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British Journal of Pharmacology

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https://www.readbyqxmd.com/read/29235100/embryonic-exposure-to-valproic-acid-affects-the-histaminergic-system-and-the-social-behavior-of-adult-zebrafish-danio-rerio
#1
Diego Baronio, Henri A J Puttonen, Maria Sundvik, Svetlana Semenova, Essi Lehtonen, Pertti Panula
BACKGROUND AND PURPOSE: Histamine modulates several behaviors and physiological functions and its deficiency is associated with neuropsychiatric disorders. Gestational intake of valproic acid (VPA) is linked to Autism Spectrum Disorder (ASD), which is characterized by impaired sociability and stereotypies. VPA effects on the neurochemistry and functional morphology of the histaminergic system in ASD are unclear. Zebrafish are highly social and given the similarities between zebrafish and human neurotransmitter systems, we decided to use zebrafish to study VPA effects on histamine...
December 12, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29235094/effects-of-corilagin-on-alleviating-cholestasis-via-fxr-associated-pathways-in-vitro-and-in-vivo
#2
Fan Yang, Yao Wang, Gang Li, Juan Xue, Zhi-Lin Chen, Feng Jin, Lei Luo, Xuan Zhou, Qian Ma, Xin Cai, Hua-Rong Li, Lei Zhao
BACKGROUND AND PURPOSE: This aim of this study was to investigate the effects of corilagin on alleviating intrahepatic cholestasis by regulating liver FXR (farnesoid X receptor)-associated pathways in vitro and in vivo. EXPERIMENTAL APPROACH: Cellular and animal models were treated with different concentrations of corilagin. In the cellular experiments, FXR expression was up-regulated by either lentiviral transduction or GW4064 treatment and down-regulated by either siRNA technology or treatment with guggulsterones...
December 12, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29235092/bumetanide-blocks-the-acquisition-of-conditioned-fear-in-adult-rats
#3
Meng-Chang Ko, Ming-Chung Lee, Tso-Hao Tang, Tamara G Amstislavskaya, Maria A Tikhonova, Yi-Ling Yang, Kwok-Tung Lu
BACKGROUND AND PURPOSE: Administration of bumetanide has anxiolytic effects in rat models of conditioned fear. As a loop diuretic, bumetanide may act as an anxiolytic by modulating GABAergic synaptic transmission through the antagonism of cation-chloride cotransporters (CCCs). Its clinical potential for the treatment of anxiety disorders deserves further investigation. In this study, we evaluated the possible role of the basolateral nucleus of amygdala (BLA) in the anxiolytic effect of bumetanide...
December 12, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29232769/antiparkinsonian-and-antidyskinetic-profiles-of-two-novel-potent-and-selective-nociceptin-orphanin-fq-receptor-agonists
#4
Ludovico Arcuri, Salvatore Novello, Martina Frassineti, Daniela Mercatelli, Clarissa Anna Pisanò, Ilaria Morella, Stefania Fasano, Blair V Journigan, Michael E Meyer, Willma E Polgar, Riccardo Brambilla, Nurulain T Zaveri, Michele Morari
BACKGROUND AND PURPOSE: We previously showed that Nociceptin/orphanin FQ opioid peptide (NOP) receptor agonists attenuate the expression of levodopa-induced dyskinesia in animal models of Parkinson's disease. We now investigate the efficacy of two novel, potent and chemically distinct NOP receptor agonists, AT-390 and AT-403, to improve parkinsonian disabilities and attenuate dyskinesia development and expression. EXPERIMENTAL APPROACH: Binding affinity and functional efficacy of AT-390 and AT-403 at the opioid receptors were determined in radioligand displacement assays and in GTPγS binding assay respectively, conducted in Chinese hamster ovary cells...
December 12, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29232759/involvement-of-cyp1b1-in-interferon-%C3%AE-induced-alterations-of-epithelial-barrier-integrity
#5
Mireille Alhouayek, Sandra Gouveia-Figueira, Marie-Louise Hammarström, Christopher J Fowler
BACKGROUND AND PURPOSE: CYP1B1 and CYP1A1 are important extra hepatic cytochromes, expressed in the colon and implicated in the metabolism of dietary constituents and exogenous compounds. CYP1B1 expression is increased by pro-inflammatory cytokines and it has been recently implicated in regulation of blood brain barrier function. We investigated its involvement in the increased permeability of the intestinal epithelial barrier observed in inflammatory conditions. EXPERIMENTAL APPROACH: (IFNγ, 10 ng...
December 12, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29215157/knockdown-of-the-transcript-of-extracellular-signal-regulated-kinase-in-the-brain-modulated-hypothalamic-neuropeptide-mediated-appetite-control-in-amphetamine-treated-rats
#6
Ching-Han Yu, Yih-Shou Hsieh, Pei-Ni Chen, Jeng-Rung Chen, Dong-Yih Kuo
BACKGROUND AND PURPOSE: Amphetamine (AMPH) is a releaser of dopamine stored in synaptic terminals, which can suppress appetite by changing the expression levels of neuropeptide Y (NPY) and proopiomelanocortin (POMC) in the hypothalamus. This study explored whether extracellular signal-regulated kinases (ERKs) were involved in appetite control mediated by cAMP response element binding protein (CREB), NPY and POMC in AMPH-treated rats. EXPERIMENTAL APPROACH: Rats were given AMPH for four days and changes in feeding behavior and expression levels of pERK, pCREB, NPY and melanocortin receptor 3 (MC3R) were examined and compared...
December 7, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29214652/pharmacology-in-translation-the-preclinical-and-early-clinical-profile-of-the-novel-%C3%AE-2-3-functionally-selective-gabaa-receptor-positive-allosteric-modulator-pf-06372865
#7
Sarah A Nickolls, Rachel Gurrell, Guido van Amerongen, Juha Kammonen, Lishuang Cao, Adam R Brown, Clara Stead, Andy Mead, Christine Watson, Cathleen Hsu, Robert M Owen, Andy Pike, Rebecca L Fish, Laigao Chen, Ruolun Qiu, Evan D Morris, Gang Feng, Mark Whitlock, Donal Gorman, Joop van Gerven, David S Reynolds, Pinky Dua, Richard P Butt
BACKGROUND AND PURPOSE: Benzodiazepines (BZDs), non-selective positive allosteric modulators (PAMs) of GABAA receptors, have significant side-effects that limit their clinical utility. As many of these side-effects are mediated by the α1 subunit there has been a concerted effort to develop α2/3 subtype-selective PAMs. EXPERIMENTAL APPROACH: In vitro screening assays were used to identify molecules with functional selectivity for receptors containing α2/3 subunits over those containing α1 subunits...
December 7, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29210063/opioid-induced-inhibition-of-the-human-serotonin-and-norepinephrine-transporters-in-vitro-link-to-clinical-reports-of-serotonin-syndrome
#8
Anna Rickli, Evangelia Liakoni, Marius C Hoener, Matthias E Liechti
BACKGROUND AND PURPOSE: Opioids may inhibit the serotonin and norepinephrine transporters (SERT and NET, respectively). NET inhibition may contribute to analgesia, and SERT inhibition or interactions with serotonin receptors may cause serotonergic toxicity. However, the effects of different opioids on the human SERT, NET, and serotonin receptors have not been sufficiently studied. EXPERIMENTAL APPROACH: We determined the potencies of different opioids to inhibit the SERT and NET in vitro using human transporter-transfected cells...
December 6, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29197066/characterisation-of-the-properties-of-a-selective-orally-bioavailable-autotaxin-inhibitor-in-preclinical-models-of-advanced-stages-of-liver-fibrosis
#9
Manuel Baader, Tom Bretschneider, Andre Broermann, Joerg F Rippmann, Birgit Stierstorfer, Christian A Kuttruff, Michael Mark
BACKGROUND AND PURPOSE: Autotaxin (ATX) is a secreted phospholipase which hydrolyses lysophosphatidylcholine (LPC) to generate lysophosphatidic acid (LPA). The extracellular signalling molecule LPA exerts its biological actions through activation of six G protein-coupled receptors expressed in various cell types including fibroblasts. Multiple preclinical studies using knockout animals, LPA receptor antagonists or ATX inhibitors have provided evidence for a potential role of the ATX/LPA axis in tissue fibrosis...
December 2, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29197072/induction-of-mast-cell-accumulation-by-chymase-via-an-enzymatic-activity-and-icam-1-dependent-mechanism
#10
Huiyun Zhang, Junling Wang, Ling Wang, Mengmeng Zhan, Shigang Li, Zeman Fang, Ciyan Xu, Yanshan Zheng, Shaoheng He
BACKGROUND AND PURPOSE: Chymase is a unique abundant secretory product of mast cells, and a potent chemoattractant for eosinophils, monocytes and neutrophils, but little is known of its influence on mast cell accumulation. EXPERIMENTAL APPROACH: Using mouse peritoneal inflammation model, cell migration assay and flowcytometry analysis, we investigated role of chymase in recruiting mast cells. KEY RESULTS: The results showed that chymase induced up to 5...
December 1, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29194564/oxaliplatin-induced-enteric-neuronal-loss-and-intestinal-dysfunction-is-prevented-by-co-treatment-with-bgp-15
#11
Rachel M McQuade, Vanesa Stojanovska, Rhian Stavely, Cara Timpani, Aaron C Petersen, Raquel Abalo, Joel C Bornstein, Emma Rybalka, Kulmira Nurgali
BACKGROUND AND PURPOSE: Gastrointestinal side-effects of chemotherapy are under-recognised clinical hurdle leading to dose reduction, delays and cessation of treatment, presenting a constant challenge for efficient and tolerable anti-cancer treatment. We have previously found that oxaliplatin treatment results in intestinal dysfunction, oxidative stress and loss of enteric neurons. BGP-15 is a novel cytoprotective compound with potential HSP72 co-inducing and PARP inhibiting properties...
November 30, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29194563/cyclic-analogues-of-%C3%AE-conotoxin-vc1-1-inhibit-colonic-nociceptors-and-provide-analgesia-in-a-mouse-model-of-chronic-abdominal-pain
#12
Joel Castro, Luke Grundy, Annemie Deiteren, Andrea M Harrington, Tracey O'Donnell, Jessica Maddern, Jessi Moore, Sonia Garcia-Caraballo, Grigori Y Rychkov, Rilei Yu, Quentin Kaas, David J Craik, David J Adams, Stuart M Brierley
BACKGROUND AND PURPOSE: Patients with Irritable Bowel Syndrome suffer from chronic visceral pain (CVP); however, limited analgesic therapeutic options are currently available. We have shown that α-conotoxin Vc1.1-induced activation of GABAB receptors on the peripheral endings of colonic afferents reduces nociceptive signalling from the viscera. However, the analgesic efficacy of more stable, cyclized versions of Vc1.1 on CVP remains to be determined. EXPERIMENTAL APPROACH: Using ex vivo colonic afferent preparations, we determined the inhibitory actions of cyclized Vc1...
November 30, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29181850/can-nonclinical-repolarization-assays-predict-the-results-of-clinical-thorough-qt-studies-results-from-a-research-consortium
#13
Eunjung Park, Gary A Gintant, Daoqin Bi, Devi Kozeli, Syril D Pettit, Jennifer B Pierson, Matthew Skinner, James Willard, Todd Wisialowski, John Koerner, Jean-Pierre Valentin
BACKGROUND AND PURPOSE: Translation of nonclinical markers of delayed ventricular repolarization to clinical QTc prolongation (a biomarker for Torsades de Pointes proarrhythmia) remains an issue in drug discovery and regulatory evaluations. A retrospective analysis of 150 submitted drug applications in a US-FDA database was conducted to determine the utility of established nonclinical in vitro iKr current (hERG), action potential duration (APD) and in vivo (QTc) repolarization assays to detect and predict clinical QTc prolongation...
November 27, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29181847/achyranthes-bidentata-polypeptide-protects-dopaminergic-neurons-from-apoptosis-in-parkinson-s-disease-models-both-in-vitro-and-in-vivo
#14
Su Peng, Caiping Wang, Jinyu Ma, Ketao Jiang, Yuhui Jiang, Xiaosong Gu, Cheng Sun
BACKGROUND AND PURPOSE: Parkinson's disease (PD) is a neurodegenerative disorder closely associated with dopaminergic neuron loss. It is well documented that Achyranthes bidentata polypeptides (ABPP) are potent neuroprotective agents in several kinds of neurons. Therefore, we predicted that ABPP might play a beneficial role against PD by protecting dopaminergic neurons from apoptosis. EXPERIMENTAL APPROACH: The SH-SY5Y cells and primary rat dopaminergic neurons were pretreated with ABPPk, a purified fraction of ABPP, and then the cells were exposure to MPP+ to induce apoptosis...
November 27, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29178246/effects-of-the-antagomirs-15b-and-200b-on-the-altered-healing-pattern-of-diabetic-mice
#15
Gabriele Pizzino, Natasha Irrera, Federica Galfo, Giovanni Pallio, Federica Mannino, Angelica D'amore, Enrica Pellegrino, Antonio Ieni, Giuseppina T Russo, Marco Calapai, Domenica Altavilla, Francesco Squadrito, Alessandra Bitto
BACKGROUND AND PURPOSE: Diabetic subjects with non-healing ulcers have a reduced expression of vascular endothelial growth factor (VEGF). Genetically diabetic mice have an altered expression pattern of VEGF and its receptor, VEGFR-2. In diabetic wounds, miR15b and miR200b which respectively inhibit VEGF and VEGF-R2 mRNAs are up-regulated, further affecting the impaired angiogenesis. We investigated whether anti-miRs directed toward miR15b and miR200b could improve wound repair in genetically diabetic mice...
November 26, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29172248/differential-involvement-of-ipsilateral-and-contralateral-spinal-cord-astrocyte-d-serine-in-carrageenan-induced-mirror-image-pain-role-of-sigma-1-receptors-and-astrocyte-gap-junctions
#16
Hoon-Seong Choi, Dae-Hyun Roh, Seo-Yeon Yoon, Sheu-Ran Choi, Soon-Gu Kwon, Suk-Yun Kang, Ji-Young Moon, Ho-Jae Han, Alvin J Beitz, Jang-Hern Lee
BACKGROUND AND PURPOSE: Although we have recently demonstrated that spinal astrocyte gap junctions mediate the development of mirror-image pain (MIP), it is still unclear which astrocyte-derived factor is responsible for the development of MIP and how its production is controlled. In the present study, we focused on the role of ipsilateral versus contralateral D-serine in the development of MIP and investigated the possible involvement of sigma-1 receptors and gap junctions in astrocyte D-serine production...
November 24, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29171021/xenopus-glp-1-derived-and-pegylated-glp-1-receptor-agonists-long-acting-hypoglycemic-and-insulinotropic-activities-with-potential-therapeutic-utilities
#17
Jing Han, Yingying Fei, Feng Zhou, Xinyu Chen, Ying Zhang, Lin Liu, Junjie Fu
BACKGROUND AND PURPOSE: Incretin-based therapies based on glucagon-like peptide-1 (GLP-1) receptor agonists are effective methods for treating type 2 diabetes. Numerous research efforts are focused on the development of long-acting GLP-1 receptor agonists. However, all GLP-1 receptor agonists in clinical use or in clinical development are based on human GLP-1 or Gila GLP-1. We previously identified xGLP-1B as a potent GLP-1 receptor agonist based on Xenopus GLP-1. EXPERIMENTAL APPROACH: To further modify the structure of xGLP-1B, alanine scanning was performed to study the structure-activity relationship of xGLP-1B...
November 24, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29164599/neurocognition-and-subjective-experience-following-acute-doses-of-the-synthetic-cannabinoid-jwh-018-a-phase-1-placebo-controlled-pilot-study
#18
Eef L Theunissen, Nadia R P W Hutten, Natasha L Mason, Stefan W Toennes, Kim P C Kuypers, Eliza B de Sousa Fernandes Perna, Johannes G Ramaekers
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...
November 22, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29161771/tetramethylpyrazine-nitrone-activates-akt-creb-through-increasing-bdnf-expression-to-promote-post-ischemic-neuroregeneration-and-recovery-of-neurological-functions-in-rats
#19
Gaoxiao Zhang, Tao Zhang, Ning Li, Liangmiao Wu, Jianbo Gu, Cuimei Li, Chen Zhao, Wei Liu, Luchen Shan, Pei Yu, Xifei Yang, Yaohui Tang, Guo-Yuan Yang, Yuqiang Wang, Yewei Sun, Zaijun Zhang
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. EXPERIMENTAL APPROACH: Sprague Dawley (SD) rats were subjected to middle cerebral artery occlusion (MCAO)...
November 21, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29161764/mechanism-of-doxorubicin-cardiotoxicity-evaluated-by-integrating-multiple-molecular-effects-into-a-biophysical-model
#20
M Fernandez-Chas, M J Curtis, S A Niederer
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. We sought to develop an in silico model that links drug effects on channels to action potential duration (APD) and intracellular Ca(2+) concentration in order to address this gap in knowledge...
November 21, 2017: British Journal of Pharmacology
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