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    23607 results match your criteria British journal of pharmacology[Journal]

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    Neurocognition and subjective experience following acute doses of the synthetic cannabinoid JWH-018: A phase 1, placebo-controlled, pilot study.
    Br J Pharmacol 2017 Nov 22. Epub 2017 Nov 22.
    Department of Neuropsychology and Psychopharmacology, Faculty of Psychology and Neuroscience, Maastricht University, Maastricht, The Netherlands.
    Background And Purpose: Synthetic cannabinoids (often sold as Spice or K2) have become a very popular alternative to cannabis due to the easy access and portrayed safety. Controlled studies on the behavioral effects of synthetic cannabinoids are currently lacking, which hampers risk assessments of these compounds.

    Experimental Approach: This is a first attempt to assess the influence of a synthetic cannabinoid, JWH-018, on neurocognition and subjective experience in humans after controlled administration. Read More

    Tetramethylpyrazine nitrone activates AKT/CREB through increasing BDNF expression to promote post-ischemic neuroregeneration and recovery of neurological functions in rats.
    Br J Pharmacol 2017 Nov 21. Epub 2017 Nov 21.
    Institute of New Drug Research and Guangzhou Key Laboratory of Innovative Chemical Drug Research in Cardio-cerebrovascular Diseases, Jinan University College of Pharmacy, Guangzhou, 510632, China.
    Background And Purpose: Neuronal regeneration from endogenous precursors is an attractive strategy for the treatment of ischemic stroke; however, most stroke-generated new born neurons die over time. Therefore, a drug that is both neuroprotective and pro-neurogenic may be promising. In this study, we assessed the neurogenic and oligodendrogenic effects of tetramethylpyrazine nitrone (TBN), a neuroprotective drug candidate for stroke, in a rat model of ischemic stroke. Read More

    Mechanism of doxorubicin cardiotoxicity evaluated by integrating multiple molecular effects into a biophysical model.
    Br J Pharmacol 2017 Nov 21. Epub 2017 Nov 21.
    Division of Imaging Sciences and Biomedical Engineering (MF, SAN) and Cardiovascular Division (MJC), King's College London, London, SE1 7EH, UK.
    Background And Purpose: Doxorubicin (DOX) is an effective cancer therapeutic agent but causes therapy-limiting cardiotoxicity. The effects of DOX and its metabolite doxorubicinol (DOXL) on individual channels have been well characterised in isolation. However, it is unknown how the action and interaction of affected channels combine to generate the phenotypic cardiotoxic outcome. Read More

    Quantifying the relationship between inhibition of VEGFR-2, drug-induced blood pressure elevation and hypertension.
    Br J Pharmacol 2017 Nov 21. Epub 2017 Nov 21.
    AstraZeneca, Cambridge Science Park, Darwin Building Milton Road, Cambridge, CB4 0WG, UK.
    Background And Purpose: Several anti-angiogenic cancer drugs that inhibit VEGF receptor (VEGFR) signalling for efficacy are associated with a 15-60% incidence of hypertension. Tyrosine kinase inhibitors (TKIs) that have off-target activity at VEGFR-2 may also cause blood pressure elevation as an undesirable side effect. Therefore, the ability to translate VEGFR-2 off-target potency into blood pressure elevation would be useful in development of novel TKIs. Read More

    Simultaneous use of erythropoietin and LFM-A13 as a new therapeutic approach for colorectal cancer.
    Br J Pharmacol 2017 Nov 21. Epub 2017 Nov 21.
    Department of Pharmacodynamics, Mickiewicza 2C, 15-222 Bialystok, Poland.
    Background And Purpose: Bruton's tyrosine kinase (BTK) is a non-receptor tyrosine kinase involved in the activation of signaling pathways responsible for cell maturation and viability. BTK has previously been reported to be overexpressed in colon cancers. This kind of cancer is often accompanied by anemia, which is treated with an erythropoietin supplement. Read More

    4-aminopyridine: a pan Kv channel inhibitor that enhances Kv7.4 currents and inhibits noradrenaline-mediated contraction of rat mesenteric small arteries.
    Br J Pharmacol 2017 Nov 20. Epub 2017 Nov 20.
    Department of Biomedical Sciences, Faculty of Health and Medical Sciences, University of Copenhagen, Denmark.
    Background And Purpose: Kv7.4 and Kv7.5 channels are regulators of vascular tone. Read More

    GI-530159, a novel, selective, mechano-sensitive K2P channel opener, reduces rat dorsal root ganglion (DRG) neuron excitability.
    Br J Pharmacol 2017 Nov 18. Epub 2017 Nov 18.
    Medway School of Pharmacy, University of Kent, Central Avenue, Chatham Maritime, Kent, ME4 4TB, UK.
    Background And Purpose: TREK two pore domain potassium channels play a critical role in regulating the excitability of somatosensory nociceptive neurons and are important mediators of pain perception. An understanding of the roles of TREK channels in pain perception and, indeed, in other pathophysiological conditions, has been severely hampered by the lack of potent and/or selective activators and inhibitors. In this study we describe a new, selective opener of TREK channels, GI-530159 (4,4'-(Hexafluoroisopropylidene)bis(p-phenyleneoxy)dianiline). Read More

    Role of p62/SQSTM1 beyond autophagy: a lesson learned from drug-induced toxicity in vitro.
    Br J Pharmacol 2017 Nov 17. Epub 2017 Nov 17.
    Departamento de Farmacología, Facultad de Medicina, Universidad de Valencia, Valencia, 46010, Spain.
    Background And Purpose: SQSTM1/p62 is a multifunctional, stress-induced, scaffold protein involved in multiple cellular processes including autophagic clearance, regulation of inflammatory responses and redox homeostasis. Alterations in its function have been associated with a long list of human pathologies such as neurodegenerative, metabolic and bone diseases (down-regulation), and cancerogenesis (up-regulation). However, its role in the off-target effects of clinically used drugs is still not understood. Read More

    The novel, potent and highly selective 5-HT4 receptor agonist YH12852 significantly improves both upper and lower gastrointestinal motility.
    Br J Pharmacol 2017 Nov 15. Epub 2017 Nov 15.
    Yuhan Research Institute, 25, Tapsil-ro 35beon-gil, Giheung-gu, Yongin-si, Gyeonggi-do, Republic of Korea, 446-902.
    Background And Purpose: 5-HT4 receptor agonists have been shown to be effective to treat various gastrointestinal tract disorders. However, a lack of selectivity against off-targets has been a limiting factor.

    Experimental Approach: The binding affinity and selectivity of YH12852 for human 5-HT4(a) receptor in CHO-K1 cells were evaluated using radioligand binding assays, and agonistic activity was assessed using a beta-lactamase reporter system. Read More

    Tauroursodeoxycholic acid inhibits intestinal inflammation and barrier disruption in NAFLD mice.
    Br J Pharmacol 2017 Nov 15. Epub 2017 Nov 15.
    Division of Gastroenterology, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, 1277 Jiefang Avenue, Wuhan, 430022, China.
    Background And Purpose: The gut-liver axis is associated with the progression of non-alcoholic fatty liver disease (NAFLD). Targeting the gut-liver axis and bile acid-based pharmaceuticals are potential therapies for NAFLD. The effect of tauroursodeoxycholic acid (TUDCA), a candidate medicine for NAFLD, on intestinal barrier function, intestinal inflammation, gut lipid transport and microbiota composition in a murine NAFLD model were analysed. Read More

    Up-regulation of PYK2/PKCα-dependent HO-1 by CO-releasing molecule (CORM)-2 attenuates TNF-α-induced lung inflammation.
    Br J Pharmacol 2017 Nov 15. Epub 2017 Nov 15.
    Research Center for Chinese Herbal Medicine and Research Center for Food and Cosmetic Safety, College of Human Ecology, Chang Gung University of Science and Technology, Tao-Yuan, Taiwan.
    Background And Purpose: Heme oxygenase-1 (HO-1) could provide cytoprotection against various inflammatory diseases. However, the mechanisms underlying carbon monoxide-releasing molecule-2 (CORM-2)-induced HO-1 expression protecting against TNF-α-induced inflammatory responses in human pulmonary alveolar epithelial cells (HPAEpiCs) remain unknown.

    Experimental Approach: CORM-2-induced HO-1 protein and mRNA expression, and signaling pathways were determined by Western blot and real-time PCR, coupled using respective pharmacological inhibitors or transfection with siRNAs. Read More

    Inhibition of acid-sensing ion channels by diminazene and APETx2 evoke partial and highly variable antihyperalgesia in a rat model of inflammatory pain.
    Br J Pharmacol 2017 Nov 14. Epub 2017 Nov 14.
    Institute for Molecular Bioscience, The University of Queensland, St Lucia, QLD, 4072, Australia.
    Background And Purpose: Acid-sensing ion channels (ASICs) are primary acid sensors in mammals, with the ASIC1b and ASIC3 subtypes being involved in peripheral nociception. The antiprotozoal drug diminazene is a moderately potent ASIC inhibitor but its analgesic activity has not been assessed.

    Experimental Approach: We determined the ASIC subtype selectivity of diminazene and the mechanism by which it inhibits ASICs using voltage-clamp electrophysiology of Xenopus oocytes expressing ASICs 1-3. Read More

    RTP801 is a critical factor in the neurodegeneration process of A53T alpha-synuclein in a mouse model of Parkinson's disease under chronic restraint stress.
    Br J Pharmacol 2017 Nov 11. Epub 2017 Nov 11.
    State Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica & Neuroscience Center, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, China.
    Background And Purpose: The incidence of Parkinson's disease exhibited a younger tendency in recent years with the constantly increased stressors of modern society, but this relationship remains obscured. We performed this study to investigate whether stress contributes to this tendency and identify the executor during this process.

    Experimental Approach: Ten-month-old α-synuclein A53T mice, a PD mice model, were treated with chronic restraint stress (CRS) to simulate a PD-sensitive person with constant stress stimulation. Read More

    Sophocarpine attenuates wear particle-induced implant loosening by inhibiting osteoclastogenesis and bone resorption via suppression of the NF-κB signaling pathway in a rat model.
    Br J Pharmacol 2017 Nov 11. Epub 2017 Nov 11.
    Department of Orthopedic Surgery, Second Affiliated Hospital, School of Medicine, Zhejiang University, Hangzhou, People's Republic of China.
    Background And Purpose: Aseptic prosthesis loosening, caused by wear particles, is one of the most common causes of arthroplasty failure. Extensive and over-activated osteoclast formation and physiological functioning are regarded as the mechanism of prosthesis loosening. Therapeutic modalities based on inhibiting osteoclast formation and bone resorption have been confirmed to be an effective way of preventing aseptic prosthesis loosening. Read More

    The Bruton's tyrosine kinase inhibitor PRN473 inhibits neutrophil recruitment via inhibition of Mac-1 signaling.
    Br J Pharmacol 2017 Nov 11. Epub 2017 Nov 11.
    Department of Anesthesiology, intensive care and pain medicine, University Hospital Münster, Albert-Schweitzer-Campus 1 Geb. A1, 48149, Münster, Germany.
    Background And Purpose: Following inflammatory stimuli neutrophils are recruited to sites of inflammation and exert effector functions that often have deleterious effects on tissue integrity, which can lead to organ failure. Btk is expressed in neutrophils, and constitutes a promising pharmacological target for neutrophil mediated tissue damage. Here we evaluate a selective reversible inhibitor of the Bruton's tyrosine kinase (PRN473) for its ability to dampen neutrophil influx via inhibition of adhesion receptor signaling pathways. Read More

    Calcimimetic and calcilytic therapies for inherited disorders of the calcium-sensing receptor signalling pathway.
    Br J Pharmacol 2017 Nov 11. Epub 2017 Nov 11.
    Academic Endocrine Unit, Radcliffe Department of Medicine, University of Oxford, Oxford, UK.
    THE CALCIUM-SENSING RECEPTOR (CAS RECEPTOR) PLAYS A PIVOTAL ROLE IN EXTRACELLULAR CALCIUM HOMEOSTASIS AND GERMLINE LOSS- AND GAIN-OF-FUNCTION MUTATIONS CAUSE FAMILIAL HYPOCALCIURIC HYPERCALCAEMIA (FHH) AND AUTOSOMAL DOMINANT HYPOCALCAEMIA (ADH), RESPECTIVELY. CAS RECEPTOR SIGNAL TRANSDUCTION IN THE PARATHYROID GLANDS IS LIKELY REGULATED BY G-PROTEIN SUBUNIT Α11 (GΑ11) AND ADAPTOR-RELATED PROTEIN COMPLEX-2 SIGMA SUBUNIT (AP2Σ), AND RECENT STUDIES HAVE IDENTIFIED GERMLINE MUTATIONS OF THESE PROTEINS AS A CAUSE OF FHH AND/OR ADH. CALCIMIMETICS AND CALCILYTICS ARE POSITIVE AND NEGATIVE ALLOSTERIC MODULATORS OF THE CAS RECEPTOR THAT HAVE POTENTIAL EFFICACY FOR SYMPTOMATIC FORMS OF FHH AND ADH. Read More

    Towards Functional Selectivity for α6®3γ2 GABAA Receptors: A Series of Novel Pyrazoloquinolinones.
    Br J Pharmacol 2017 Nov 11. Epub 2017 Nov 11.
    Department of Molecular Neurosciences, Center for Brain Research, Medical University Vienna, Spitalgasse 4 -, 1090, Vienna, Austria.
    Background And Purpose: The γ - aminobutyric acid type A (GABAA ) receptors are ligand-gated ion channels which play an important role in neurotransmission. Their variety of binding sites serves as an appealing target for many clinically relevant drugs. Here, we explored the functional selectivity of modulatory effects at specific extracellular α+/®- interfaces, using a systematically varied series of pyrazoloquinolinones. Read More

    Usefulness of knockout mice to clarify the role of the opioid system in chronic pain.
    Br J Pharmacol 2017 Nov 10. Epub 2017 Nov 10.
    Laboratory of Neuropharmacology, Department of Experimental and Health Sciences, Universitat Pompeu Fabra, PRBB, C/ Doctor Aiguader 88, 08003, Barcelona, Spain.
    Several lines of knockout mice deficient in the genes encoding each component of the endogenous opioid system have been used for decades to clarify the specific role of the different opioid receptors and peptide precursors in multiple physiopathological conditions. The use of these genetically modified mice has improved our knowledge of the specific involvement of each endogenous opioid component in nociceptive transmission during acute and chronic pain conditions. The present review summarizes the recent advances obtained using these genetic tools in understanding the role of the opioid system in the pathophysiological mechanisms underlying chronic pain. Read More

    Microbial biotransformations in the human distal gut.
    Br J Pharmacol 2017 Nov 8. Epub 2017 Nov 8.
    uBiome, Inc., San Francisco, California, United States of America.
    The human distal gut is home to a rich and dense microbial community with representatives of all three domains of life which are intricately connected with our physiology and health. The combined genomes of these microbes, collectively called the human microbiome, vastly expand the metabolic capacities of our own genome, allowing us to break down and extract energy from dietary compounds that human enzymes cannot digest. In addition, the variable composition of these communities and their biotransformations might explain inter-individual differences in toxicities, tolerances, and efficacies for certain drugs. Read More

    Protease-activated receptor 1 inhibition protects mice against thrombin-dependent respiratory syncytial virus and human metapneumovirus infections.
    Br J Pharmacol 2017 Nov 4. Epub 2017 Nov 4.
    Infectious Disease Research Centre, Laval University, Quebec city, Quebec, Canada.
    Background And Purpose: Protease-activated receptor 1 (PAR1) has been demonstrated to be involved in the pathogenesis of viral diseases. However, its role remains controversial. The goal of our study was to investigate the contribution of PAR1 to respiratory syncytial virus (RSV) and human metapneumovirus (hMPV) infections. Read More

    Immune-Pineal Axis - Acute inflammatory responses coordinate melatonin synthesis by pinealocytes and phagocytes.
    Br J Pharmacol 2017 Nov 4. Epub 2017 Nov 4.
    Laboratory of Chronopharmacology and Laboratory of Neuroimmunomodulation - Department of Physiology, Institute of Bioscience, University of São Paulo, São Paulo, Brazil.
    Melatonin is well known for its circadian production by the pineal gland, with a growing body of data showing its production by many other cells and organs, including immune cells. The chronobiotic role of pineal melatonin, as well as its protective effects in vitro and in vivo, have been extensively explored. However, the interaction between chronobiotic and defence functions of endogenous melatonin has been little investigated. Read More

    Targeting inflammation to reduce cardiovascular disease risk.
    Br J Pharmacol 2017 Nov;174(22):3895-3897
    Department of Pharmacy, University of Naples Federico II, Naples, Italy.
    This joint themed section of the British Journal of Pharmacology and the British Journal of Clinical Pharmacology stems from a joint British Pharmacological Society - Italian Society of Pharmacology symposium held at the 37(th) National Congress of the Italian Society of Pharmacology in Naples (Italy) from 27 to 30 October 2015.

    Linked Articles: This article is part of a themed section on Targeting Inflammation to Reduce Cardiovascular Disease Risk. To view the other articles in this section visit http://onlinelibrary. Read More

    GPR35 mediates lodoxamide-induced migration inhibitory response but not CXCL17-induced migration stimulatory response in THP-1 cells; Is GPR35 a receptor for CXCL17?
    Br J Pharmacol 2017 Oct 25. Epub 2017 Oct 25.
    Molecular Inflammation Research Center for Aging Intervention (MRCA) and College of Pharmacy, Pusan National University, Busan, 609-735, Republic of Korea.
    GPR35 has long been considered an orphan G protein-couple receptor, and although no endogenous ligand of GPR35 has been discovered, synthetic agonists and antagonists have been developed. CXCL17 (a chemokine) has been reported to be an endogenous ligand of GPR35, and it has even been suggested that it be called CXCR8 (Journal of Immunology 2015; 194:29-33). However, no supporting report on the CXCL17-GPR35 relation has been issued since, although GPR35 is supposed to be a potential therapeutic target in several pathologic conditions. Read More

    Berberine Attenuates Hepatic Steatosis and Enhances Energy Expenditure in Mice by Inducing Autophagy and Fibroblast Growth Factor 21.
    Br J Pharmacol 2017 Oct 24. Epub 2017 Oct 24.
    Department of Endocrinology and Metabolism, Zhongshan Hospital, Fudan University, Shanghai, China.
    Background And Purpose: Berberine, a compound from rhizome coptidis, is traditionally used to treat gastrointestinal infections, such as bacteria diarrhea. Recently, hypoglycemic and hypolipidemic efficacies of berberine were identified. We investigate mechanisms by which berberine regulates hepatic lipid metabolism and energy expenditure in mice. Read More

    Selectivity, cell permeability and oral availability studies of novel bromophenol derivative HPN as PTP1B inhibitor.
    Br J Pharmacol 2017 Oct 23. Epub 2017 Oct 23.
    Key Laboratory of Experimental Marine Biology, Institute of Oceanology, Chinese Academy of Sciences, Qingdao, China.
    Background And Purpose: Protein tyrosine phosphatase 1B (PTP1B) negatively regulates insulin signaling by tyrosine dephosphorylation of insulin receptor. It is a highly validated target for type 2 diabetes therapeutics. Here, the anti-diabetic effects of HPN were evaluated in the diabetic BKS db mice. Read More

    Update on the pharmacology of calcitonin/CGRP family of peptides: IUPHAR Review:"X".
    Br J Pharmacol 2017 Oct 23. Epub 2017 Oct 23.
    School of Biological Science, University of Auckland, New Zealand.
    The calcitonin/calcitonin gene-related peptide (CGRP) family of peptides includes calcitonin, α and β CGRP, amylin, adrenomedullin (AM) and adrenomedullin 2/intermedin (AM2/IMD). Their receptors consist of one of two G protein-coupled receptors (GPCRs), the calcitonin receptor (CTR) or the calcitonin receptor-like receptor (CLR). Further diversity arises from heterodimerisation of these GPCRs with one of three receptor activity-modifying proteins (RAMPs). Read More

    Vortioxetine exerts antiinflammatory and immunomodulatory effects on human monocytes/macrophages.
    Br J Pharmacol 2017 Oct 22. Epub 2017 Oct 22.
    Department of Health Sciences, School of Medicine, University of Piemonte Orientale, Via Solaroli, 17 -, 28100, Novara, Italy.
    Background And Purpose: A crosstalk between the immune system and depression has been postulated, with a key role played by monocytes/macrophages and cytokines. In this paper we examined whether vortioxetine, a multimodal anti-depressive drug, was endowed of antiinflammatory and anti-oxidative activity, leading to immunomodulatory effects on human monocytes and macrophages.

    Experimental Approaches: Human monocytes were isolated from buffy coats and used as such or differentiated into M1 and M2 macrophages. Read More

    IGF-1 activates PI3K/Akt signaling to protect human retinal pigment epithelial cells from amiodarone-induced oxidative injury.
    Br J Pharmacol 2017 Oct 22. Epub 2017 Oct 22.
    Faculty of Health Sciences, University of Macau, Taipa, Macau, China.
    Background And Purpose: Amiodarone (AM) is one of the most effective anti-arrhythmic drugs available. However, clinical applications of AM are limited by its toxic side effects including optic toxicity. The purpose of this study was to investigate the toxic effect of AM on D407 cells (a human Retinal Pigmented Epithelial cell line) and the mechanisms of the protective effect of insulin-like growth factor-1 (IGF-1). Read More

    Differential effects of selective agonists of neuromedin U1 and 2 receptors in obese and diabetic mice.
    Br J Pharmacol 2017 Oct 22. Epub 2017 Oct 22.
    Research, Takeda Pharmaceutical Company Limited, Fujisawa, Japan.
    Background And Purpose: Neuromedin U (NMU) may be a novel target for obesity treatment owing to its anorectic and energy expenditure enhancing effects. Although two receptors, NMU1 and NMU2, are both responsible for the NMU-mediated anti-obesity effects, the receptor agonist with the most appropriate profiles for treating obesity and diabetes in terms of efficacy and safety is as yet unknown. Thus, we developed and evaluated novel NMU1/2 receptor-selective agonists. Read More

    Cannabidiolic acid methyl ester, a stable synthetic analogue of cannabidiolic acid, can produce 5-HT1A receptor-mediated suppression of nausea and anxiety in rats.
    Br J Pharmacol 2017 Oct 22. Epub 2017 Oct 22.
    Institute for Drug Research, Medical Faculty, Hebrew University, Jerusalem, Israel.
    Background And Purpose: To compare the abilities of cannabidiolic acid methyl ester (HU-580) and cannabidiolic acid (CBDA) to enhance 5-HT1A receptor activation in vitro and to produce 5-HT1A -mediated reductions of nausea and anxiety in vivo.

    Experimental Approach: We investigated the effects of HU-580 and CBDA on (i) activation by 8-hydroxy-2-(di-n-propylamino)tetralin of human 5-HT1A receptors in CHO cell membranes, using [(35) S]GTPγS binding assays, (ii) gaping by rats in acute and anticipatory nausea models, and (iii) stress-induced anxiety-like behaviour, as indicated by exit time from the light compartment of a light-dark box of rats subjected 24 h earlier to six tone-paired foot shocks.

    Key Results: HU-580 and CBDA increased the Emax of 8-hydroxy-2-(di-n-propylamino)tetralin in vitro at 0. Read More

    5-HT1F Receptor-Mediated Mitochondrial Biogenesis for the Treatment of Parkinson's Disease.
    Br J Pharmacol 2017 Oct 22. Epub 2017 Oct 22.
    Department of Pharmacology and Toxicology, College of Pharmacy, University of Arizona, Tucson, AZ, 85721.
    Background And Purpose: Parkinson's disease is characterized by progressive decline in motor function due to degeneration of nigrostriatal dopaminergic neurons, as well as other deficits including cognitive impairment and behavioral abnormalities. Mitochondrial dysfunction, leading to loss of ATP-dependent cellular functions, calcium overload, excitotoxicity and oxidative stress, is implicated in the pathophysiology of Parkinson's disease. Using the 5-HT1F receptor agonist LY344864, a known inducer of mitochondrial biogenesis (MB), this study investigated the therapeutic efficacy of stimulating MB on dopaminergic neuron loss in a mouse model of Parkinson's disease. Read More

    THE CONCISE GUIDE TO PHARMACOLOGY 2017/18: G protein-coupled receptors.
    Br J Pharmacol 2017 Dec;174 Suppl 1:S17-S129
    Centre for Integrative Physiology, University of Edinburgh, Edinburgh, EH8 9XD, UK.
    The Concise Guide to PHARMACOLOGY 2017/18 provides concise overviews of the key properties of nearly 1800 human drug targets with an emphasis on selective pharmacology (where available), 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 properties. Read More

    THE CONCISE GUIDE TO PHARMACOLOGY 2017/18: Other ion channels.
    Br J Pharmacol 2017 Dec;174 Suppl 1:S195-S207
    Centre for Integrative Physiology, University of Edinburgh, Edinburgh, EH8 9XD, UK.
    The Concise Guide to PHARMACOLOGY 2017/18 provides concise overviews of the key properties of nearly 1800 human drug targets with an emphasis on selective pharmacology (where available), 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 properties. Read More

    THE CONCISE GUIDE TO PHARMACOLOGY 2017/18: Ligand-gated ion channels.
    Br J Pharmacol 2017 Dec;174 Suppl 1:S130-S159
    Centre for Integrative Physiology, University of Edinburgh, Edinburgh, EH8 9XD, UK.
    The Concise Guide to PHARMACOLOGY 2017/18 provides concise overviews of the key properties of nearly 1800 human drug targets with an emphasis on selective pharmacology (where available), 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 properties. Read More

    THE CONCISE GUIDE TO PHARMACOLOGY 2017/18: Overview.
    Br J Pharmacol 2017 Dec;174 Suppl 1:S1-S16
    Centre for Integrative Physiology, University of Edinburgh, Edinburgh, EH8 9XD, UK.
    The Concise Guide to PHARMACOLOGY 2017/18 is the third in this series of biennial publications. This version provides concise overviews of the key properties of nearly 1800 human drug targets with an emphasis on selective pharmacology (where available), plus links to an open access knowledgebase of drug targets and their ligands (www.guidetopharmacology. Read More

    THE CONCISE GUIDE TO PHARMACOLOGY 2017/18: Catalytic receptors.
    Br J Pharmacol 2017 Dec;174 Suppl 1:S225-S271
    Centre for Integrative Physiology, University of Edinburgh, Edinburgh, EH8 9XD, UK.
    The Concise Guide to PHARMACOLOGY 2017/18 provides concise overviews of the key properties of nearly 1800 human drug targets with an emphasis on selective pharmacology (where available), 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 properties. Read More

    THE CONCISE GUIDE TO PHARMACOLOGY 2017/18: Transporters.
    Br J Pharmacol 2017 Dec;174 Suppl 1:S360-S446
    Centre for Integrative Physiology, University of Edinburgh, Edinburgh, EH8 9XD, UK.
    The Concise Guide to PHARMACOLOGY 2017/18 provides concise overviews of the key properties of nearly 1800 human drug targets with an emphasis on selective pharmacology (where available), 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 properties. Read More

    THE CONCISE GUIDE TO PHARMACOLOGY 2017/18: Enzymes.
    Br J Pharmacol 2017 Dec;174 Suppl 1:S272-S359
    Centre for Integrative Physiology, University of Edinburgh, Edinburgh, EH8 9XD, UK.
    The Concise Guide to PHARMACOLOGY 2017/18 provides concise overviews of the key properties of nearly 1800 human drug targets with an emphasis on selective pharmacology (where available), 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 properties. Read More

    THE CONCISE GUIDE TO PHARMACOLOGY 2017/18: Voltage-gated ion channels.
    Br J Pharmacol 2017 Dec;174 Suppl 1:S160-S194
    Centre for Integrative Physiology, University of Edinburgh, Edinburgh, EH8 9XD, UK.
    The Concise Guide to PHARMACOLOGY 2017/18 provides concise overviews of the key properties of nearly 1800 human drug targets with an emphasis on selective pharmacology (where available), 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 properties. Read More

    THE CONCISE GUIDE TO PHARMACOLOGY 2017/18: Nuclear hormone receptors.
    Br J Pharmacol 2017 Dec;174 Suppl 1:S208-S224
    Centre for Integrative Physiology, University of Edinburgh, Edinburgh, EH8 9XD, UK.
    The Concise Guide to PHARMACOLOGY 2017/18 provides concise overviews of the key properties of nearly 1800 human drug targets with an emphasis on selective pharmacology (where available), 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 properties. Read More

    TRPV4 regulates vascular endothelial permeability during colonic inflammation in dextran sulphate sodium-induced murine colitis.
    Br J Pharmacol 2017 Oct 20. Epub 2017 Oct 20.
    Division of Pathological Sciences, Department of Pharmacology and Experimental Therapeutics, Kyoto Pharmaceutical University, Kyoto, Japan.
    Background And Purpose: The transient receptor potential vanilloid 4 (TRPV4) is a nonselective cation channel involved in physical sensing in various tissue types. The present study aimed to elucidate the function and expression of TRPV4 in colonic vascular endothelial cells during dextran sulphate sodium (DSS)-induced colitis.

    Experimental Approach: The role of TRPV4 in the progression of colonic inflammation was examined in the 2 % DSS-induced murine colitis model using immunohistochemical analysis, western blotting, and Evans blue dye extrusion assay. Read More

    Whole body physiologically based modelling of beta-blockers in the rat: Events in tissues and plasma following an intravenous bolus dose.
    Br J Pharmacol 2017 Oct 20. Epub 2017 Oct 20.
    Centre for Applied Pharmacokinetic Research, Manchester Pharmacy School, University of Manchester, Manchester, UK.
    Background And Purpose: Whole body physiologically based pharmacokinetic (PBPK) models have been increasingly applied in drug development to describe kinetic events of therapeutic agents in animals and human. The advantage of such modelling is the ability to incorporate vast amounts of physiological information, such as organ blood flow and volume, to ensure that the model is as close to reality as possible.

    Experimental Approach: Prior PBPK model development of enantiomers of a series of seven racemic betablockers, namely acebutolol, betaxolol, bisoprolol, metoprolol, oxprenolol, pindolol and propranolol, together with S-timolol in rat was based on tissue and blood concentration data at steady state. Read More

    FL-926-16, a novel bioavailable carnosinase-resistant carnosine derivative, prevents onset and stops progression of diabetic nephropathy in db/db mice.
    Br J Pharmacol 2017 Oct 20. Epub 2017 Oct 20.
    Department of Clinical Molecular Medicine, "La Sapienza" University, Rome, Italy.
    Background And Purpose: The advanced glycation endproducts (AGEs) participate in the pathogenesis of diabetic nephropathy (DN) by promoting renal inflammation and injury. L-carnosine acts as a quencher of the AGE precursors reactive carbonyl species (RCS), but it is rapidly inactivated by carnosinase. This study evaluated the effect of FL-926-16, a carnosinase-resistant and bioavailable carnosine derivative, on the onset and progression of DN in db/db mice. Read More

    New insights into cardiotoxicity caused by chemotherapeutic agents.
    Br J Pharmacol 2017 Nov;174(21):3675-3676
    The Hatter Cardiovascular Institute, University College London, London, UK.
    Linked Articles: This article is part of a themed section on New Insights into Cardiotoxicity Caused by Chemotherapeutic Agents. To view the other articles in this section visit http://onlinelibrary.wiley. Read More

    Amelioration of autoimmunity with an inhibitor selectively targeting all active centers of the immunoproteasome.
    Br J Pharmacol 2017 Oct 15. Epub 2017 Oct 15.
    Biotechnology Institute Thurgau (BITg) at the University of Konstanz, 8280, Kreuzlingen, Switzerland.
    Background And Purpose: MECL-1 (β2i), LMP2 (β1i), and LMP7 (β5i) are the proteolytically active subunits of the immunoproteasome, a special type of proteasome mainly expressed in hematopoietic cells. Targeting LMP7 has been shown to be therapeutically effective in pre-clinical models of autoimmune diseases. In this study, a recently described inhibitor of the immunoproteasome LU-005i was investigated with respect to selectivity and biological activity. Read More

    Heterogeneous distribution of alectinib in neuroblastoma xenografts revealed by matrix-assisted laser desorption ionization mass spectrometry imaging: a pilot study.
    Br J Pharmacol 2017 Oct 13. Epub 2017 Oct 13.
    Division of Molecular Pharmacology, National Cancer Center Research Institute, Tokyo, Japan.
    Background And Purpose: The penetration of the anaplastic lymphoma kinase (ALK) inhibitor alectinib in neuroblastomas and the relationship between alectinib and ALK expression are unknown. The aim of this study was to perform a quantitative investigation of the inter- and intra-tumoural distribution of alectinib in different neuroblastoma xenograft models using matrix-assisted laser desorption ionization MS imaging (MALDI-MSI).

    Experimental Approach: The distribution of alectinib in NB1 (ALK amplification) and SK-N-FI (ALK wild-type) xenograft tissues was analysed using MALDI-MSI. Read More

    Transient receptor potential vanilloid 1 inhibitors block laparotomy- and opioid-induced infarct size reduction in rats.
    Br J Pharmacol 2017 Oct 5. Epub 2017 Oct 5.
    Department of Anesthesiology, Perioperative and Pain Medicine, School of Medicine, Stanford University, Stanford, CA, USA.
    Background And Purpose: In light of the opioid epidemic, physicians are increasingly prescribing non-opioid analgesics to surgical patients. Transient receptor potential vanilloid 1 (TRPV1) inhibitors are potentially alternative pain therapeutics for surgery. Here, we examined in rodents whether the cardioprotection conferred by two common procedures during surgery, a laparotomy or morphine delivery, is mediated by the TRPV1 channel. Read More

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