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https://www.readbyqxmd.com/read/28432819/identification-of-bioactive-compounds-in-shaoyao-gancao-decoction-using-%C3%AE-2-adrenoceptor-affinity-chromatography
#1
Zehua Li, Haiyang Gao, Jiangying Li, Yajun Zhang
Shaoyao-Gancao decoction, a Chinese herbal formula, is composed of Paeoniae Radix alba and Glycyrrhiza Radix et rhizoma. It has been widely used to treat muscle spasms and asthma. However, little is known about the bioactive components of Shaoyao-Gancao decoction. In the present study, the bioactive compounds in water-extract of Shaoyao-Gancao decoction were separated by the immobilized β2 -adrenoceptor affinity column and identified using quadrupole time-of-flight mass spectrometry. The affinity constants of the separated compounds that bound to β2 -adrenoceptor were determined by frontal analysis...
April 22, 2017: Journal of Separation Science
https://www.readbyqxmd.com/read/28432600/potentially-inappropriate-antihypertensive-prescriptions-to-elderly-patients-results-of-a-prospective-observational-study
#2
Paola H Ponte Márquez, Olga H Torres, Anonio San-José, Xavier Vidal, Antonia Agustí, Francesc Formiga, Alfonso López-Soto, Nieves Ramírez-Duque, Antonio Fernández-Moyano, Juana Garcia-Moreno, Juan A Arroyo, Domingo Ruiz
INTRODUCTION: Previous studies of antihypertensive treatment of older patients have focused on blood pressure control, cardiovascular risk or adherence, whereas data on inappropriate antihypertensive prescriptions to older patients are scarce. OBJECTIVES: The aim of the study was to assess inappropriate antihypertensive prescriptions to older patients. METHODS: An observational, prospective multicentric study was conducted to assess potentially inappropriate prescription of antihypertensive drugs, in patients aged 75 years and older with arterial hypertension (HTN), in the month prior to hospital admission, using four instruments: Beers, Screening Tool of Older Person's Prescriptions (STOPP), Screening Tool to Alert Doctors to the Right Treatment (START) and Assessing Care of Vulnerable Elders 3 (ACOVE-3)...
April 21, 2017: Drugs & Aging
https://www.readbyqxmd.com/read/28432535/exploring-the-carbamazepine-interaction-with-human-pregnane-x-receptor-and-effect-on-abcc2-using-in-vitro-and-in-silico-approach
#3
Gurpreet K Grewal, Khuraijam D Singh, Neha Kanojia, Chitra Rawat, Samiksha Kukal, Ajay Jajodia, Anshika Singhal, Richa Misra, Selvaraman Nagamani, Karthikeyan Muthusamy, Ritushree Kukreti
PURPOSE: Over expression of ATP-binding cassette transporters is considered one of the major reasons for non-responsiveness to antiepileptic drugs. Carbamazepine (CBZ), one of first line antiepileptic drug is known to influence ABCC2 expression but its exact molecular mechanism is unknown. METHODS: We investigated the effect of CBZ on expression of ABCC2 and pregnane X receptor (PXR) in HepG2 cell line and compared with hyperforin (agonist of PXR) and ketoconazole (antagonist of PXR) through realtime PCR and western blot assay...
April 21, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28432473/vasopressin-and-vasopressin-antagonists-in-heart-failure
#4
Julie K Vishram-Nielsen, Finn Gustafsson
Despite the introduction of multiple new pharmacological agents over the past three decades in the field of heart failure (HF), overall prognosis remains poor. Hyponatremia is prevalent in HF patients and has been suggested as a contributor to poor response to standard therapy. Elevated levels of arginine vasopressin (AVP), a peptide hormone produced in the hypothalamus, play a role in development of hyponatremia, and AVP and its surrogate, copeptin, are related to changes in osmolality, hemodynamics, neuro-hormones as well as in overall outcome in HF patients...
April 22, 2017: Handbook of Experimental Pharmacology
https://www.readbyqxmd.com/read/28432337/agarose-spot-as-a-comparative-method-for-in-situ-analysis-of-simultaneous-chemotactic-responses-to-multiple-chemokines
#5
Mohaned Ahmed, Haneen A Basheer, Jose M Ayuso, Djevdet Ahmet, Marco Mazzini, Roshan Patel, Steven D Shnyder, Victoria Vinader, Kamyar Afarinkia
We describe a novel protocol to quantitatively and simultaneously compare the chemotactic responses of cells towards different chemokines. In this protocol, droplets of agarose gel containing different chemokines are applied onto the surface of a Petri dish, and then immersed under culture medium in which cells are suspended. As chemokine molecules diffuse away from the spot, a transient chemoattractant gradient is established across the spots. Cells expressing the corresponding cognate chemokine receptors migrate against this gradient by crawling under the agarose spots towards their centre...
April 21, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28432191/gene-expression-effects-of-glucocorticoid-and-mineralocorticoid-receptor-agonists-and-antagonists-on-normal-human-skeletal-muscle
#6
Jessica A Chadwick, James Spencer Hauck, Celso E Gomez-Sanchez, Elise P Gomez-Sanchez, Jill A Rafael-Fortney
Mineralocorticoid and glucocorticoid receptors are closely related steroid hormone receptors that regulate gene expression through many of the same hormone response elements. However, their transcriptional activities and effects in skeletal muscles are largely unknown. We recently identified mineralocorticoid receptors (MR) in skeletal muscles after finding that combined treatment with the angiotensin-converting enzyme inhibitor lisinopril and MR antagonist spironolactone was therapeutic in Duchenne muscular dystrophy mouse models...
April 21, 2017: Physiological Genomics
https://www.readbyqxmd.com/read/28432157/effect-of-interleukin-6-inhibition-on-coronary-microvascular-and-endothelial-function-in-myocardial-infarction
#7
Espen Holte, Ola Kleveland, Thor Ueland, Gabor Kunszt, Marte Bratlie, Kaspar Broch, Annika E Michelsen, Bjørn Bendz, Brage H Amundsen, Svend Aakhus, Jan Kristian Damås, Lars Gullestad, Pål Aukrust, Rune Wiseth
OBJECTIVE: Interleukin-6 (IL-6) is a driver of inflammation and associated endothelial cell activation in acute coronary syndromes. We evaluated the effect of the IL-6 receptor antagonist tocilizumab on coronary microvascular function and endothelial dysfunction measured by coronary flow reserve (CFR) and markers of endothelial cell activation in patients with non-ST-elevation myocardial infarction (NSTEMI). METHODS: This substudy was part of a two-centre, double-blind, randomised, placebo-controlled trial evaluating the effect of a single dose of tocilizumab in NSTEMI...
April 21, 2017: Heart: Official Journal of the British Cardiac Society
https://www.readbyqxmd.com/read/28432149/cd73-on-t-cells-orchestrates-cardiac-wound-healing-after-myocardial-infarction-by-purinergic-metabolic-reprogramming
#8
Nadine Borg, Christina Alter, Nicole Görldt, Christoph Jacoby, Zhaoping Ding, Bodo Steckel, Christine Quast, Florian Bönner, Daniela Friebe, Sebastian Temme, Ulrich Flögel, Jürgen Schrader
Background -T-cells are required for proper healing after myocardial infarction. The mechanism of their beneficial action, however, is unknown. The pro-inflammatory "danger signal" adenosine triphosphate (ATP), released from damaged cells, is degraded by the ectonucleotidases CD39 and CD73 to the anti-inflammatory mediator adenosine. Here, we investigate the contribution of CD73-derived adenosine produced by T-cells to cardiac remodeling after ischemia/reperfusion and define its mechanism of action. Methods -Myocardial ischemia (50 min /reperfusion) was induced in global CD73(-/-) and CD4-CD73(-/-) mice...
April 21, 2017: Circulation
https://www.readbyqxmd.com/read/28432022/a-crosstalk-between-muscarinic-and-crf2-receptors-regulates-cellular-adhesion-properties-of-human-colon-cancer-cells
#9
M Pelissier-Rota, N T Chartier, B Bonaz, M R Jacquier-Sarlin
Patients with inflammatory bowel disease often suffer from chronic and relapsing intestinal inflammation that favor the development of colitis associated cancer. An alteration of the epithelial intestinal barrier function observed in IBD is supposed to be a consequence of stress. It has been proposed that corticotrophin-releasing factor receptor (CRF2), one of the two receptors of CRF, the principal neuromediator of stress, acts on cholinergic nerves to induce stress-mediated epithelial barrier dysfunction...
April 18, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28431969/crfr1-in-the-ventromedial-caudate-putamen-modulates-acute-stress-enhanced-expression-of-cocaine-locomotor-sensitization
#10
Shuli Liu, Zhiyan Wang, Yijing Li, Xiaowei Sun, Feifei Ge, Mingda Yang, Xinjuan Wang, Na Wang, Junkai Wang, Cailian Cui
Repeated exposure to psychostimulants induces a long-lasting enhancement of locomotor activity called behavioral sensitization, which is often reinforced by stress after drug withdrawal. The mechanisms underlying these phenomena remain elusive. Here we explored the effects of acute stress 3 or 14 days after the cessation of chronic cocaine treatment on the expression of locomotor sensitization induced by a cocaine challenge in rats and the key brain region and molecular mechanism underlying the phenomenon. A single session of forced swimming, as an acute stress (administered 2 days after the cessation of cocaine), significantly enhanced the expression of cocaine locomotor sensitization 14 days after the final cocaine injection (challenge at 12 days after acute stress) but not 3 days after the cessation of cocaine (challenge at 1 day after acute stress)...
April 18, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28431901/clozapine-reduces-toll-like-receptor-4-nf-%C3%AE%C2%BAb-mediated-inflammatory-responses-through-inhibition-of-calcium-calmodulin-dependent-akt-activation-in-microglia
#11
Seunghyun Jeon, Se Hyun Kim, Soon Young Shin, Young Han Lee
Clozapine is an atypical antipsychotic agent used in the treatment of schizophrenia and severe mood disorders. Accumulating evidence suggests that neuroinflammation is closely associated with the pathogenesis of various neurodegenerative diseases and psychiatric disorders. Clozapine exerts anti-inflammatory activity. However, the molecular mechanism underlying the anti-inflammatory activity of clozapine is poorly understood. In this study, we found that clozapine suppressed lipopolysaccharide (LPS)-induced phosphorylation of IκBα at Ser-32 and of p65/RelA at Ser-468, as well as nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB)-dependent transcriptional activity in microglial cells...
April 18, 2017: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/28431780/tolterodine-tartrate
#12
Gennady Ananchenko, Jasmina Novakovic
Tolterodine tartrate belongs to the family of muscarinic receptor antagonists and is indicated for the treatment of overactive urinary bladder syndrome. This chapter provides an overview of physical, analytical, and ADME profiles; highlights methods of chemical synthesis; and discusses stability of tolterodine as a free base and/or its l-tartrate salt in solution and in the solid state. The information presented in this chapter is based on the peer-reviewed literature, compendial reports (USP, EP), and authors' data...
2017: Profiles of Drug Substances, Excipients, and related Methodology
https://www.readbyqxmd.com/read/28431685/galr3-mediates-galanin-proliferative-effects-on-postnatal-hippocampal-precursors
#13
D Khan, M Khan, Johan Runesson, M Zaben, W P Gray
Galanin, a neuropeptide co-released from noradrenergic and serotonergic projection neurons to the dentate gyrus, has recently emerged as an important mediator for signaling neuronal activity to the subgranular neurogenic stem cell niche supporting adult hippocampal neurogenesis. Galanin and its receptors appear to play key roles in depression-like behavior, and effects on hippocampal neurogenesis are relevant to pharmacological strategies for treating depression, which in part appear to rely on restoring altered neurogenesis...
April 5, 2017: Neuropeptides
https://www.readbyqxmd.com/read/28431630/kynurenic-acid-and-its-analogue-can-alter-the-opioid-receptor-g-protein-signaling-after-acute-treatment-via-nmda-receptor-in-rat-cortex-and-striatum
#14
Reza Samavati, Ferenc Zádor, Edina Szűcs, Bernadett Tuka, Diána Martos, Gábor Veres, Róbert Gáspár, István M Mándity, Ferenc Fülöp, László Vécsei, Sándor Benyhe, Anna Borsodi
Previously, we have shown that the N-methyl d-aspartate (NMDA)-receptor antagonist kynurenic acid (KYNA) and its analogue KYNA1 do not bind directly to mu, kappa and delta opioid receptors in vitro. On the other hand, chronic administration of KYNA and KYNA1 resulted in region (cortex vs striatum) and opioid receptor-type specific alterations in G-protein activation of mouse brain homogenates. Here we describe for the first time the acute effect of KYNA and KYNA1 on opioid receptor function with the possible involvement of the NMDA receptor...
May 15, 2017: Journal of the Neurological Sciences
https://www.readbyqxmd.com/read/28431607/sigma-1-receptor-in-brain-ischemia-reperfusion-possible-role-in-the-nr2a-induced-pathway-to-regulate-brain-derived-neurotrophic-factor
#15
Qian Xu, Xue-Fei Ji, Tian-Yan Chi, Peng Liu, Ge Jin, Ling Chen, Li-Bo Zou
Sigma-1 receptor (σ1r) activation could attenuate the learning and memory deficits in the AD model, ischemia model and others. In our previous study, the activation of σ1r increased the expression of brain-derived neurotrophic factor (BDNF), possibly through the NR2A-induced pathway, and σ1r agonists might function as neuroprotectant agents in vascular dementia. Here, we used σ1r knockout mice to confirm the role of σ1r. Furthermore, an antagonist of NR2A was first used to investigate whether the NR2A-induced pathway is the necessary link between σ1r and BDNF...
May 15, 2017: Journal of the Neurological Sciences
https://www.readbyqxmd.com/read/28431434/bright-light-suppresses-form-deprivation-myopia-development-with-activation-of-dopamine-d1-receptor-signaling-in-the-on-pathway-in-retina
#16
Si Chen, Zhina Zhi, Qingqing Ruan, Qingxia Liu, Fen Li, Fen Wan, Peter S Reinach, Jiangfan Chen, Jia Qu, Xiangtian Zhou
Purpose: To determine whether dopamine receptor D1 (D1R) signaling pathway activation by bright light (BL) in specific retinal neuronal cell types contributes to inhibiting form-deprivation myopia (FDM) in mice. Methods: Mice (3-weeks old) were raised under either normal light (NL: 100-200 lux) or BL (2500-5000 lux) conditions with or without form deprivation. Refraction changes were evaluated with an eccentric infrared photorefractor, and ocular axial components with optical coherence tomography...
April 1, 2017: Investigative Ophthalmology & Visual Science
https://www.readbyqxmd.com/read/28431287/age-and-gender-effects-of-11-c-itmm-binding-to-metabotropic-glutamate-receptor-type-1-in-healthy-human-participants
#17
Muneyuki Sakata, Jun Toyohara, Kenji Ishibashi, Kei Wagatsuma, Kenji Ishii, Ming-Rong Zhang, Kiichi Ishiwata
We examined possible age- and gender-related changes in binding of the selective antagonist N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-4-(11)C-methoxy-N-methylbenzamide ((11)C-ITMM) to metabotropic glutamate receptor type 1 in healthy human brains. Dynamic (11)C-ITMM positron emission tomography scans (90 min) with serial arterial blood sampling were performed in 15 young and 24 older healthy adult volunteers. The total distribution volume (VT) of several brain regions was estimated with 2-tissue compartment model analysis...
March 28, 2017: Neurobiology of Aging
https://www.readbyqxmd.com/read/28431111/correction-of-abnormal-b-cell-subset-distribution-by-interleukin-6-receptor-blockade-in-polymyalgia-rheumatica
#18
Guillermo Carvajal Alegria, Valérie Devauchelle-Pensec, Yves Renaudineau, Alain Saraux, Jacques-Olivier Pers, Divi Cornec
Objectives.: The aim was to study lymphocyte subsets and circulating cytokines at diagnosis of PMR and after tocilizumab monotherapy. Methods.: Eighteen untreated patients with PMR were included in a prospective study and received 3-monthly tocilizumab infusions without glucocorticoids. Lymphocyte subset distribution was assessed by flow cytometry and serum cytokines were assayed by a 34-cytokine array and ELISA, at baseline and during follow-up. Baseline data were also compared with age- and sex-matched controls...
April 20, 2017: Rheumatology
https://www.readbyqxmd.com/read/28430981/central-nervous-system-glp-1-receptors-regulate-islet-hormone-secretion-and-glucose-homeostasis-in-male-rats
#19
Lene Jessen, Eric P Smith, Yvonne Ulrich-Lai, James P Herman, Randy J Seeley, Darleen Sandoval, David D'Alessio
The glucagon-like peptide 1 (GLP-1) system plays an important role in blood glucose regulation, in great part through coordinate control of insulin and glucagon secretion. These effects are generally attributed to GLP-1 produced in peripheral sites, principally the intestine. GLP-1 is also produced in hindbrain neurons that signal through GLP-1 receptors (GLP-1r) expressed in brain regions involved in metabolic regulation. GLP-1 in the central nervous system (CNS) induces satiety, visceral illness, and stress responses...
April 18, 2017: Endocrinology
https://www.readbyqxmd.com/read/28430979/effect-of-physical-exercise-and-acute-escitalopram-on-the-excitability-of-brain-monoamine-neurons-in-vivo-electrophysiological-study-in-rats
#20
Eliyahu Dremencov, Kristína Csatlósová, Barbora Durišová, Lucia Lapínová, Lubica Lacinová, Daniela Ježová
Background: The antidepressant effect of physical exercise has been reported in several clinical and animal studies. Since serotonin (5-HT), norepinephrine and dopamine play a central role in depression, it is possible that the beneficial effects of physical exercise are mediated via monoamine pathways. This study investigates the effects of voluntary wheel running (VWR) on the excitability of monoamine neurons. Material and methods: Male Sprague-Dawley rats were used in the study...
April 18, 2017: International Journal of Neuropsychopharmacology
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