to determine whether the increase of cannabinoid and opioid concentration in cerebrospinal fluid affects impulse transmission between the motor centers localized in the vicinity of the third and fourth cerebral ventricles. EXPERIMENTAL APPROACH: The study objectives were realized on rats using the method allowing to record the amplitude of evoked tongue jerks (ETJ) in response to noxious tooth pulp stimulation...
August 3, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28768052/cardioprotective-effects-of-5-hydroxymethylfurfural-mediated-by-inhibition-of-l-type-ca-2-current
#15
G Wölkart, A Schrammel, C N Koyani, S Scherübel, K Zorn-Pauly, E Malle, B Pelzmann, M Andrä, A Ortner, B Mayer
BACKGROUND AND PURPOSE: The antioxidant 5-hydroxymethylfurfural (5-HMF) exerts documented beneficial effects in several experimental pathologies and is currently tested as antisickling drug in clinical trials. In the present study we examined the cardiovascular effects of 5-HMF and elucidated the mode of action of the drug. EXPERIMENTAL APPROACH: The cardiovascular effects of 5-HMF were studied with precontracted porcine coronary arteries and isolated normoxic perfused rat hearts...
August 2, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28768046/carbon-monoxide-released-from-its-pharmacological-donor-tricarbonyldichlororuthenium-ii-dimer-corm-2-accelerates-the-healing-of-pre-existing-gastric-ulcers
#16
Magierowski Marcin, Magierowska Katarzyna, Hubalewska-Mazgaj Magdalena, Sliwowski Zbigniew, Ginter Grzegorz, Pajdo Robert, Chmura Anna, Kwiecien Slawomir, Brzozowski Tomasz
BACKGROUND AND PURPOSE: Carbon monoxide (CO), gaseous mediator produced by heme oxygenases (HO), has been shown to prevent stress-, ethanol-, aspirin- or alendronate-induced gastric damage, however, its role in the gastric ulcer healing has not been fully explained. We investigated whether CO released from tricarbonyldichlororuthenium (II) dimer (CORM-2) can affect gastric ulcer healing and determined mechanisms involved in healing action of this compound. EXPERIMENTAL APPROACH: Gastric ulcers were induced in Wistar rats by serosal application of acetic acid...
August 2, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28755521/antibiotic-induced-microbiota-dysbiosis-impairs-neuromuscular-function-in-juvenile-mice
#17
Valentina Caputi, Ilaria Marsilio, Viviana Filpa, Silvia Cerantola, Genny Orso, Michela Bistoletti, Nicola Paccagnella, Sara De Martin, Monica Montopoli, Stefano Dall'Acqua, Francesca Crema, Iole-Maria Di Gangi, Francesca Galuppini, Isabella Lante, Sara Bogialli, Massimo Rugge, Patrizia Debetto, Cristina Giaroni, Maria Cecilia Giron
BACKGROUND AND PURPOSE: Gut microbiota is essential for the development of the gastrointestinal system, including the enteric nervous system (ENS). Early life perturbations of gut microbiota can potentially impact neurodevelopment leading to functional bowel disorders later in life. We examined the hypothesis that gut dysbiosis impairs ENS structural and functional integrity leading to gut dysmotility in juvenile mice. EXPERIMENTAL APPROACH: To induce gut dysbiosis broad-spectrum antibiotics were administered by gavage to juvenile male C57Bl/6 mice for 14 days...
July 29, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28752891/inhibition-of-nuclear-wnt-signaling-challenges-of-an-elusive-target-for-cancer-therapy
#18
REVIEW
Yung Lyou, Amber N Habowski, George T Chen, Marian L Waterman
The highly conserved Wnt signaling pathway plays an important role in embryonic development and disease pathogenesis, most notably cancer. The "canonical," or β-catenin-dependent Wnt signal initiates at the cell plasma membrane with the binding of Wnt proteins to Frizzled:LRP5/LRP6 receptor complexes, and is mediated by the translocation of the transcription co-activator protein, β-catenin, into the nucleus. β-catenin then forms a complex with TCF/LEF transcription factors to regulate multiple gene programs...
July 28, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28750135/ameliorative-effect-of-chlorpromazine-hydrochloride-on-visceral-hypersensitivity-in-rats-possible-involvement-of-5-ht2a-receptor
#19
Teita Asano, Ken-Ichiro Tanaka, Arisa Tada, Hikaru Shimamura, Rikako Tanaka, Hiroki Maruoka, Tohru Mizushima, Mitsuko Takenaga
BACKGROUND AND PURPOSE: Visceral hypersensitivity is responsible for pathogenesis of irritable bowel syndrome (IBS). Therefore, its prevention can help avoid abdominal pain and discomfort in IBS. To find candidate drugs for visceral hypersensitivity, we screened existing medicines for their ability to prevent visceral sensitivity induced by colorectal distension (CRD) in rats and identified chlorpromazine, a typical antipsychotic drug, as a candidate compound. In this study, we investigated the effect of chlorpromazine on visceral hypersensitivity...
July 27, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28749537/sodium-channels-and-pain-from-toxins-to-therapies
#20
REVIEW
Fernanda C Cardoso, Richard J Lewis
Voltage-gated sodium channels (NaV ) are essential to initiation and propagation of action potentials that critically influence our ability to respond to a diverse range of stimuli. Physiological and pharmacological studies have linked abnormal function of Nav channels to many human disorders, including chronic neuropathic pain. These findings, along with the description of the functional properties and expression pattern of NaV channels subtypes, are helping to uncover subtype specific roles in acute and chronic pain, and revealing potential opportunities to target these with selective inhibitors...
July 27, 2017: British Journal of Pharmacology
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