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European Journal of Pharmacology

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https://www.readbyqxmd.com/read/28716726/early-life-risperidone-enhances-locomotor-responses-to-amphetamine-during-adulthood
#1
Bobbie Lee Stubbeman, Clifford J Brown, Justin R Yates, Mark E Bardgett
Antipsychotic drug prescriptions for pediatric populations have increased over the past 20 years, particularly the use of atypical antipsychotic drugs such as risperidone. Most antipsychotic drugs target forebrain dopamine systems, and early-life antipsychotic drug exposure could conceivably reset forebrain neurotransmitter function in a permanent manner that persists into adulthood. This study determined whether chronic risperidone administration during development modified locomotor responses to the dopamine/norepinephrine agonist, D-amphetamine, in adult rats...
July 14, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28716725/cardamonin-attenuates-lung-carcinoma-and-promotes-autophagy-via-targeting-p53-and-regulating-mtor
#2
Shasha Hou, Xiaoyao Yin, Ziling Wang, Jinhua Zhang, Qi Yuan, Zhinan Chen
As a chalcone extracted from Alpinia rafflesiana, Cardamonin has been reported to serve as anticancer agent and induces autophagy. This study was to elucidate the effects of Cardamonin on cell proliferation and autophagy and its potential mechanism in lung carcinoma cells. In this study, CCK-8 and MTT assay were carried out to examine the impact of Cardamonin on cell multiplication in vitro. Tumor cell growth and Ki-67 (a marker of proliferation) levels were observed in a murine model; Autophagy levels were monitored by western blot, quantitative PCR and transmission electron microscope in human lung cancer cells and tumor tissues...
July 14, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28716724/the-ppar%C3%AE-activator-fenofibrate-inhibits-voltage-dependent-k-channels-in-rabbit-coronary-arterial-smooth-muscle-cells
#3
Hongliang Li, Sung Eun Shin, Mi Seon Seo, Jin Ryeol An, Won-Kyo Jung, Kwon-Soo Ha, Eun-Taek Han, Seok-Ho Hong, Hyoweon Bang, Young Min Bae, Amy L Firth, Il-Whan Choi, Won Sun Park
We examined the effects of the PPARα activator fenofibrate on voltage-dependent K(+) (Kv) channels using a patch clamp technique in native rabbit coronary arterial smooth muscle cells. Kv current was inhibited by application of fenofibrate in a concentration-dependent manner, with an apparent IC50 value of 6.39 ± 0.53μM and a slope value (Hill coefficient) of 1.63 ± 0.10. Fenofibrate accelerated the decay rate of Kv channel inactivation. The rate constants of association and dissociation for fenofibrate were 0...
July 14, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28716723/pharmacological-characterization-of-the-interaction-between-umeclidinium-and-vilanterol-in-human-bronchi
#4
Luigino Calzetta, Paola Rogliani, Francesco Facciolo, Erino Rendina, Mario Cazzola, Maria Gabriella Matera
The long-acting β2-agonist (LABA) / long-acting muscarinic antagonist (LAMA) fixed dose combination (FDC) therapy represents the cornerstone for the treatment of chronic obstructive pulmonary disease (COPD). Nevertheless, conflicting clinical findings still exist on the real benefit of the LABA/LAMA FDCs. Therefore, we investigated whether combining the LABA vilanterol with the LAMA umeclidinium may induce synergistic bronchorelaxant effect in isolated airways. The effect of umeclidinium and vilanterol, administered alone, in combination at the ratio of concentrations reproducing the doses delivered by Anoro(®) Ellipta(®) (55:22), or at isoeffective low concentrations, was investigated on the cholinergic contractile tone induced by the parasympathetic activation of human isolated airways...
July 14, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28709622/genipin-protects-d-galactosamine-and-lipopolysaccharide-induced-hepatic-injury-through-suppression-of-the-necroptosis-mediated-inflammasome-signaling
#5
Min-Jong Seo, Jeong-Min Hong, Seok-Joo Kim, Sun-Mee Lee
Acute liver failure (ALF) is a life-threatening syndrome resulting from massive inflammation and hepatocyte death. Necroptosis, a programmed cell death controlled by receptor-interacting protein kinase (RIP) 1 and RIP3, has been shown to play an important role in regulating inflammation via crosstalk between other intracellular signaling. The inflammasome is a major intracellular multiprotein that induces inflammatory responses by mediating immune cell infiltration, thus potentiating injury. Genipin, a major active compound of the gardenia fruit, exhibits anti-inflammatory, antioxidant, and anti-apoptotic properties...
July 11, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28709621/role-of-n-acetyl-galactosamine-4-so4-a-ligand-of-cd206-in-hsv-induced-mouse-model-of-beh%C3%A3-et-s-disease
#6
Bunsoon Choi, Hasan M Sayeed, S M Shamsul Islam, Seonghyang Sohn
CD206 is a macrophage mannose receptor involved in variety of autoimmune and inflammatory diseases. This study aimed to identify the pathogenic role of CD206 in a herpes simplex virus (HSV) induced Behçet's disease (BD) mouse model. CD206 positive cells were detected in peripheral blood mononuclear cells and quantified by flow cytometry. Levels of cytokines were measured by ELISA. CD206 was found to be down-regulated both in vitro (10(-6) M) and in vivo (200μg/mouse) after treatment with N-acetylgalactosamine (GalNAc), a ligand for CD206...
July 11, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28705714/aristeromycin-and-dznep-cause-growth-inhibition-of-prostate-cancer-via-induction-of-mir-26a
#7
Noriko Uchiyama, Yukiya Tanaka, Tomohiro Kawamoto
Most prostate cancers initially respond to androgen deprivation therapy, but then progress from androgen-dependent to androgen-independent prostate cancers. In the present study, a differential cytotoxicity screen of hormone-resistant prostate cancer LNCaP-hr cells and the parental LNCaP-FGC cells against normal MRC5 fibroblast cells, identified a small molecule compound, Aristeromycin (a derivative of 3-deazaneplanocin A (DZNeP)). The molecular target was shown to be S-adenosylhomocysteine hydrolase (AHCY), which catalyzes reversible hydrolysis of S-adenosylhomocysteine (SAH) to adenosine and L-homocysteine...
July 10, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28705713/sn003-a-crf1-receptor-antagonist-attenuates-depressive-like-behavior-and-detrusor-overactivity-symptoms-induced-by-13-cis-retinoic-acid-in-rats
#8
Andrzej Wróbel, Urszula Doboszewska, Ewa Rechberger, Piotr Wlaź, Tomasz Rechberger
Overactive bladder (OAB) often co-exists with depression in women. The corticotropin-releasing factor (CRF) system participates in the pathophysiology of both disorders. Therefore, we tested the effects of acute treatment with a reversible CRF receptor type-1 (CRF1) antagonist, SN003 (1mg/kg, i.v.), representatives of first (solifenacin, 0.03mg/kg, i.v.) and second (mirabegron, 1mg/kg, i.v.) line treatments for OAB as well as an antidepressant imipramine (30mg/kg, i.p.) on changes in behavior and detrusor overactivity (DO) symptoms induced by a 6-week administration of 13-cis-retinoic acid (13-cis-RA, 1mg/kg/day, i...
July 10, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28697992/pde3-inhibition-by-c-type-natriuretic-peptide-induced-cgmp-enhances-camp-mediated-signaling-in-both-non-failing-and-failing-hearts
#9
Silja Meier, Kjetil Wessel Andressen, Jan Magnus Aronsen, Ivar Sjaastad, Karina Hougen, Tor Skomedal, Jan-Bjørn Osnes, Eirik Qvigstad, Finn Olav Levy, Lise Román Moltzau
We have previously shown that the natriuretic peptide receptor B (NPR-B) agonist C-type natriuretic peptide (CNP) enhances cyclic adenosine 3´,5´-monophosphate (cAMP)-mediated signaling in failing hearts, through cyclic guanosine 3´,5´-monophosphate (cGMP)-mediated phosphodiesterase (PDE) 3 inhibition. As several signaling pathways are importantly changed in failing hearts, it could not be taken for granted that this crosstalk would be the same in non-failing hearts. Thus, we wanted to clarify to which extent this effect of CNP occurred also in non-failing hearts...
July 8, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28697991/carbamazepine-effects-on-pain-management-and-serum-il-6-il-10-evaluation-in-addicted-patients-undergoing-surgery
#10
Alireza Salimi, Masoumeh Sabetkasaei, Hanna Raisi, Farzaneh Labibi, Haleh Ameli, Yalda Khazaei-Poul, Kamran Mottaghi, Farhad Safari, Ali Nazem-Bokaei, Seyed-Amir Mohajerani, Malek Zarei, Taraneh Moini-Zanjani
Postoperative pain control remains an important issue in the field of surgery. Assessing and managing patients with acute pain who are addicted to opioids are often challenging. It has been shown that, addicted patients are less tolerant to pain. There is limited evidence to guide the management of acute pain in these patients. Here we studied the effect of preemptive use of carbamazepine on pain behavior and serum IL-6, IL-10 levels in the addicted patients. 90 male patients (25-45 years, BMI 20-27), were divided into 3 group of 30 patients: 1- control, 2- addicted, 3- addicted patients receiving carbamazepine 400mg before surgery...
July 8, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28694068/jkb-122-is-effective-alone-or-in-combination-with-prednisolone-in-con-a-induced-hepatitis
#11
Mei-Chi Hsu, Sheng-Hung Liu, Chiung-Wen Wang, Nai-Yun Hu, Edwin S C Wu, Ying-Chu Shih, Peter J S Chiu
Con A-induced hepatitis in mice is an established model of autoimmune hepatitis (AIH). JKB-122, a toll-like receptor 4 (TLR4) antagonist, was tested for hepatotprotectant activity. Within several hours of Con A challenge (15mg/kg iv), increased production of proinflammatory cytokines with inflammatory infiltrate occurred in the liver. The severity of tissue necrosis and the amount of circulating liver enzymes peak at 24h post Con A challenge. JKB-122 was given 24 and 16h before, then concurrently, and 4 and 8h (× 5 doses) after challenge with Con A...
July 8, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28690192/suppression-of-osteogenic-differentiation-in-mesenchymal-stem-cells-from-patients-with-ossification-of-the-posterior-longitudinal-ligament-by-a-histamine-2-receptor-antagonist
#12
Xizhe Liu, Gentaro Kumagai, Kanichiro Wada, Toshihiro Tanaka, Taku Fujita, Ayako Sasaki, Ken-Ichi Furukawa, Yasuyuki Ishibashi
Mesenchymal stem cells (MSCs) in ossification of the posterior longitudinal ligament (OPLL) patients have a high propensity toward osteogenesis. Histamine receptor H2 (H2R) antagonists (H2 blockers) like famotidine decrease ossification in patients, by an unclear mechanism. To confirm that MSCs express H2R and to clarify how H2 blockers suppress osteogenic differentiation, we used spinal-ligament MSCs from patients with OPLL or with cervical spondylotic myelopathy (CSM) (control). The MSCs were treated with 10, 30, or 100nM famotidine for 7 or 21 days...
July 8, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28694067/pharmacological-analysis-of-the-inhibition-produced-by-moxonidine-and-agmatine-on-the-vasodepressor-sensory-cgrpergic-outflow-in-pithed-rats
#13
Eloísa Rubio-Beltrán, Alejandro Labastida-Ramírez, Oswaldo Hernández-Abreu, Antoinette MaassenVanDenBrink, Carlos M Villalón
Calcitonin gene-related peptide (CGRP) plays a role in several (patho)physiological functions, and modulation of its release is considered a therapeutic target. In this respect, electrical spinal (T9-T12) stimulation of the perivascular sensory outflow in pithed rats produces vasodepressor responses mediated by CGRP release. This study investigated the role of imidazoline I1 and I2 receptors in the inhibition by moxonidine and agmatine of these vasodepressor responses. Male Wistar pithed rats (pretreated i...
July 7, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28690193/synergistic-inhibition-of-a%C3%AE-production-by-combinations-of-%C3%AE-secretase-modulators
#14
Alan S Robertson, Lawrence G Iben, Cong Wei, Jere E Meredith, Dieter M Drexler, Martyn Banks, Gregory D Vite, Richard E Olson, Lorin A Thompson, Charles F Albright, Michael K Ahlijanian, Jeremy H Toyn
Alzheimer's disease is associated with the accumulation of amyloid-β (Aβ) in the brain. In particular, the 42-amino acid form, Aβ1-42, is thought to play a key role in the disease. It is therefore of interest that diverse compounds, known as γ-secretase modulators (GSM), can selectively decrease Aβ1-42 production without inhibiting the production of other forms of Aβ. Here we describe the novel discovery of synergistic inhibition of Aβ by certain combinations of GSMs. Cell cultures were treated with pairwise combinations of GSMs to determine how Aβ peptide production was affected...
July 6, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28690191/methyl-e-3-3-4-dihydroxyphenyl-acryloyl-tryptophanate-can-suppress-mcp-1-expression-by-inhibiting-p38-map-kinase-and-nf-%C3%AE%C2%BAb-in-lps-stimulated-differentiated-thp-1-cells
#15
Jae B Park, Thomas T Y Wang
Methyl (E)-(3-(3,4-dihydroxyphenyl)acryloyl)tryptophanate (MHAT) is an O-methyl ester of javamide-II showing strong anti-inflammatory activity. Therefore, in this study, MHAT was chemically synthesized, and its effects on p38 MAP kinase, NF-κB, and monocyte chemotactic factor-1 (MCP-1) expression were investigated in LPS-stimulated differentiated THP-1 cells. MHAT inhibited p38 MAP kinase with an IC50 of 12μM, and the inhibition was supported by an in silico model showing that its binding to p38 MAP kinase was stronger than that of SB203580...
July 6, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28690190/immunomodulatory-potential-of-hesperetin-and-chrysin-through-the-cellular-and-humoral-response
#16
Aïcha Sassi, Imen Mokdad Bzéouich, Nadia Mustapha, Mouna Maatouk, Kamel Ghedira, Leila Chekir-Ghedira
Flavonoids are polyphenols frequently consumed in the diet they have been suggested to exert a number of beneficial actions on human health, including anti-inflammatory activity. This study investigated the immunomodulatory effects of two flavonoids, Chrysin and Hesperetin. The effects of flavonoids on B and T cell proliferation were assessed on splenocytes stimulated or not with mitogens. However, their effects on cytotoxic T lymphocyte (CTL) and natural killer (NK) activities were assessed in splenocytes co-incubated with target cells...
July 6, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28690189/efavirenz-what-is-known-about-the-cellular-mechanisms-responsible-for-its-adverse-effects
#17
REVIEW
Nadezda Apostolova, Ana Blas-Garcia, Maria J Galindo, Juan V Esplugues
The HIV infection remains an important health problem worldwide. However, due to the efficacy of combined antiretroviral therapy (cART), it has ceased to be a mortal condition, becoming a chronic disease instead. Efavirenz, the most prescribed non-nucleoside analogue reverse transcriptase inhibitor (NNRTI), has been a key component of cART since its commercialization in 1998. Though still a drug of choice in many countries, its primacy has been challenged by the arrival of newer antiretroviral agents with better toxicity profiles and treatment adherence...
July 6, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28688913/neuroprotective-effect-of-lovastatin-on-motor-deficit-induced-by-sciatic-nerve-crush-in-the-rat
#18
Mohammad B Ghayour, Arash Abdolmaleki, Morteza B Rassouli
Following severe peripheral nerve injury (PNI), regeneration is often insufficient and functional recovery is incomplete. Any agents that limit the spread of neural tissue damage may enhance the nerve regeneration. In this regard, statins have been shown to have neuroprotective properties. We investigated the effects of Lovastatin against sciatic nerve crush injury in male Wistar Rats. Lovastatin or vehicle was given parenteraly to rats for 7 days postoperative. In Lovastatin treatment groups, a single dose of agent (2 and 5mg/kg) was administered daily...
July 6, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28688914/glucagon-and-glucagon-like-peptide-1-as-novel-anti-inflammatory-and-immunomodulatory-compounds
#19
REVIEW
Daniella B R Insuela, Vinicius F Carvalho
Glucagon and glucagon-like peptide-1 (GLP-1) are polypeptide hormones that are produced by pancreatic α-cells and the intestine, respectively, whose main function is to control glucose homeostasis. The glucagon and GLP-1 levels are imbalanced in diabetes. Furthermore, type 1diabetic patients and animals present with a diminished inflammatory response, which is related to some morbidities of diabetes, such as a higher incidence of infectious diseases, including sepsis. The focus of this review is to briefly summarize the state of the art concerning the effects of glucagon and GLP-1 on the inflammatory response...
July 5, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28688912/inhibition-of-the-kynurenine-pathway-protects-against-reactive-microglial-associated-reductions-in-the-complexity-of-primary-cortical-neurons
#20
Katherine O'Farrell, Eimear Fagan, Thomas J Connor, Andrew Harkin
Brain glia possess the rate limiting enzyme indoleamine 2, 3-dioxygenase (IDO) which catalyses the conversion of tryptophan to kynurenine. Microglia also express kynurenine monooxygenase (KMO) and kynureninase (KYNU) which lead to the production of the free radical producing metabolites, 3-hydroxykynurenine and 3-hydroxyanthranillic acid respectively and subsequently production of the NMDA receptor agonist quinolinic acid. The aim of this study was to examine the effect of IFNγ-stimulated kynurenine pathway (KP) induction in microglia on neurite outgrowth and complexity, and to determine whether alterations could be abrogated using pharmacological inhibitors of the KP...
July 5, 2017: European Journal of Pharmacology
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