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British Journal of Pharmacology

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https://www.readbyqxmd.com/read/29682743/the-selective-mineralcorticoid-receptor-mr-antagonist-eplerenon-prevents-decompensation-of-liver-cirrhosis
#1
Barbara Schreier, Anja Wolf, Stefanie Hammer, Sabine Pohl, Sigrid Mildenberger, Sindy Rabe, Michael Gekle, Alexander Zipprich
BACKGROUND & AIMS: The MR contributes to fibrosis in various tissues and MR antagonists, like eplerenone, are used to prevent fibrosis. The role of MR antagonists for hepatic fibrosis and cirrhosis is unknown. Here, we investigated the role of MR and eplerenone in cirrhosis development. METHODS: Liver fibrosis (5 weeks), cirrhosis without (8w) and with ascites (12w) were induced by CCl4 in rats and comprehensively analyzed. In addition the effect of eplerenone (MR antagonist) on the development of cirrhosis with ascites was assessed...
April 22, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29679953/antinociception-by-the-anti-oxidized-phospholipid-antibody-e06
#2
Milad Mohammadi, Beatrice Oehler, Jan Kloka, Corinna Martin, Alexander Brack, Robert Blum, Heike L Rittner
BACKGROUND AND PURPOSE: Reactive oxygen species (ROS) and their downstream molecules such as oxidized phospholipids (OxPL) and 4-hydroxynonenal (4-HNE) activate transient receptor potential ankyrin 1 (TRPA1) and vanilloid 1 (TRPV1) ion channels in vivo and in vitro shaping thermal and mechanical hypersensitivity in inflammatory pain. E06/T15 is a monoclonal autoantibody against oxidized phosphatidylcholine (OxPC) used in diagnostics in arteriosclerosis. Recently, we provided evidence that E06 also ameliorates inflammatory pain...
April 21, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29679507/novel-inhibitors-of-the-cellular-ras-components-poricoic-acids-target-smad3-phosphorylation-and-wnt-%C3%AE-catenin-pathway-against-renal-fibrosis
#3
Ming Wang, Dan-Qian Chen, Lin Chen, Gang Cao, Hui Zhao, Dan Liu, Nosratola D Vaziri, Yan Guo, Ying-Yong Zhao
BACKGROUND AND PURPOSE: Tubulo-interstitial fibrosis is the final pathway of progression of CKD to ESRD. Renin-angiotensin system (RAS) plays a major role in CKD progression. Present study demonstrates efficacy of the novel RAS inhibitors isolated from Poria cocos against renal fibrosis. EXPERIMENTAL APPROACH: The effect of three novel tetracyclic triterpenoid compounds poricoic acid ZC (PZC), poricoic acid ZD (PZD) and poricoic acid ZE (PZE) was investigated on TGF-β1- and angiotensin II (AngII)-treated HK-2 cells and UUO mice...
April 21, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29679502/new-paradigms-in-adenosine-receptor-pharmacology-allostery-oligomerization-and-biased-agonism
#4
REVIEW
Elizabeth A Vecchio, Jo-Anne Baltos, Anh T N Nguyen, Arthur Christopoulos, Paul J White, Lauren T May
Adenosine receptors (ARs) are a family of G protein-coupled receptors (GPCRs) containing four subtypes (A1 AR, A2A AR, A2B AR and A3 AR), all of which bind the ubiquitous nucleoside adenosine. ARs play an important role in physiology and pathophysiology and therefore represent attractive drug targets for a range of conditions. The theoretical framework surrounding AR drug action now extends beyond the notion of prototypical agonism and antagonism to encompass more complex pharmacological concepts. New paradigms include allostery, whereby ligands bind a topographically distinct receptor site from that of the endogenous agonist, homomeric or heteromeric interactions across receptor oligomers and biased agonism; that is, ligand-dependent differential intracellular signalling...
April 21, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29679493/ppars-and-pain
#5
REVIEW
Bright N Okine, Jessica C Gaspar, David P Finn
Chronic pain is a common cause of disability worldwide and remains a global health and socioeconomic challenge. Current analgesics are either ineffective in a significant proportion of patients with chronic pain, or associated with significant adverse side effects. The peroxisome proliferator-activated receptors (PPARs), a family of nuclear hormone transcription factors, have emerged as important modulators of pain in preclinical studies and therefore a potential therapeutic target for the treatment of pain...
April 21, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29679485/identification-and-structure-elucidation-of-the-proresolving-mediators-provides-novel-leads-for-resolution-pharmacology
#6
REVIEW
Jesmond Dalli, Charles N Serhan
Inflammatory diseases are a major socioeconomic burden, with the incidence of such conditions on the rise, especially in western societies. For decades, the primary treatment paradigm for many of these conditions was to develop drugs that inhibit or antagonize the production and biological actions of molecules that were thought to be the culprits in propagating disease, these include cytokines and eicosanoids. This approach is effective in controlling disease propagation; however, long-term exposure to these anti-inflammatories is also associated with many side effects, some of which severe, including immune-suppression...
April 21, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29679484/the-role-of-autoimmune-reactivity-induced-by-heat-shock-protein-70-in-the-pathogenesis-of-essential-hypertension
#7
REVIEW
Bernardo Rodriguez-Iturbe, Miguel A Lanaspa, Richard J Johnson
Autoimmunity is increasingly recognized as having a central role in essential hypertension. Heat shock proteins are immunodominant molecules with high interspecies homology and autoimmune reactivity directed against HSP70 may play a role in the pathogenesis of hypertension. Autoimmunity to HSP70 may result from molecular mimicry between human HSP and bacterial HSP, or alternatively, as a response to HSP70-peptide complexes generated during cellular stress and delivered to the major histocompatibility complex in antigen presenting cells...
April 21, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29679483/prostaglandin-fp-receptor-antagonists-discovery-pharmacological-characterization-and-therapeutic-utility
#8
REVIEW
Najam A Sharif, Peter G Klimko
In contrast to the availability of potent and selective antagonists of several prostaglandin (PG) receptor types (including DP1 , DP2 , EP, and TP receptors), there has been a paucity of well-characterized, selective FP-receptor antagonists. The earliest ones included dimethyl amide and dimethyl amine derivatives of PGF2α , but these have failed to gain prominence. The fluorinated PGF2α analogs, AL-8810 and AL-3138, were subsequently discovered as competitive and non-competitive FP-receptor antagonists, respectively...
April 21, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29671869/regulation-of-vascular-permeability-in-anaphylaxis
#9
REVIEW
Tatsuro Nakamura, Takahisa Murata
Anaphylaxis is a life-threatening type I allergic reaction. Antigen-antibody complexes lead mast cells, basophils, and neutrophils to release large amounts of histamine and/or platelet activating factor (PAF). These mediators induce hypotension and vascular hyperpermeability and subsequent anaphylaxis dependent on the endothelial production of NO. Here, we have summarised previous studies reporting the mechanisms underlying the functional changes within the vasculature, specifically focusing on vascular permeability triggered by histamine or PAF...
April 19, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29669174/inorganic-hydrogen-polysulfides-chemistry-chemical-biology-and-detection
#10
REVIEW
Heng Liu, Miles N Radford, Chun-Tao Yang, Wei Chen, Ming Xian
Recent studies suggest inorganic hydrogen polysulfides (H2 Sn , n≥2) play important regulatory roles in redox biology. Modulation of their cellular levels could have potential therapeutic value. This review article focuses on our current understanding of the biosynthesis, biofunctions, fundamental physical/chemical properties, detection methods, and delivery techniques of H2 Sn .
April 18, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29669171/prostaglandin-analogues-and-nitric-oxide-contribution-in-the-treatment-of-ocular-hypertension-and-glaucoma
#11
REVIEW
Francesco Impagnatiello, Elena Bastia, Nicoletta Almirante, Stefania Brambilla, Brigitte Duquesroix, Angela C Kothe, Michael V W Bergamini
In patients with ocular hypertension or glaucoma all treatments aim at lowering intraocular pressure (IOP) by modulating aqueous humor (AH) production and/or uveoscleral and trabecular meshwork /Schlemm's canal AH drainage. Prostaglandin (PG) analogues are considered the 'gold standard', and are the most frequently used IOP-lowering agents. Recent data support an important role of nitric oxide (NO) in regulating IOP. Thus novel PG analogues carrying a NO-donating moiety were recently advanced. Latanoprostene bunod (LBN) and NCX 470, respectively a NO-donating derivative of latanoprost and bimatoprost, are examples of such compounds...
April 18, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29669164/galantamine-is-not-a-positive-allosteric-modulator-of-human-%C3%AE-4%C3%AE-2-or-%C3%AE-7-nicotinic-acetylcholine-receptors
#12
Natalia M Kowal, Philip K Ahring, Vivian W Y Liao, Dinesh C Indurti, Benjamin S Harvey, Susan M O'Connor, Mary Chebib, Elin S Olafsdottir, Thomas Balle
BACKGROUND AND PURPOSE: The alkaloid galantamine was originally isolated from the green snowdrop Galanthus woronowii and is currently marketed as a drug for treatment of mild to moderate dementia in Alzheimer's disease patients. In addition to a well-documented proficiency of inhibiting the acetylcholinesterase enzyme, galantamine has been reported to increase neuronal nicotinic acetylcholine (nACh) receptor function by acting as a positive allosteric modulator. Yet, there remains controversy regarding these findings in the literature...
April 18, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29667180/pde5-inhibitors-pharmacology-and-clinical-applications-20-years-after-sildenafil-discovery
#13
REVIEW
K-E Andersson
The discovery of the nitric oxide/cyclic cGMP pathway was the basis for our understanding of many normal physiological functions and the pathophysiology of several diseases. Since the discovery and introduction of sildenafil, inhibitors of phosphodiesterase isoenzymes type 5 (PDE5) have been first-line therapy for erectile dysfunction (ED). The success of sildenafil in the treatment of ED stimulated research in the field of PDE5 inhibition and led to many new applications, such as treatment of lower urinary symptoms (LUTS), and pulmonary arterial hypertension, which are now approved indications...
April 17, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29665040/discovery-characterization-and-clinical-utility-of-prostaglandin-agonists-for-the-treatment-of-glaucoma
#14
REVIEW
Peter G Klimko, Najam A Sharif
Topical ophthalmic formulations of analogs of the endogenous arachidonic acid cyclooxygenase metabolite, prostaglandin F2α (PGF2α ), are the standard of care for treating the blinding disease glaucoma. These are the most potent and efficacious medical therapies for lowering intraocular pressure (IOP), the most important identified risk factor for disease progression. They have few side-effects and offer the convenience of once-a-day dosing. It was initially believed that endogenous PGs raised IOP and caused substantial ocular surface adverse effects...
April 17, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29663308/insight-on-the-impact-of-endocannabinoid-system-in-cancer-a-review
#15
REVIEW
Ana Isabel Fraguas-Sánchez, Cristina Martín-Sabroso, Ana Isabel Torres-Suárez
In the last decades, the endocannabinoid system has attracted a great interest in medicine and cancer disease is probably one of its most promising therapeutic areas. On the one hand, endocannabinoid system expression has been found altered in numerous types of tumours compared to healthy tissue, and this aberrant expression has been related to cancer prognosis and disease outcome, suggesting a role of this system in tumour growth and progression that depends on cancer type. On the other hand, it has been reported that cannabinoids exert an anticancer activity by inhibiting the proliferation, migration and/or invasion of cancer cells; and also tumour angiogenesis...
April 16, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29624642/cannabidiol-regulates-behavioural-alterations-and-gene-expression-changes-induced-by-spontaneous-cannabinoid-withdrawal
#16
Francisco Navarrete, Auxiliadora Aracil-Fernández, Jorge Manzanares
BACKGROUND AND PURPOSE: Cannabidiol (CBD) represents a promising therapeutic tool for treating cannabis use disorder (CUD). This study aimed to evaluate the effects of CBD on the behavioural and gene expression alterations induced by spontaneous cannabinoid withdrawal. EXPERIMENTAL APPROACH: Spontaneous cannabinoid withdrawal was evaluated 12 h after cessation of CP-55,940 treatment (0.5 mg·kg-1 /12 h; intraperitoneally (i.p.); 7 days) in C57BL/6J mice. The effects of CBD (5, 10 and 20 mg·kg-1 ; i...
April 6, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29582428/selective-late-sodium-current-inhibitor-gs-458967-suppresses-torsades-de-pointes-by-mostly-affecting-perpetuation-but-not-initiation-of-the-arrhythmia
#17
Alexandre Bossu, Marien J C Houtman, Veronique M F Meijborg, Rosanne Varkevisser, Henriette D M Beekman, Albert Dunnink, Jacques M T de Bakker, Nevena Mollova, Sridharan Rajamani, Luiz Belardinelli, Marcel A G van der Heyden, Marc A Vos
BACKGROUND AND PURPOSE: Enhanced late sodium current (late INa ) in heart failure and long QT syndrome type 3 is proarrhythmic. GS-458967 (GS967) is a selective and potent late INa inhibitor. This study aimed to evaluate the antiarrhythmic effect of late INa inhibition by GS967 in the chronic atrioventricular block (CAVB) dog model sensitive to Torsade de Pointes arrhythmias (TdP) and to elucidate its electrophysiological mode of action in vivo and in vitro. METHODS - RESULTS: GS967 (IC50 for late INa ~ 200 nM) markedly shortened action potential duration of canine ventricular cardiomyocytes and repolarization parameters in vivo in sinus rhythm (SR, n=10) dogs, in a concentration-dependent manner...
March 27, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29582417/dissecting-the-spinal-nop-receptor-distribution-under-a-chronic-pain-model-using-nop-egfp-knock-in-mice
#18
Akihiko Ozawa, Gloria Brunori, Andrea Cippitelli, Nicholas Toll, Jennifer Schoch, Brigitte L Kieffer, Lawrence Toll
BACKGROUND AND PURPOSE: The Nociceptin/orphanin FQ Opioid Peptide (NOP) receptor system plays a significant role in the regulation of pain, and functions differently in the spinal cord and brain. The mechanism by which the NOP receptor agonists regulate pain transmission in these regions is not clearly understood. Here we investigate the peripheral and spinal NOP receptor distribution and antinociceptive effects of intrathecally (i.t) administered nociceptin/orphanin FQ (N/OFQ) under chronic neuropathic pain state...
March 26, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29582416/body-fat-reduction-without-cardiovascular-alteration-in-mice-under-oral-treatment-by-the-mao-inhibitor-phenelzine
#19
Christian Carpéné, Josep Mercader, Sophie Le Gonidec, Stéphane Schaak, Jeanne Mialet-Perez, Alexia Zakaroff-Girard, Jean Galitzky
BACKGROUND AND PURPOSE: Phenelzine is an antidepressant drug increasing the risk of hypertensive crisis when dietary tyramine is not restricted. However, this monoamine oxidase (MAO) inhibitor is known to inhibit other enzymes not limited to the nervous system. We studied whether its antiadipogenic and antilipogenic effects in cultured adipocytes could contribute to a mitigation of fattening without unwanted hypertensive or cardiovascular effects. EXPERIMENTAL APPROACH: Mice were fed a standard chow and subjected to a 0...
March 26, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29582414/the-novel-%C3%AE-opioid-receptor-agonist-pzm21-depresses-respiration-and-induces-tolerance-to-antinociception
#20
Rob Hill, Alex Disney, Alex Conibear, Katy Sutcliffe, William Dewey, Stephen Husbands, Chris Bailey, Eamonn Kelly, Graeme Henderson
BACKGROUND AND PURPOSE: PZM21 is a novel μ-opioid receptor (MOPr) ligand that has been reported to induce minimal arrestin recruitment and be devoid of the respiratory depressant effects characteristic of classical μ-opioid ligands such as morphine. We have re-examined the signalling profile of PZM21 and its ability to depress respiration. EXPERIMENTAL APPROACH: G protein (Gi ) activation and arrestin-3 translocation were measured in vitro in MOPr expressing HEK 293 cells using BRET assays...
March 26, 2018: British Journal of Pharmacology
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