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https://www.readbyqxmd.com/read/28803116/efficient-molecularly-imprinted-polymer-as-a-pipette-tip-solid-phase-sorbent-for-determination-of-carvedilol-enantiomers-in-human-urine
#1
Anny Talita Maria da Silva, Hanna Leijoto de Oliveira, Camilla Fonseca Silva, Matheus Cecílio Fonseca, Thales Fernando Dias Pereira, Clebio Soares Nascimento, Eduardo Costa de Figueiredo, Keyller Bastos Borges
In this work, an efficient pipette tip based on molecularly imprinted polymers solid-phase extraction (PT-MIP-SPE) method was developed for carvedilol (CAR) analysis. This compound is available in clinical practice as a racemic mixture, in which (-)-(S)-CAR is a β- and α1-adrenergic antagonist, while (+)-(R)-CAR only acts as an α1-adrenergic antagonist. Enantioseparation of CAR presented satisfactory retention times (5.85 and 14.84min), acceptable theoretical plates (N=2048 and 2018) and good resolution (Rs=9...
August 1, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28802864/%C3%AE-3-adrenergic-receptor-regulates-hepatic-apolipoprotein-a-i-gene-expression
#2
Xiaojing Cao, Yanfang Li
BACKGROUND: β3-adrenergic receptor (β3-AR) was shown to upregulate hepatic apolipoprotein A-I (apoA-I) expression and reverse atherosclerotic plaques in vivo experiments. However, the effect of β3-AR on apoA-I expression in vitro is unknown. The specific mechanism underlying β3-AR prevention of atherosclerosis is unclear. OBJECTIVE: The present study was designed to investigate the molecular mechanism of β3-AR-mediated regulation of hepatic apoA-I gene expression...
July 27, 2017: Journal of Clinical Lipidology
https://www.readbyqxmd.com/read/28801655/%C3%AE-1-adrenergic-receptor-o-glycosylation-regulates-n-terminal-cleavage-and-signaling-responses-in-cardiomyocytes
#3
Misun Park, Gopireddy R Reddy, Gerd Wallukat, Yang K Xiang, Susan F Steinberg
β1-adrenergic receptors (β1ARs) mediate catecholamine actions in cardiomyocytes by coupling to both Gs/cAMP-dependent and Gs-independent/growth-regulatory pathways. Structural studies of the β1AR define ligand-binding sites in the transmembrane helices and effector docking sites at the intracellular surface of the β1AR, but the extracellular N-terminus, which is a target for post-translational modifications, typically is ignored. This study identifies β1AR N-terminal O-glycosylation at Ser(37)/Ser(41) as a mechanism that prevents β1AR N-terminal cleavage...
August 11, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28801517/effect-of-densely-ionizing-radiation-on-cardiomyocyte-differentiation-from-human-induced-pluripotent-stem-cells
#4
Erdene Baljinnyam, Sundararajan Venkatesh, Richard Gordan, Satvik Mareedu, Jianyi Zhang, Lai-Hua Xie, Edouard I Azzam, Carolyn K Suzuki, Diego Fraidenraich
The process of human cardiac development can be faithfully recapitulated in a culture dish with human pluripotent stem cells, where the impact of environmental stressors can be evaluated. The consequences of ionizing radiation exposure on human cardiac differentiation are largely unknown. In this study, human-induced pluripotent stem cell cultures (hiPSCs) were subjected to an external beam of 3.7 MeV α-particles at low mean absorbed doses of 0.5, 3, and 10 cGy. Subsequently, the hiPSCs were differentiated into beating cardiac myocytes (hiPSC-CMs)...
August 2017: Physiological Reports
https://www.readbyqxmd.com/read/28801400/protein-misfolding-amyotrophic-lateral-sclerosis-and-guanabenz-protocol-for-a-phase-ii-rct-with-futility-design-promise-trial
#5
Eleonora Dalla Bella, Irene Tramacere, Giovanni Antonini, Giuseppe Borghero, Margherita Capasso, Claudia Caponnetto, Adriano Chiò, Massimo Corbo, Roberto Eleopra, Massimiliano Filosto, Fabio Giannini, Enrico Granieri, Vincenzo La Bella, Christian Lunetta, Jessica Mandrioli, Letizia Mazzini, Sonia Messina, Maria Rosaria Monsurrò, Gabriele Mora, Nilo Riva, Romana Rizzi, Gabriele Siciliano, Vincenzo Silani, Isabella Simone, Gianni Sorarù, Paolo Volanti, Giuseppe Lauria
INTRODUCTION: Recent studies suggest that endoplasmic reticulum stress may play a critical role in the pathogenesis of amyotrophic lateral sclerosis (ALS) through an altered regulation of the proteostasis, the cellular pathway-balancing protein synthesis and degradation. A key mechanism is thought to be the dephosphorylation of eIF2α, a factor involved in the initiation of protein translation. Guanabenz is an alpha-2-adrenergic receptor agonist safely used in past to treat mild hypertension and is now an orphan drug...
August 11, 2017: BMJ Open
https://www.readbyqxmd.com/read/28801325/aluminium-phosphide-poisoning-with-severe-cardiac-dysfunction-and-the-role-of-digoxin
#6
Khalid Hamid Changal, Muzamil Latief, Manzoor Parry, Farhat Abbas
Aluminium phosphide (ALP) is a common cause of suicidal poisoning in India where it is easily available and commonly known as 'rice tablet'. In rural areas of India, it is still used to protect rice and stored grains from rodents and pests. (1) There is no specific antidote for phosphide poisoning and treatment involves meticulous supportive care. Ingestion can lead to severe cardiac suppression and cardiogenic shock. For patients poisoned with ALP who continue to have refractory shock with persistent myocardial suppression despite the use of adrenergic inotropic agents, the addition of digoxin may be beneficial...
August 11, 2017: BMJ Case Reports
https://www.readbyqxmd.com/read/28800452/identification-of-3-4-dihydro-2h-thiochromene-1-1-dioxide-derivatives-with-a-phenoxyethylamine-group-as-highly-potent-and-selective-%C3%AE-1d-adrenoceptor-antagonists
#7
Nobuki Sakauchi, Hideki Furukawa, Junya Shirai, Ayumu Sato, Haruhiko Kuno, Reiko Saikawa, Masato Yoshida
A series of phenoxyethylamine derivatives was designed and synthesized to discover potent and selective human α1D adrenoceptor (α1D adrenergic receptor; α1D-AR) antagonists. Compound 7 was taken from our internal compound collection as an attractive starting point and exhibited moderate binding affinity for α1D-AR and high selectivity against α1A- and α1B-ARs. We focused on modifying the 2-methylsulfonylbenzyl group of 7 to discover novel compounds structurally distinct from other reported α1-AR antagonists containing the phenoxyethylamine motif...
August 1, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28798477/er-k-linked-gpcr-g-protein-fusions-systematically-modulate-second-messenger-response-in-cells
#8
Rabia U Malik, Matthew Dysthe, Michael Ritt, Roger K Sunahara, Sivaraj Sivaramakrishnan
FRET and BRET approaches are well established for detecting ligand induced GPCR-G protein interactions in cells. Currently, FRET/BRET assays rely on co-expression of GPCR and G protein, and hence depend on the stoichiometry and expression levels of the donor and acceptor probes. On the other hand, GPCR-G protein fusions have been used extensively to understand the selectivity of GPCR signaling pathways. However, the signaling properties of fusion proteins are not consistent across GPCRs. In this study, we describe and characterize novel sensors based on the Systematic Protein Affinity Strength Modulation (SPASM) technique...
August 10, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28797476/temperature-effects-on-aerobic-scope-and-cardiac-performance-of-european-perch-perca-fluviatilis
#9
Denise Lyager Jensen, Johannes Overgaard, Tobias Wang, Hans Gesser, Hans Malte
Several recent studies have highlighted how impaired cardiac performance at high temperatures and in hypoxia may compromise the capacity for oxygen transport. Thus, at high temperatures impaired cardiac capacity is proposed to reduce oxygen transport to a degree that lowers aerobic scope and compromises thermal tolerance (the oxygen- and capacity-limited thermal tolerance (OCLTT) hypothesis). To investigate this hypothesis, we measured aerobic and cardiac performance of a eurythermal freshwater teleost, the European perch (Perca fluviatilis)...
August 2017: Journal of Thermal Biology
https://www.readbyqxmd.com/read/28795786/necroulcerative-hemorrhagic-gastritis-in-a-cat-secondary-to-the-administration-of-3-hydrogen-peroxide-as-an-emetic-agent
#10
Teresa D Obr, Joanna K Fry, Justine A Lee, Heidi A Hottinger
OBJECTIVE: To describe a case of necroulcerative gastritis in a cat secondary to administration of 3% hydrogen peroxide as an emetic agent. CASE SUMMARY: A 10-year-old neutered male domestic shorthair was evaluated for hematemesis less than 24 hours following ingestion of a piece of foam. The pet owner had administered 2 doses of 0.5-1.0 tablespoons (7.5-15 mL) of 3% hydrogen peroxide in an attempt to induce emesis at home; emesis was achieved and produced the foam foreign body...
August 10, 2017: Journal of Veterinary Emergency and Critical Care
https://www.readbyqxmd.com/read/28795305/microrna-133a-attenuates-cardiomyocyte-hypertrophy-by-targeting-pkc%C3%AE-and-gq
#11
Se-Yeon Lee, Chang Youn Lee, Onju Ham, Jae Yoon Moon, Jiyun Lee, Hyang-Hee Seo, Sunhye Shin, Sang Woo Kim, Seahyoung Lee, Soyeon Lim, Ki-Chul Hwang
During the past decade, microRNAs have continuously been suggested as a promising therapeutic tool due to their beneficial effects, such as their multi-targets and multi-functions in pathologic conditions. As a pathologic phenotype is generally regulated by multiple signaling pathways, in this study we identified a microRNA regulating multiple target genes within cardiac hypertrophic signaling pathways. microRNA-133a is known to play a crucial role in cardiac hypertrophy. However, the role of microRNA-133a, which may regulate several signaling pathways in norepinephrine-induced cardiac hypertrophy via multi-targeting, has not been investigated...
August 9, 2017: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/28795276/topiramate-via-nmda-ampa-kainate-gabaa-and-alpha2-receptors-and-by-modulation-of-creb-bdnf-and-akt-gsk3-signaling-pathway-exerts-neuroprotective-effects-against-methylphenidate-induced-neurotoxicity-in-rats
#12
Majid Motaghinejad, Manijeh Motevalian, Sulail Fatima, Tabassom Beiranvand, Shiva Mozaffari
Chronic abuse of methylphenidate (MPH) often causes neuronal cell death. Topiramate (TPM) carries neuroprotective effects, but its exact mechanism of action remains unclear. In the present study, the role of various doses of TPM and its possible mechanisms, receptors and signaling pathways involved against MPH-induced hippocampal neurodegeneration were evaluated in vivo. Thus, domoic acid (DOM) was used as AMPA/kainate receptor agonist, bicuculline (BIC) as GABAA receptor antagonist, ketamine (KET) as NMDA receptor antagonist, yohimbine (YOH) as α2 adrenergic receptor antagonist and haloperidol (HAL) was used as dopamine D2 receptor antagonist...
August 9, 2017: Journal of Neural Transmission
https://www.readbyqxmd.com/read/28795160/performance-and-in-house-validation-of-a-bioassay-for-the-determination-of-beta1-autoantibodies-found-in-patients-with-cardiomyopathy
#13
Katrin Wenzel, Sarah Schulze-Rothe, Annekathrin Haberland, Johannes Müller, Gerd Wallukat, Hanna Davideit
BACKGROUND: Autoantibodies specific for the adrenergic beta1-receptor were identified to be an essential factor for the pathogenesis of dilated cardiomyopathy. For the detection of these autoantibodies, a bioassay was developed and has been used, measuring the positive chronotropic effect on spontaneously beating neonatal rat cardiomyocytes. In order to use this bioassay as an analytical tool to monitor the effectiveness of autoantibody neutralizing therapy in a regulated field, there is a need to assess its analytical performance and validate it according to current guidelines...
July 2017: Heliyon
https://www.readbyqxmd.com/read/28794003/antenatal-early-postnatal-hypothyroidism-alters-arterial-tone-regulation-in-2-week-old-rats
#14
Svetlana I Sofronova, Dina K Gaynullina, Anastasia A Shvetsova, Anna A Borzykh, Ekaterina K Selivanova, Anna P Sharova, Andrey A Martyanov, Olga S Tarasova
The mechanisms of vascular alterations resulting from early thyroid hormones deficiency are poorly understood. We tested the hypothesis that antenatal/early postnatal hypothyroidism would alter the activity of endothelial NO-pathway and Rho-kinase pathway, which are specific for developing vasculature. Dams were treated with propylthiouracil (PTU, 7 ppm) in drinking water during gestation and 2 weeks after delivery, their progeny had normal body weight but markedly reduced blood levels of thyroid hormones (ELISA)...
August 9, 2017: Journal of Endocrinology
https://www.readbyqxmd.com/read/28793270/pancreatic-islet-blood-flow-dynamics-in-primates
#15
Juan A Diez, Rafael Arrojo E Drigo, Xiaofeng Zheng, Olga V Stelmashenko, Minni Chua, Rayner Rodriguez-Diaz, Masahiro Fukuda, Martin Köhler, Ingo Leibiger, Sai Bo Bo Tun, Yusuf Ali, George J Augustine, Veluchamy A Barathi, Per-Olof Berggren
Blood flow regulation in pancreatic islets is critical for function but poorly understood. Here, we establish an in vivo imaging platform in a non-human primate where islets transplanted autologously into the anterior chamber of the eye are monitored non-invasively and longitudinally at single-cell resolution. Engrafted islets were vascularized and innervated and maintained the cytoarchitecture of in situ islets in the pancreas. Blood flow velocity in the engrafted islets was not affected by increasing blood glucose levels and/or the GLP-1R agonist liraglutide...
August 8, 2017: Cell Reports
https://www.readbyqxmd.com/read/28791474/acetylcholine-nicotinic-receptor-subtypes-in-chromaffin-cells
#16
REVIEW
Manuel Criado
In the adrenal gland, acetylcholine released on stimulation of the sympathetic splanchnic nerve activates neuronal-type nicotinic receptors (nAChRs) in chromaffin cells and triggers catecholamine secretion. At least two subtypes of nAChRs have been described in bovine chromaffin cells. The main subtype, a heteromeric assembly of α3, β4 and perhaps α5 subunits, is involved in the activation step of the catecholamine secretion process and is not blocked by the snake toxin α-bungarotoxin. The other is α-bungarotoxin-sensitive, and its functional role has not yet been well defined...
August 8, 2017: Pflügers Archiv: European Journal of Physiology
https://www.readbyqxmd.com/read/28783759/senescence-as-a-novel-mechanism-involved-in-%C3%AE-adrenergic-receptor-mediated-cardiac-hypertrophy
#17
Rongrong Sun, Baoling Zhu, Kai Xiong, Yan Sun, Dandan Shi, Li Chen, Youyi Zhang, Zijian Li, Lixiang Xue
Pathological cardiac hypertrophy used to be elucidated by biomechanical, stretch-sensitive or neurohumoral mechanisms. However, a series of hints have indicated that hypertrophy process simulates senescence program. However, further evidence need to be pursued. To verify this hypothesis and examine whether cardiac senescence is a novel mechanism of hypertrophy induced by isoproterenol, 2-month-old male Sprague Dawley rats were subjected to isoproterenol infusion (0.25mg/kg/day) for 7 days by subcutaneous injection)...
2017: PloS One
https://www.readbyqxmd.com/read/28781164/imaging-sympathetic-neurogenic-ca-2-signaling-in-blood-vessels
#18
REVIEW
Withrow Gil Wier, Joseph R H Mauban
We review the information that has been provided by optical imaging experiments directed at understanding the role and effects of sympathetic nerve activity (SNA) in the functioning of blood vessels. Earlier studies utilized electric field stimulation of nerve terminals (EFS) in isolated arteries and vascular tissues (ex vivo) to elicit SNA, but more recently, imaging studies have been conducted in vivo, enabling the study of SNA in truly physiological conditions. Ex vivo: In vascular smooth muscle cells (VSMC) of isolated arteries, the three sympathetic neurotransmitters, norepinephrine (NE), ATP and neuropeptide Y (NPY), elicit or modulate distinct patterns of Ca(2+) signaling, as revealed by confocal imaging of exogenous fluorescent Ca(2+) indicators...
July 29, 2017: Autonomic Neuroscience: Basic & Clinical
https://www.readbyqxmd.com/read/28780894/gene-therapy-for-hypertension
#19
Ludovit Paulis, Heinrich Franke, Fedor Simko
The control of hypertension and the resulting cardiovascular events is still insufficient. Thus, the search for novel means for blood pressure (BP) reduction remains worth further clinical and research attention. The advances in vector and construct design sketch the use of gene therapy in hypertension. Areas covered: The authors have searched for studies using gene therapy in hypertension reporting BP outcomes. They have identified 63 experimental studies demonstrating feasible targeting of the classical and new renin-angiotensin-aldosterone system, β1-adrenergic receptor, NO-cGMP axis, endothelin, natriuretic peptides, kallikrein system, cytochrome P-450 hydroxylase, oncogenes, growth factors, interleukins, angiopoietin-1, adrenomedullin or Klotho in small rodents...
August 7, 2017: Expert Opinion on Biological Therapy
https://www.readbyqxmd.com/read/28780421/antihypertensive-drugs
#20
REVIEW
Stéphane Laurent
Successful treatment of hypertension is possible with limited side effects given the availability of multiple antihypertensive drug classes. This review describes the various pharmacological classes of antihypertensive drugs, under two major aspects: their mechanisms of action and side effects. The mechanism of action is analysed through a pharmacological approach, i.e. the molecular receptor targets, the various sites along the arterial system, and the extra-arterial sites of action, in order to better understand in which type of hypertension a given pharmacological class of antihypertensive drug is most indicated...
August 2, 2017: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
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