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Naunyn-Schmiedeberg's Archives of Pharmacology

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https://www.readbyqxmd.com/read/28331977/role-of-plasma-membrane-associated-akaps-for-the-regulation-of-cardiac-ik1-current-by-protein-kinase-a
#1
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
#2
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
#3
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
https://www.readbyqxmd.com/read/28229171/potential-biomarkers-associated-with-oxidative-stress-for-risk-assessment-of-colorectal-cancer
#4
REVIEW
Paramita Mandal
Cells are continuously threatened by the damage caused by reactive oxygen/nitrogen species (ROS/RNS), which are produced during physiological oxygen metabolism. In our review, we will summarize the latest reports on the role of oxidative stress and oxidative stress-induced signaling pathways in the etiology of colorectal cancer. The differences in ROS generation may influence the levels of oxidized proteins, lipids, and DNA damage, thus contributing to the higher susceptibility of colon. Reactive species (RS) of various types are formed and are powerful oxidizing agents, capable of damaging DNA and other biomolecules...
February 22, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28229170/molecular-insight-of-arsenic-induced-carcinogenesis-and-its-prevention
#5
REVIEW
Paramita Mandal
Population of India and Bangladesh and many other parts of the world are badly exposed to arsenic through drinking water. Due to non-availability of safe drinking water, they are dependent on arsenic-contaminated water. Generally, poverty level is high in those areas with lack of proper nutrition. Arsenic is considered to be an environmental contaminant and widely distributed in the environment due to its natural existence and anthropogenic applications. Contamination of arsenic in both human and animal could occur through air, soil, and other sources...
February 22, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28224182/parp-inhibition-ameliorates-nephropathy-in-an-animal-model-of-type-2-diabetes-focus-on-oxidative-stress-inflammation-and-fibrosis
#6
Esraa M Zakaria, Nabila N El-Maraghy, Ahmed F Ahmed, Abdelmonim A Ali, Hany M El-Bassossy
Poly(ADP-ribose) polymerase (PARP) enzyme contributes to nephropathy, a serious diabetic complication which may lead to end-stage renal disease. The study aims to investigate the effect of PARP over-activation on kidney functions in a type 2 diabetic rat model. The study also tests the therapeutic use of PARP inhibitors in diabetic nephropathy. Type 2 diabetes was induced in adult male rats by high-fructose/high-fat diet and low streptozotocin dose. Then, the PARP inhibitor 4-aminobenzamide (4-AB) was administered daily for 10 weeks...
February 21, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28220212/rho-kinase-inhibition-ameliorates-cyclophosphamide-induced-cystitis-in-rats
#7
Andrzej Wróbel, Urszula Doboszewska, Ewa Rechberger, Karol Rojek, Anna Serefko, Ewa Poleszak, Krystyna Skalicka-Woźniak, Jarosław Dudka, Piotr Wlaź
Hemorrhagic cystitis often develops in patients treated with cyclophosphamide (CYP). Studies have indicated that Rho kinase (ROCK) inhibitors may suppress detrusor overactivity symptoms and possess anti-inflammatory properties. The aim of the present study was to investigate whether inhibition of ROCK reduces cystometric and histopathological changes associated with CYP-induced cystitis. The rats received GSK 269962, a ROCK inhibitor, at a dose of 30 mg/kg daily, or vehicle for 7 days. Then, acute chemical cystitis leading to bladder overactivity was induced by CYP injection (200 mg/kg i...
February 21, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28220211/competitive-association-binding-kinetic-assays-a-new-tool-to-detect-two-different-binding-orientations-of-a-ligand-to-its-target-protein-under-distinct-conditions
#8
Hans-Joachim Wittmann, Andrea Strasser
Within the last years, for several ligands, binding to G protein-coupled receptors or other target proteins, a binding of the ligand in two different orientations is described. One appropriate experimental technique to detect two different binding orientations is the crystallization of the ligand-protein-complex, but crystallization and subsequent X-ray analysis do not belong to the routine methods. By traditional competitive radioligand equilibrium binding assays, it is not possible to detect or to distinguish between two different binding orientations, but there is a possibility to identify two different binding orientations by performing kinetic competitive radioligand-binding assays...
February 20, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28220210/applicability-of-in-vitro-in-vivo-translation-of-cathepsin-k-inhibition-from-animal-species-to-human-with-the-use-of-free-drug-hypothesis
#9
Bennett Ma, Bin Luo, Danielle H Euler, Tara E Cusick, Gregg Wesolowski, Helmut Glantschnig, Le T Duong, Yangsi Ou, Steven S Carroll, Laura S Lubbers
The correlation of in vitro inhibition of cathepsin K (CatK) activity and in vivo suppression of collagen I biomarkers was examined with three selective CatK inhibitors to explore the potential translatability from animal species to human. These inhibitors exhibited good in vitro potencies toward recombinant CatK enzymes across species, with IC50 values ranging from 0.20 to 6.1 nM. In vivo studies were conducted in animal species following multiple-day dosing of the CatK inhibitors to achieve steady-state plasma drug concentration-time profiles...
February 20, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28210753/puerarin-7-o-glucuronide-a-water-soluble-puerarin-metabolite-prevents-angiotensin-ii-induced-cardiomyocyte-hypertrophy-by-reducing-oxidative-stress
#10
Ning Hou, Bin Cai, Cai-Wen Ou, Zhen-Hui Zhang, Xia-Wen Liu, Mu Yuan, Gan-Jian Zhao, Shi-Ming Liu, Long-Gen Xiong, Jian-Dong Luo, Cheng-Feng Luo, Min-Sheng Chen
This study aimed to investigate the anti-oxidant and anti-hypertrophic effects of puerarin-7-O-glucuronide, a water-soluble puerarin metabolite. The anti-oxidant effects of puerarin-7-O-glucuronide were assessed by measurement of intracellular superoxide levels, total superoxide dismutase (SOD) activity, total anti-oxidant capacity, and glutathione (GSH)/glutathione disulfide (GSSG) ratio in cultured neonatal rat cardiomyocytes (NRCMs) stimulated with the xanthine oxidase (XO)/xanthine (X) system or angiotensin II...
February 16, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28190245/pharmacokinetic-pharmacodynamic-modeling-of-the-antihypertensive-interaction-between-azilsartan-medoxomil-and-chlorthalidone-in-spontaneously-hypertensive-rats
#11
Santosh Kumar Puttrevu, Rachumallu Ramakrishna, Manisha Bhateria, Moon Jain, Kashif Hanif, Rabi Sankar Bhatta
A pharmacokinetic-pharmacodynamic (PK-PD) model was developed to describe the time course of blood pressure following oral administration of azilsartan medoxomil (AZM) and/or chlorthalidone (CLT) in spontaneously hypertensive (SH) rats. The drug concentration and pharmacological effects, including systolic blood pressure (SBP) and diastolic blood pressure (DBP) were measured by liquid chromatography-tandem mass spectrometry (LC-MS/MS) and tail-cuff manometry, respectively. Sequential PK-PD analysis was performed, wherein the plasma concentration-time data was modeled by one compartmental analysis...
February 11, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28190244/nadph-oxidase-its-potential-role-in-promotion-of-pulmonary-arterial-hypertension
#12
REVIEW
Jing-Jie Peng, Bin Liu, Jin-Yun Xu, Jun Peng, Xiu-Ju Luo
NADPH oxidases (NOXs) are a group of enzymes for superoxide anion (O2(·-) ) generation through transferring electrons from NADPH to molecular oxygen, which is rapidly converted into hydrogen peroxide (H2O2). There are seven members in NOX family, including NOX1 to NOX5, dual oxidase1, and dual oxidase 2. Recent studies have demonstrated that NOX subtypes may have different functions in different types of pulmonary arterial hypertension (PAH). The NOX-derived reactive oxygen species (ROS) are key factors that are involved in promoting the processes of pulmonary vascular remodeling, such as endothelial dysfunction, proliferation of pulmonary arterial smooth muscle cells (PASMCs), and cellular trans-differentiation, which are the basic pathologic characteristics of PAH...
February 11, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28190243/effect-of-short-term-androgen-deficiency-on-bladder-contractility-and-urothelial-mediator-release
#13
Giselle Bravo, Helen Massa, Roselyn Rose'Meyer, Russ Chess-Williams, Catherine McDermott, Donna J Sellers
In men, testosterone levels decline by 1% per year after the age of 40. Reduced androgen levels may directly contribute to lower urinary tract symptoms and bladder dysfunction, although the mechanisms are unclear. This study examined the effect of low testosterone and testosterone replacement on key mechanisms involved in local bladder function. Intraluminal release of the mediators ATP and ACh in response to bladder distension was measured in whole bladders from rats 8 weeks following castration, whilst bladder contractility was assessed using isolated strips...
February 11, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28188358/protective-effect-of-valproic-acid-in-streptozotocin-induced-sporadic-alzheimer-s-disease-mouse-model-possible-involvement-of-the-cholinergic-system
#14
Mirna Ezzat Sorial, Nesrine Salah El Dine El Sayed
Sporadic Alzheimer's disease (SAD) is a slowly progressive neurological disorder that is the most common form of dementia. Cholinergic system dysfunction and amyloid beta formation are the two main underlying pathological mechanisms for the disease development. In recent studies, insulin receptor desensitization and disturbances in the downstream effects of insulin receptor signaling were observed in the brains of Alzheimer's patients. Currently, intracereberoventricular (ICV) injection of streptozotocin (STZ) is found to induce behavioral, neurochemical, and structural alterations in animals resembling those found in SAD patients...
February 10, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28188357/analgesic-antiallodynic-and-anticonvulsant-activity-of-novel-hybrid-molecules-derived-from-n-benzyl-2-2-5-dioxopyrrolidin-1-yl-propanamide-and-2-2-5-dioxopyrrolidin-1-yl-butanamide-in-animal-models-of-pain-and-epilepsy
#15
Anna Rapacz, Krzysztof Kamiński, Jolanta Obniska, Paulina Koczurkiewicz, Elżbieta Pękala, Barbara Filipek
The purpose of the present study was to examine the analgesic activity of six novel hybrid molecules, which demonstrated in the previous research anticonvulsant activity in the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole seizure (scPTZ) tests in mice. The antinociceptive properties were estimated in three models of pain in mice-the hot plate test, the formalin test, and in the oxaliplatin-induced neuropathy. Moreover, extended anticonvulsant studies were carried out and the antiseizure activity was investigated in the 6-Hz test...
February 10, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28160016/nicotine-at-clinically-relevant-concentrations-affects-atrial-inward-rectifier-potassium-current-sensitive-to-acetylcholine
#16
Markéta Bébarová, Peter Matejovič, Olga Švecová, Roman Kula, Milena Šimurdová, Jiří Šimurda
Nicotine abuse is associated with variety of diseases including arrhythmias, most often atrial fibrillation (AF). Altered inward rectifier potassium currents including acetylcholine-sensitive current I K(Ach) are known to be related to AF pathogenesis. Since relevant data are missing, we aimed to investigate I K(Ach) changes at clinically relevant concentrations of nicotine. Experiments were performed by the whole cell patch clamp technique at 23 ± 1 °C on isolated rat atrial myocytes. Nicotine was applied at following concentrations: 4, 40 and 400 nM; ethanol at 20 mM (∼0...
February 3, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28160015/stimulation-of-%C3%AE-1-and-%C3%AE-2-adrenoceptors-dilates-retinal-blood-vessels-in-rats
#17
Asami Mori, Akane Sekito, Kenji Sakamoto, Kunio Ishii, Tsutomu Nakahara
Our previous studies have demonstrated that adrenaline dilates rat retinal arterioles by stimulating propranolol-sensitive β-adrenoceptors and β3-adrenoceptors, and selective stimulation of β2- or β3-adrenoceptors causes retinal vasodilator responses. In the present study, we compared the effects of β1- and β2-adrenoceptor stimulation on rat retinal arterioles in vivo. Rat ocular fundus images were captured using an original high-resolution digital fundus camera. Diameters of retinal arterioles contained in the images were measured...
February 3, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28144710/selective-venous-vasodilator-properties-of-the-analgesic-metamizole-dipyrone-in-a-human-ex-vivo-model-implications-for-postoperative-pain-management
#18
Markus Hoenicka, Hagen Gorki, Karl Traeger, Andreas Liebold
Metamizole (dipyrone) is a first-line, non-opioid analgesic used for postoperative pain management. Clinical data and animal experiments indicate a possible vasodilator action of this drug. We investigated the effects of metamizole on human artery and vein tone in an ex vivo model to assess potential contributions to venous pooling. Excess segments of bypass grafts were harvested during coronary artery bypass grafting procedures. Tensions were measured in an organ bath for 120 min after adding metamizole to the preconstricted vessels...
January 31, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28144709/glucagon-increase-after-chronic-at1-blockade-is-more-likely-related-to-an-indirect-leptin-dependent-than-to-a-pancreatic-%C3%AE-cell-dependent-mechanism
#19
Martin Mildner, Helge Müller-Fielitz, Ines Stölting, Olaf Jöhren, Muscha Steckelings, Walter Raasch
AT1 blockers (ARB) prevent diabetes by improving pancreatic β cell function. Less is known about whether α cells are affected although they express angiotensin II (AngII) receptors. We aimed to investigate glucagon release upon AngII stimulation. We determined glucagon release after AngII stimulation (0.01-100 μM) in α cells (InR1G9) and isolated murine islets. We determined plasma glucagon in rats that were chronically treated with AngII (9 μg/h) or the ARBs telmisartan (8 mg/kg/day) and candesartan (16 mg/kg/day) and correlated glucagon with additional hormones (e...
January 31, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28124089/evening-primrose-oil-or-forskolin-ameliorates-celecoxib-enhanced-upregulation-of-tissue-factor-expression-in-mice-subjected-to-lipopolysaccharide-induced-endotoxemia
#20
Sarah M Mosaad, Sawsan A Zaitone, Amal A M Ahmed, Dina M Abo-Elmatty, Amani A El-Baz, Yasser M Moustafa
Celecoxib, a selective cyclooxygenase-2 inhibitor, produces thrombotic events in patients predisposed to cardiovascular risk factors. One theory reported an increase in endothelial expression of tissue factor (TF) as a predisposing factor. This work explored the effect of evening primrose oil (EPO), a source of prostaglandin E1, and forskolin (a cyclic adenosine monophosphate stimulator) against the prothrombotic effect of celecoxib in mice. Lipopolysaccharide mouse model of endotoxemia was used to induce an upregulation of TF activity...
January 26, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
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