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Pharmacological Reports: PR

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https://www.readbyqxmd.com/read/28095353/liver-alpha-amylase-gene-expression-as-an-early-obesity-biomarker
#1
Marzieh Mojbafan, Zohreh Afsartala, Mahsa M Amoli, Mahdi Mahmoudi, Parichehreh Yaghmaei, Bagher Larijani, Azadeh Ebrahim-Habibi
BACKGROUND: Obesity is a major health problem worldwide, for which preventive and therapeutic means are still needed. Alpha-amylase is a digestive enzyme whose inhibition has been targeted as a potential anti-obesity strategy. However, alpha-amylase gene expression has not been particularly attended to, and in contrast with pancreatic and salivary amylases, fewer studies have focused on liver alpha-amylase. The present study aimed at investigating the expression of alpha-amylase gene in obese and normal mice at RNA and protein level as well as acarbose effect on this gene expression in hepatocyte cell culture...
November 5, 2016: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28092808/antinociceptive-effect-of-co-administered-nmda-and-histamine-h4-receptor-antagonists-in-a-rat-model-of-acute-pain
#2
Renata Wolińska, Anna Leśniak, Małgorzata Żochowska, Mariusz Sacharczuk, Katarzyna Kieć-Kononowicz, Magdalena Bujalska-Zadrożny
BACKGROUND: The histamine H4 receptor (H4R) has attracted a lot of attention in terms of its role in antinociception. The N-Methyl-d-aspartic acid (NMDA) receptor is a well-characterized participant in pain pathways. However, it's influence on H4R signaling is poorly understood. Thus, in the present study we investigated the effect of a selective H4R antagonist JNJ7777120 (25mg/kg) and a NMDA receptor antagonist MK-801 (0.1-10μg) on nociceptive thresholds in a rat acute pain model. METHODS: The influence of intrathecally (it), intracerebroventricularly (icv) and intraplantarly (ipl) administered MK-801 co-injected with JNJ7777120 administered intraperitoneally (ip) was determined in the modified Randall-Selitto paw pressure, the tail flick and plantar tests...
October 29, 2016: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28092807/application-of-the-dreadd-technique-in-biomedical-brain-research
#3
REVIEW
Grzegorz Dobrzanski, Małgorzata Kossut
The DREADD (Designer Receptors Exclusively Activated by Designer Drugs) technique is a new chemogenetic approach allowing for selective and remote control of neural activity with a high degree of spatial resolution. Since its discovery in 2007 the DREADD technique was successfully employed into basic research, and together with the optogenetic method provided so far the best tool to influence the activity of the brain circuits and cell populations. The first aim of this review was to concisely describe the technique with regard to such issues like the history of its development, biochemistry as well as modes of the designer receptors delivery and expression...
October 29, 2016: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/27940401/dna-damage-induced-by-nadph-cytochrome-p450-reductase-activated-idarubicin-in-sensitive-and-multidrug-resistant-mcf7-breast-cancer-cells
#4
Wojciech Żwierełło, Agnieszka Maruszewska, Robert Nowak, Dorota Kostrzewa-Nowak, Jolanta Tarasiuk
BACKGROUND: Idarubicin (IDA) is one of clinically important anticancer drugs belonging to the anthracycline antibiotic family. The aim of this study was to examine DNA damage induced by NADPH cytochrome P450 reductase (CPR)-activated IDA in human sensitive MCF7 and multidrug resistant MCF7/DOX500 (overexpressing P-gp) breast adenocarcinoma cells. METHODS: The evaluation of DNA fragmentation caused by single strand breaks (SSB) and double strand breaks (DSB) was performed using terminal deoxynucleotidyl transferase-mediated dUTP nick end labelling (TUNEL) test...
February 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/27923162/comparison-of-different-osmotic-therapies-in-a-mouse-model-of-traumatic-brain-injury
#5
Vinoth K M Khandelwal, Prabhakar Singh, Tatiana Ravingerova, Marslin Gregory, Hardik Gandhi, Manu Chaudhary
BACKGROUND: Inflammation in the affected region, increased intracranial pressure, consequent oedema and congestion contribute to the negative outcome of traumatic brain injury. Osmotic therapies are recommended for improvement in cognitive and motor functions. Aim of the present study was to evaluate the effect of osmotic therapies in a mice model of traumatic brain injury. METHODS: Experimental closed head injury was performed in adult Swiss albino mice by the weight-drop method...
February 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/27923161/antinociceptive-tolerance-to-nsaids-in-the-rat-formalin-test-is-mediated-by-the-opioid-mechanism
#6
Nana Tsiklauri, Ivliane Nozadze, Gulnaz Gurtskaia, Merab G Tsagareli
BACKGROUND: In the past decade it has been shown that tolerance develops to the antinociceptive effect of repeated systemic administration of commonly used non-steroidal anti-inflammatory drugs (NSAIDs) in acute pain models using rats. This is similar to the tolerance observed with opioid-induced analgesia. In the present study, we investigated the development of tolerance to the analgesic effects of NSAIDs diclofenac, ketorolac and xefocam in a chronic inflammatory pain model, the formalin test...
February 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/27923160/adolescent-and-adult-mice-display-differential-sensitivity-to-the-effects-of-bupropion-on-the-acquisition-of-a-water-maze-task
#7
Carmen Gómez, Carmen Carrasco, Rosa Redolat
BACKGROUND: Adolescence is characterized by major neurobiological changes, and the effects of some psychoactive drugs seem to differ between adolescents and adults. Bupropion, an antidepressant that is also used to treat nicotine addiction, induces behavioral actions in both adolescent and adult rodents. However, the effects of this drug on spatial ability have not been compared in animals at different stages of their development. The present study was conducted to assess the effects of bupropion on spatial learning and memory in adolescent and adult mice...
February 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/27923159/apoptotic-effect-of-chalcone-derivatives-of-2-acetylthiophene-in-human-breast-cancer-cells
#8
Tatiana B Fogaça, Rosiane M Martins, Karine R Begnini, Caroline Carapina, Marina Ritter, Claudio M P de Pereira, Fabiana K Seixas, Tiago Collares
BACKGROUND: A variety of chalcones have demonstrated cytotoxic activity toward several cancer cell lines. This study aimed to investigate the cytotoxicity of four chalcones derivatives of 2-acetylthiophene in human breast cancer cell lines. METHODS: MCF-7 and MDA-MB-231 cells were treated with synthesized chalcones and the cytotoxicity was evaluated by tetrazolium dye (MTT), live/dead, and DAPI assays. RESULTS: Chalcones significantly decreased MCF-7 and MDA-MB-231 cells viability in vitro in a dose dependent manner...
February 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/27923158/effect-of-intensive-lipid-lowering-therapies-on-cholinesterase-activity-in-patients-with-coronary-artery-disease
#9
Edyta Pytel, Bożena Bukowska, Maria Koter-Michalak, Małgorzata Olszewska-Banaszczyk, Paulina Gorzelak-Pabiś, Marlena Broncel
BACKGROUND: Many disease entities, including coronary artery disease (CAD), demonstrate abnormalities in the activity of cholinesterases. As CAD is characterized by an increase in cholesterol level, patients with this disease are treated with lipid-lowering drugs. The present study attempts to determine how statin or combined statin and ezetimibe therapy influences cholinesterase activity. METHODS: Plasma and erythrocytes were isolated from the peripheral blood of CAD patients (n=61) and healthy subjects (n=63)...
February 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/27923157/adjuvant-neuronal-nitric-oxide-synthase-inhibition-for-combined-treatment-of-epilepsy-and-comorbid-depression
#10
Tanveer Singh, Rajesh Kumar Goel
BACKGROUND: Elevated nitric oxide (NO) levels in the brain have been apparently associated with depression in kindled animals. Owing to the major role of neuronal nitric oxide synthase (nNOS) in brain and ineffectiveness of antiepileptic drugs (AEDs) in restoring nitrosative stress, the present study was envisaged to evaluate the adjuvant nNOS inhibitor, 7-nitroindazole (7-NI) with valproic acid for combined treatment of epilepsy and associated depression. METHODS: Pentylenetetrazole kindled animals associated with depression were treated with vehicle, valproate (300mg/kg/day ip), valproate with 7-NI (10mg/kg; 20mg/kg; 40mg/kg)/day ip and 7-NI (40mg/kg/day ip) for 15days...
February 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/27919002/inhibitory-effect-of-fentanyl-citrate-on-the-release-of-endothlin-1-induced-by-bradykinin-in-melanoma-cells
#11
Tsugunobu Andoh, Akira Shinohara, Yasushi Kuraishi
BACKGROUND: Our previous study showed that the μ-opioid receptor agonist fentanyl citrate inhibits endothelin-1-and bradykinin-mediated pain responses in mice orthotopically inoculated with melanoma cells. We also demonstrated that bradykinin induces endothelin-1 secretion in melanoma cells. However, the analgesic mechanisms of fentanyl citrate remain unclear. Thus, the present study was conducted to determine whether fentanyl citrate affects bradykinin-induced endothelin-1 secretion in B16-BL6 melanoma cells...
February 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/27915186/role-of-the-purinergic-signaling-in-epilepsy
#12
REVIEW
Marek Cieślak, Andrzej Wojtczak, Michał Komoszyński
Adenine nucleotides and adenosine are signaling molecules that activate purinergic receptors P1 and P2. Activation of A1 adenosine receptors has an anticonvulsant action, whereas activation of A2A receptors might initiate seizures. Therefore, a significant limitation to the use of A1 receptor agonists as drugs in the CNS might be their peripheral side effects. The anti-epileptic activity of adenosine is related to its increased concentration outside the cell. This increase might result from the inhibition of the equilibrative nucleoside transporters (ENTs)...
February 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/27915185/anti-inflammatory-analgesic-and-anti-tumor-properties-of-gold-nanoparticles
#13
Raimundo Fernandes de Araújo, Aurigena Antunes de Araújo, Jonas Bispo Pessoa, Franscisco Paulo Freire Neto, Gisele Ribeiro da Silva, Ana Luiza C S Leitão Oliveira, Thaís Gomes de Carvalho, Heloiza F O Silva, Mateus Eugênio, Celso Sant'Anna, Luiz H S Gasparotto
BACKGROUND: Gold nanoparticles (GNPs) are regarded as potential platforms for drug delivery. However, their interaction with live organisms must be understood prior to their utilization as drug carriers. The present study reports the anti-inflammatory, analgesic and anti-tumor effects of GNPs. The biodistribution of GNPs and their effect on various tissues have also been studied. METHODS: GNPs were synthesized through an environmentally friendly route and characterized with TEM and UV-vis...
February 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/27915184/anti-atherosclerotic-effects-of-pravastatin-in-brachiocephalic-artery-in-comparison-with-en-face-aorta-and-aortic-roots-in-apoe-ldlr-mice
#14
Renata B Kostogrys, Magdalena Franczyk-Zarow, Marlena Gasior-Glogowska, Edyta Kus, Agnieszka Jasztal, Tomasz P Wrobel, Malgorzata Baranska, Izabela Czyzynska-Cichon, Anna Drahun, Angelika Manterys, Stefan Chlopicki
BACKGROUND: Cholesterol-dependent and independent mechanisms were proposed to explain anti-atherosclerotic action of statins in humans. However, their effects in murine models of atherosclerosis have not been consistently demonstrated. Here, we studied the effects of pravastatin on atherosclerosis in ApoE/LDLR(-/-) mice fed a control and atherogenic diet. METHODS: ApoE/LDLR(-/-) mice were fed a control (CHOW) or an atherogenic (Low Carbohydrate High Protein, LCHP) diet...
February 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/27915183/search-for-new-potential-anticonvulsants-with-anxiolytic-and-antidepressant-properties-among-derivatives-of-4-4-diphenylpyrrolidin-2-one
#15
Katarzyna Malawska, Aleksandra Rak, Beata Gryzło, Kinga Sałat, Małgorzata Michałowska, Elżbieta Żmudzka, Krzysztof Lodarski, Barbara Malawska, Katarzyna Kulig
BACKGROUND: The aim of this study was to synthesize a series of new N-Mannich bases derived from 4,4-diphenylpyrrolidin-2-one having differently substituted 4-phenylpiperazines as potential anticonvulsant agents with additional (beneficial) pharmacological properties. METHODS: The target compounds 8-12 were prepared in one step from the 4-substituted phenylpiperazines, paraformaldehyde, and synthesized 4,4-diphenylpyrrolodin-2-one (7) by a Mannich-type reaction...
February 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/27914294/selective-agonism-of-mglu8-receptors-by-s-3-4-dicarboxyphenylglycine-does-not-affect-sleep-stages-in-the-rat
#16
María Cavas, Gianluigi Scesa, Mercedes Martín-López, José Francisco Navarro
BACKGROUND: Metabotropic glutamate receptors (mGlu) play a role in a number of physiological processes and behaviors, as well as in certain pathological conditions and diseases. New drugs targetting mGlu receptors are being developed with treatment purposes. Recent data indicates that glutamate is involved in sleep, and pharmacological manipulation of distinct subtypes of mGlu receptors affect sleep. Here the consequences of selective pharmacological agonism of mGlu8 receptor upon sleep and wakefulness are explored for the first time...
February 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/27914293/diethylcarbamazine-attenuates-lps-induced-acute-lung-injury-in-mice-by-apoptosis-of-inflammatory-cells
#17
Ingrid Tavares Fragoso, Edlene Lima Ribeiro, Fabiana Oliveira Dos Santos Gomes, Mariana Aragão Matos Donato, Amanda Karolina Soares Silva, Amanda Costa O de Oliveira, Shyrlene Meiry da Rocha Araújo, Karla Patrícia Sousa Barbosa, Laise Aline Martins Santos, Christina Alves Peixoto
BACKGROUND: Acute lung injury (ALI) is characterized by extensive neutrophil infiltration, and apoptosis delay considered part of the pathogenesis of the condition. Despite great advances in treatment strategies, few effective therapies are known for ALI. Diethylcarbamazine (DEC) is used against lymphatic filariasis, a number of studies have described its anti-inflammatory activities and pro-apoptotic effect. These properties have been associated with nuclear factor kappa-B inactivation...
February 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/27912102/toyocamycin-induces-apoptosis-via-the-crosstalk-between-reactive-oxygen-species-and-p38-erk-mapks-signaling-pathway-in-human-prostate-cancer-pc-3-cells
#18
Sul-Gi Park, Sang-Hun Kim, Kwang-Youn Kim, Sun-Nyoung Yu, Hyeun-Deok Choi, Young-Wook Kim, Hyo-Won Nam, Young-Kyo Seo, Soon-Cheol Ahn
BACKGROUND: Toyocamycin, an antibiotic agent isolated from Streptomyces species, has been shown to have anticancer and chemopreventive effects on various cancer cells. Until now, Toyocamycin-induced apoptosis has not been reported to be involved in the regulation between mitogen-activated protein kinases (MAPKs) and reactive oxygen species (ROS) production. METHODS: Cell viability assay, western blot, cell-cycle arrest, annexin V/propidium iodide assay, reactive oxygen species (ROS) production, mitochondrial membrane potential and intracellular Ca(2+) flux were assayed...
February 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/27907839/influence-of-picolinic-acid-on-seizure-susceptibility-in-mice
#19
Anna Cioczek-Czuczwar, Piotr Czuczwar, Waldemar Andrzej Turski, Jolanta Parada-Turska
BACKGROUND: The mechanism of drug resistance in epilepsy remains unknown. Picolinic acid (PIC) is an endogenous metabolite of the kynurenine pathway and a chelating agent added to dietary supplements. Both inhibitory and excitatory properties of PIC were reported. The aim of this study was to determine the influence of exogenously applied PIC upon the electroconvulsive threshold and the activity of chemical convulsants in eight models of epilepsy in mice. METHODS: All experiments were performed on adult male Swiss albino mice...
February 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/27907838/fear-memory-in-a-neurodevelopmental-model-of-schizophrenia-based-on-the-postnatal-blockade-of-nmda-receptors
#20
Joachim Latusz, Aleksandra Radaszkiewicz, Ewelina Bator, Krzysztof Wędzony, Marzena Maćkowiak
BACKGROUND: Epidemiological data have indicated that memory impairment is observed during adolescence in groups at high risk for schizophrenia and might precede the appearance of schizophrenia symptoms in adulthood. METHODS: In the present study, we used a neurodevelopmental model of schizophrenia based on the postnatal blockade of N-methyl-d-aspartate (NMDA) receptors in rats to investigate fear memory in adolescence and adulthood. The rats were treated with increasing doses of CGP 37849 (CGP), a competitive antagonist of the NMDA receptor (1...
February 2017: Pharmacological Reports: PR
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