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Naunyn-Schmiedeberg's Archives of Pharmacology

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https://www.readbyqxmd.com/read/28509114/implicating-the-potential-role-of-orexin-in-hypertension
#1
REVIEW
Monika Rani, Raghuvansh Kumar, Pawan Krishan
Orexins (orexin A and orexin B), neuropeptides of hypothalamic origin also known as hypocretins, have been well documented for regulating the different physiological functions including feeding, sleep wakefulness, stress, and reward. However, from the past few years, orexins have evolved as an emerging biomarker for various endocrine disorders including diabetes mellitus and obesity which ultimately leads to various cardiovascular risk factors. Orexins exist in two isoforms orexin A and orexin B and exert their effect by acting on the G protein-coupled receptors orexin 1 receptor (OX1R) and orexin 2 receptor (OX2R)...
May 16, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28493050/fasudil-ameliorates-endothelial-dysfunction-in-streptozotocin-induced-diabetic-rats-a-possible-role-of-rho-kinase
#2
Amal Hofni, Basim A Shehata Messiha, Safwat A Mangoura
Endothelial dysfunction is a major contributor to the pathogenesis of vascular disease in diabetes mellitus and RhoA/Rho-kinase (ROCK) system appears to play a crucial role in this setting. The present study was conducted to investigate the effect of the selective ROCK inhibitor, fasudil, on diabetes-related endothelial dysfunction and elucidated its underlying mechanism(s). Diabetes was induced by a single intraperitoneal injection of streptozotocin (STZ, 50 mg/kg), and fasudil (5 mg/kg per day) was orally administered for 8 weeks...
May 11, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28477086/effects-of-salvianolic-acid-b-on-l-type-calcium-channels-and-myocardial-contractility-in-isolated-rat-ventricular-myocytes-and-herg-k-channels-expressed-in-hek293-cells
#3
Qiongtao Song, Xue Han, Yuchong Xue, Tao Song, Xi Chu, Xuan Zhang, Yuanyuan Zhang, Ying Zhang, Jianping Zhang, Li Chu
Salvianolic acid B (Sal B), one of the chief water-soluble constituents in Radix Salviae Milthiorrhizae, has often been reported to possess considerable cardiovascular regulatory effects. However, the underlying biochemical and cellular mechanisms of its cardioprotection remain unclear. This study was designed to evaluate the role of Sal B regulation in L-type Ca(2+) channel currents (ICa,L) and cell contractility in rat cardiomyocytes and hERG K(+) channels expressed in HEK293 cells with the patch-clamp and Ca(2+) imaging techniques to clarify its underlying cardioprotective mechanisms...
May 5, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28474169/denominator-changes-may-obscure-results-from-single-well-assays-%C3%AE-3-adrenoceptor-ligand-induced-changes-of-cell-number-as-example
#4
LETTER
Katerina Okeke, Martina B Michel-Reher, Martin C Michel
No abstract text is available yet for this article.
May 4, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28451724/chronic-loss-of-inhibitor-1-diminishes-cardiac-ryr2-phosphorylation-despite-exaggerated-camkii-activity
#5
Stefan Neef, Jordi Heijman, Kristian Otte, Matthias Dewenter, Ali R Saadatmand, Stefanie Meyer-Roxlau, Christopher L Antos, Johannes Backs, Dobromir Dobrev, Michael Wagner, Lars S Maier, Ali El-Armouche
Inhibitor-1 (I-1) modulates protein phosphatase 1 (PP1) activity and thereby counteracts the phosphorylation by kinases. I-1 is downregulated and deactivated in failing hearts, but whether its role is beneficial or detrimental remains controversial, and opposing therapeutic strategies have been proposed. Overactivity of Ca(2+)/calmodulin-dependent protein kinase II (CaMKII) with hyperphosphorylation of ryanodine receptors (RyR2) at the CaMKII-site is recognized to be central for heart failure and arrhythmias...
April 27, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28439630/myriocin-treatment-of-cf-lung-infection-and-inflammation-complex-analyses-for-enigmatic-lipids
#6
Anna Caretti, Michele Vasso, Fabiola Tecla Bonezzi, Andrea Gallina, Marco Trinchera, Alice Rossi, Raffaella Adami, Josefina Casas, Monica Falleni, Delfina Tosi, Alessandra Bragonzi, Riccardo Ghidoni, Cecilia Gelfi, Paola Signorelli
Our aim was to use quantitative and qualitative analyses to gain further insight into the role of ceramide in cystic fibrosis (CF). Sphingolipid ceramide is a known inflammatory mediator, and its accumulation in inflamed lung has been reported in different types of emphysema, chronic obstructive pulmonary disease and CF. CF is caused by a mutation of the chloride channel and associated with hyperinflammation of the respiratory airways and high susceptibility to ongoing infections. We have previously demonstrated that de novo ceramide synthesis is enhanced in lung inflammation and sustains Pseudomonas aeruginosa pulmonary infection in a CF murine model...
April 24, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28429110/inhibition-of-the-crf1-receptor-influences-the-activity-of-antidepressant-drugs-in-the-forced-swim-test-in-rats
#7
Andrzej Wróbel, Anna Serefko, Aleksandra Szopa, Karol Rojek, Ewa Poleszak, Krystyna Skalicka-Woźniak, Jarosław Dudka
Hyperactivity of the hypothalamic-pituitary-adrenal axis (HPA) and impairment of the central corticotropin-releasing factor (CRF) system are factors in the pathogenesis of depression. Though several antagonists of the CRF1 receptor were effective in the recognized behavioral tests for antidepressant activity, there is still little information on the potential interactions between CRF1 receptor inhibitors and conventional antidepressant therapy. The aim of our study was to assess the influence of SN003, a CRF1 receptor blocker, on the activity of imipramine and fluoxetine in the forced swim test (FST) in rats which presented some signs of depression...
April 20, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28409209/2-acetyl-5-tetrahydroxybutyl-imidazole-thi-protects-661w-cells-against-oxidative-stress
#8
Carlotta Fabiani, Aida Zulueta, Fabiola Bonezzi, Josefina Casas, Riccardo Ghidoni, Paola Signorelli, Anna Caretti
Retinal degeneration and in particular retinitis pigmentosa (RP) is associated to ceramide (Cer) accumulation and cell death induction. Cer and sphingosine-1-phosphate (S1P) belong to the sphingolipids class and exert a pro-apoptotic and pro-survival activity, respectively. Our aim is to target sphingolipid metabolism by inhibiting S1P lyase that regulates one of the S1P degradation pathways, to reduce retinal photoreceptor damage. The murine 661W cone-like cell line was pretreated with THI, an inhibitor of S1P lyase and exposed to H2O2-induced oxidative stress...
April 13, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28409208/inhibitors-of-ceramide-de-novo-biosynthesis-rescue-damages-induced-by-cigarette-smoke-in-airways-epithelia
#9
Aida Zulueta, Anna Caretti, Giuseppe Matteo Campisi, Andrea Brizzolari, Jose Luis Abad, Rita Paroni, Paola Signorelli, Riccardo Ghidoni
Exposure to cigarette smoke represents the most important risk factor for the development of chronic obstructive pulmonary disease (COPD). COPD is characterized by chronic inflammation of the airways, imbalance of proteolytic activity resulting in the destruction of lung parenchyma, alveolar hypoxia, oxidative stress, and apoptosis. Sphingolipids are structural membrane components whose metabolism is altered during stress. Known as apoptosis and inflammation inducer, the sphingolipid ceramide was found to accumulate in COPD airways and its plasma concentration increased as well...
April 13, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28391533/the-validation-of-calophyllum-brasiliense-guanandi-uses-in-brazilian-traditional-medicine-as-analgesic-by-in-vivo-antinociceptive-evaluation-and-its-chemical-analysis
#10
Luiz Carlos Klein-Júnior, Daniele Zambiasi, Giovana Rocha Salgado, Franco Delle Monache, Valdir Cechinel Filho, Fátima de Campos Buzzi
Calophyllum brasiliense is used as anti-inflammatory and analgesic in Brazilian traditional medicine. Thus, the main purpose of this study is to evaluate the antinociceptive effect of the chloroform fraction of C. brasiliense (CFCB) roots and to investigate its main mechanism of action. The antinociceptive effect of CFCB was evaluated in mice using acetic acid-induced writhing, formalin-induced paw licking, and hot-plate tests and capsaicin- and glutamate-induced nociception. Brasiliensic acid and 1,2-dimethoxyxanthone were isolated and evaluated in writhing test...
April 8, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28382499/sitagliptin-exerts-anti-apoptotic-effect-in-nephrotoxicity-induced-by-cisplatin-in-rats
#11
Rehab S Abdelrahman
Sitagliptin is a selective inhibitor of dipeptidylpeptidase-4 enzyme used for the management of diabetes mellitus type II. The anti-inflammatory, antioxidant, and anti-apoptotic properties of sitagliptin were documented. This study was designed to explore the effect of sitagliptin (10 mg/kg, orally) on nephrotoxicity induced by cisplatin (7 mg/kg, i.p.) in Sprague-Dawley rats. Nephrotoxicity of cisplatin was manifested by elevation in renal somatic index, proteinuria, blood urea nitrogen, creatinine in serum, lactate dehydrogenase, kidney malondialdehyde, NF-κB, Bax, and annexin V...
April 5, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28374099/dalbergioidin-dal-protects-mc3t3-e1-osteoblastic-cells-against-h2o2-induced-cell-damage-through-activation-of-the-pi3k-akt-smad1-pathway
#12
Yu-Qin Jin, Jia-Ling Li, Jin-Dong Chen, Chang-Liang Xu, Huang Li
Reactive oxygen species (ROS) is a pivotal pathogenic factor in the development of osteoporosis. Dalbergioidin (DAL) can be isolated from Uraria crinite, an edible herb used as a natural food for childhood skeletal dysplasia. Recent research has implicated DAL as having an antiosteoporosis effect, although the mechanism of this is unclear. We used an effective oxidative stress model, induced by hydrogen peroxide (H2O2) in osteoblastic MC3T3-E1 cells, to investigate the protective effects of DAL in osteoporosis and the underlying molecular mechanisms...
April 3, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28365825/inhibition-of-inwardly-rectifying-kir2-x-channels-by-the-novel-anti-cancer-agent-gambogic-acid-depends-on-both-pore-block-and-pip2-interference
#13
Daniel Scherer, Benedikt Schworm, Claudia Seyler, Panagiotis Xynogalos, Eberhard P Scholz, Dierk Thomas, Hugo A Katus, Edgar Zitron
The caged xanthone gambogic acid (GA) is a novel anti-cancer agent which exhibits anti-proliferative, anti-inflammatory and cytotoxic effects in many types of cancer tissues. In a recent phase IIa study, GA exhibits a favourable safety profile. However, limited data are available concerning its interaction with cardiac ion channels. Heteromeric assembly of Kir2.x channels underlies the cardiac inwardly rectifying IK1 current which is responsible for the stabilization of the diastolic resting membrane potential...
April 2, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28365824/gastroprotective-potential-of-methanolic-extract-and-dimethyl-cardamonin-from-campomanesia-reitziana-fruits-in-mice
#14
Carolina de Oliveira Cabral, Adriana Campos, Luisa Mota da Silva, Thaise Boeing, Sérgio Faloni de Andrade, Valdir Cechinel Filho, Luciane Ângela Nottar Nesello
This study evaluated the gastroprotective potential of methanolic extract from fruits of Campomanesia reitziana (MECR) and its isolated chalcone dimethyl cardamonin (DMC). The phenolic compound in the extract, and the free radical scavenging activity of MECR and DMC, were quantified. The gastroprotective activity of MECR (30-300 mg/kg, p.o) and DMC (1 and 3 mg/kg, p.o) was determined by ethanol/HCl-induced gastric ulcers in mice. Histological, histochemical, and biochemical analyses were performed in the ulcerated tissue...
April 1, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28361247/the-potential-curative-effect-of-rebamipide-in-hepatic-ischemia-reperfusion-injury
#15
Abdallah M Gendy, Dalaal M Abdallah, Hanan S El-Abhar
Rebamipide (Reba), a gastroprotective drug, has signified its hepatoprotective activity; however, its possible post-therapeutic intervention in hepatic ischemia/reperfusion (I/R) remains elusive. Consequently, the intent of this study was to test Reba modulatory effect on nuclear factor (NF)-κB signaling in hepatic I/R model. Rats were randomized into sham, I/R, Reba 60, and Reba100 (60 and 100 mg/kg, respectively) groups. Ischemia was induced for 30 min followed by 3-day reperfusion to set up a model of partial (70%) warm hepatic ischemia...
March 30, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28357464/monosodium-glutamate-associated-alterations-in-open-field-anxiety-related-and-conditioned-place-preference-behaviours-in-mice
#16
Olakunle James Onaolapo, Olaleye Samuel Aremu, Adejoke Yetunde Onaolapo
The present study investigated changes in behaviour associated with oral monosodium glutamate (a flavouring agent), using the open field, elevated plus maze and conditioned place preference (CPP) paradigms, respectively. Mice were assigned to two groups for CPP [monosodium glutamate (MSG)-naïve (n = 40) and MSG-pretreated (n = 40)] and two groups for open field (OF) and elevated plus maze (EPM) tests [n = 40 each], respectively. Animals in respective groups were then divided into four subgroups (n = 10) (vehicle or MSG (80, 160 and 320 mg/kg))...
March 29, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28349183/resveratrol-protects-the-loss-of-connexin-43-induced-by-ethanol-exposure-in-neonatal-mouse-cardiomyocytes
#17
Su Tu, Fu-Tao Cao, Xiao-Chun Fan, Cheng-Jian Yang
Excessive alcohol consumption provides risk to cardiomyopathy with unknown mechanisms. Resveratrol, a plant polyphenol, is widely reported for its cardiovascular benefits, while its effect on alcohol-induced impairments in cardiomyocytes largely remains unknown. Effects of resveratrol on the cardiomyocytes under ethanol insult were studied in vitro. Ethanol exposure in mouse neonatal cardiomyocytes increased cell death and induced a specific loss of tight junction protein, connexin 43. In spite of adverse effects at higher concentrations, resveratrol at 10 μM improved cell viability of cardiomyocytes in the presence of a deleterious dose of ethanol...
March 28, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28331977/role-of-plasma-membrane-associated-akaps-for-the-regulation-of-cardiac-ik1-current-by-protein-kinase-a
#18
Claudia Seyler, Daniel Scherer, Christoph Köpple, Martin Kulzer, Sevil Korkmaz, Panagiotis Xynogalos, Dierk Thomas, Ziya Kaya, Eberhard Scholz, Johannes Backs, Christoph Karle, Hugo A Katus, Edgar Zitron
The cardiac IK1 current stabilizes the resting membrane potential of cardiomyocytes. Protein kinase A (PKA) induces an inhibition of IK1 current which strongly promotes focal arrhythmogenesis. The molecular mechanisms underlying this regulation have only partially been elucidated yet. Furthermore, the role of A-kinase anchoring proteins (AKAPs) in this regulation has not been examined to date. The objective of this project was to elucidate the molecular mechanisms underlying the inhibition of IK1 by PKA and to identify novel molecular targets for antiarrhythmic therapy downstream β-adrenoreceptors...
March 22, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28280849/a-novel-synthetic-derivative-of-squamosamide-flz-inhibits-the-high-mobility-group-box-1-protein-mediated-neuroinflammatory-responses-in-murine-bv2-microglial-cells
#19
De-Chuan Li, Xiu-Qi Bao, Xiao-Liang Wang, Hua Sun, Dan Zhang
High mobility group box 1 (HMGB1) is a critical pro-inflammatory cytokine that contributes to the pathogenesis of various human diseases. FLZ, a squamosamide derivative, has been demonstrated to have neuroprotective effects in Parkinson's disease models and shows strong anti-inflammatory activity, while the precise mechanism remains unclear. Here, we investigated the anti-inflammatory mechanism of FLZ on HMGB1-mediated inflammatory responses. The effects of FLZ on HMGB1 release from microglial cells induced by lipopolysaccharide were first explored by Western blot assay and ELISA...
March 9, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28265686/inhibition-of-cloned-herg-potassium-channels-by-risperidone-and-paliperidone
#20
Hong Joon Lee, Jin-Sung Choi, Bok Hee Choi, Sang June Hahn
Risperidone and one of its active metabolites, paliperidone, are widely used for the treatment of schizophrenia. We used a patch-clamp study to investigate the effects of paliperidone on hERG potassium channels expressed in HEK cells. Western blot analyses were used to study the effects of risperidone and paliperidone on hERG and hERG 3.1 isoform channel trafficking. Risperidone and paliperidone inhibited the hERG tail currents in a concentration-dependent manner with IC50 values of 0.16 and 0.57 μM, respectively...
March 6, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
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