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Calcium Antagonist

Douglas J Hermes, Changqing Xu, Justin L Poklis, Micah J Niphakis, Benjamin F Cravatt, Ken Mackie, Aron H Lichtman, Bogna M Ignatowska-Jankowska, Sylvia Fitting
The HIV-1 transactivator of transcription (Tat) is a neurotoxin involved in the pathogenesis of HIV-1 associated neurocognitive disorders (HAND). The neurotoxic effects of Tat are mediated directly via AMPA/NMDA receptor activity and indirectly through neuroinflammatory signaling in glia. Emerging strategies in the development of neuroprotective agents involve the modulation of the endocannabinoid system. A major endocannabinoid, anandamide (N-arachidonoylethanolamine, AEA), is metabolized by fatty acid amide hydrolase (FAAH)...
August 13, 2018: Neuropharmacology
Mun Fei Yam, Chu Shan Tan, Ruan Shibao
Orthosiphon stamineus Benth. (Lambiaceae) is an important traditional plant for the treatment of hypertension. Previous studies have demonstrated that the sinensetin content in O. stamineus is correlated with its vasorelaxant activity. However, there is still very little information regarding the vasorelaxant effect of sinensetin due to a lack of scientific studies. Therefore, the present study was designed to investigate the underlying mechanism of action of sinensetin in vasorelaxation using an in vitro precontraction aortic ring assay...
August 15, 2018: Hypertension Research: Official Journal of the Japanese Society of Hypertension
Douglas E Brenneman, Dean Petkanas, William A Kinney
Cannabidiol (CBD) exhibits neuroprotective properties in many experimental systems. However, development of CBD as a drug has been confounded by the following: (1) low potency; (2) a large number of molecular targets; (3) marginal pharmacokinetic properties; and (4) designation as a schedule 1 controlled substance. The present work compared the properties of CBD with a novel molecule (KLS-13019) that has structural similarities to CBD. The design strategy for KLS-13019 was to increase hydrophilicity while optimizing neuroprotective potency against oxidative stress toxicity relevant to hepatic encephalopathy...
August 14, 2018: Journal of Molecular Neuroscience: MN
Sara R Oliveira, Cláudia Figueiredo-Pereira, Carlos B Duarte, Helena L A Vieira
Carbon monoxide (CO) is an endogenous gasotransmitter that limits inflammation and prevents apoptosis in several tissues, including the brain. Low concentrations of CO are cytoprotective in astrocytes, neurons, and microglia, but the underlying molecular mechanisms remain poorly understood. This work aims at identification of alterations in gene expression conferred by CO in primary cultures of cortical astrocytes, for further disclosure of the molecular mechanism of action of the gasotransmitter. Astrocytes were treated with the CO-releasing molecule CORM-A1 for 40 min, and transcriptional changes were analyzed using RNASeq...
August 13, 2018: Molecular Neurobiology
Julian M C Choy, Fransiscus A Agahari, Li Li, Christian Stricker
Somatosensory cortex is innervated by afferents originating from the locus coeruleus which typically release noradrenaline. We tested if activation of presynaptic α1 -adrenoceptors (AR) coupled to a Gq -mediated signaling cascade resulted in calcium (Ca2+ ) release from stores and thereby increased spontaneous transmitter release in rat barrel cortex. Adding 1-100 μM noradrenaline (NA) or 5 μM cirazoline (CO), a α1 -AR specific agonist, to the standard artificial cerebrospinal fluid increased the frequency of miniature excitatory postsynaptic currents (mEPSC) by 64 ± 7% in 51% of pyramidal cells in layer II (responders) with no effect on the amplitude...
2018: Frontiers in Cellular Neuroscience
Yu Wang, Ying Zhou, Pei-Jun Li, Xi-Xi Wang, Ke-Zhou Cai, Cong-Gui Chen
The combined effect of calcium chloride (CaCl2 ) (20-100 mM) and high pressure processing (HPP, 200 MPa) on the solubility of myofibrillar proteins (MP) was investigated under sodium-reduced conditions (0.3 M sodium chloride). The results revealed that HPP combined with low concentrations (<40 mM) of CaCl2 synergistically increased the solubility of MP, but an antagonistic effect occurred when a high concentration (100 mM) of CaCl2 was present. This synergistic effect could be attributed to a mildly destabilized conformation of myosin, an increased surface hydrophobicity and the decreased total sulfhydryl group content of MP...
December 15, 2018: Food Chemistry
Stefan M Kolašinac, Slavoljub S Lekić, Jelena Golijan, Tanja Petrović, Goran Todorovic, Aleksandar Ž Kostić
The aim of this work was to determine elements composition and bioaccumulation process in ripe tomato fruits influenced by zinc feeding of plants which was applied in three different doses. Macro- and microelement content in growing soil, seeds, and fruits was determined by ICP-OES method. Health risk assessment was calculated according to the presence of some toxic elements. It was found that predominant macroelements were phosphorus, potassium, calcium, and magnesium followed by other ten determined elements...
August 10, 2018: Environmental Monitoring and Assessment
Febrina A Saputri, Devinna Kang, Arif S W Kusuma, Taofik Rusdiana, Aliya N Hasanah, Mutakin, Ingrid S Surono, Hiroshi Koyama, Rizky Abdulah
Objective Probiotics are beneficial in human health. In this study, we investigated the effect of probiotics on absorption of amlodipine, a dihydropyridine calcium antagonist used in the treatment of angina and hypertension, in a rabbit model. Methods Lactobacillus plantarum IS-10506 probiotic was administered for 14 days to male New Zealand rabbits. Blood samples were collected before and after probiotic supplementation. Amlodipine (10 mg) was then administered to all groups. Blood samples from a marginal vein were withdrawn at 5, 15, 30, 60, and 120 minutes to determine amlodipine concentrations in rabbit plasma...
August 9, 2018: Journal of International Medical Research
Angela Balistrieri, Laura Hobohm, Trisha Srivastava, Angela Meier, Ross Corriden
Bisphenol-A is a synthetic organic compound frequently present in consumer plastics, including plastic-lined cans, water bottles, toys, and teeth sutures. Previous studies have shown that BPA can produce adverse health effects that include defects in reproductive function and altered prenatal/childhood development. However, little is known regarding the effects of BPA on immune function. In this study, we assessed the effect of BPA on human neutrophils, a critical component of the innate immune system's defense against pathogens...
August 8, 2018: American Journal of Physiology. Cell Physiology
Seema Ali, Jeremy Turner, Samuel J Fountain
Adipose tissue contains self-renewing multipotent cells termed mesenchymal stromal cells. In situ, these cells serve to expand adipose tissue by adipogenesis, but their multipotency has gained interest for use in tissue regeneration. Little is known regarding the repertoire of receptors expressed by adipose-derived mesenchymal stromal cells (AD-MSCs). The purpose of this study was to undertake a comprehensive analysis of purinergic receptor expression. Mesenchymal stromal cells were isolated from human subcutaneous adipose tissue and confirmed by flow cytometry...
August 7, 2018: Purinergic Signalling
Emily E Hohman, Joanna K Hodges, Meryl E Wastney, Pamela J Lachcik, Chun-Ya Han, Denise Dwyer, Munro Peacock, Paul J Kostenuik, Connie M Weaver
Serum calcium is maintained in a narrow range through regulation of Ca metabolism in the intestine, kidney, and bone. Calcium is incorporated and resorbed from bone during bone remodeling via cellular processes as well as by exchange. Both routes contribute to calcium homeostasis. To assess the magnitude of bone turnover contribution to calcium homeostasis we labeled bone with a Ca tracer and measured Ca release following stimulation or suppression of bone resorption. Young growing male rats (n = 162) were dosed with 45 Ca to label skeletal Ca...
August 2, 2018: Bone
Kazuhiko Mizukami, Hiroaki Kamada, Hiroyuki Yoshida, Ikuko Ishii, Eisuke Nozawa, Koichi Wada, Tohru Ugawa
We determined the pharmacologic profile of ASP7657, trans-4-[({[1-(quinolin-2-ylmethyl)-5-(trifluoromethyl)-1H-indol-7 yl] carbonyl} amino) methyl] cyclohexanecarboxylic acid methanesulfonate (1:1), a newly synthesized selective E-type prostaglandin (EP)4 receptor antagonist using several in vitro and in vivo experiments. ASP7657 exhibited high affinity for rat and human EP4 receptors, with Ki values of 6.02 nM and 2.21 nM, respectively. In addition, ASP7657 potently inhibited the PGE2 -induced cyclic adenosine monophosphate (cAMP) increase in Chinese hamster ovary (CHO) cells expressing rat EP4 receptors and human lymphoblastoid T (Jurkat) cells, with IC50 values of 0...
August 3, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Nair Olguín, Marie-Lena Müller, Eduard Rodríguez-Farré, Cristina Suñol
Methylmercury (MeHg) is an environmental toxicant with detrimental effects on the developing brain and adult nervous system. The main mechanisms identified include oxidative stress, changes in intracellular calcium, mitochondrial changes, inhibition of glutamate uptake, of protein synthesis and disruption of microtubules. However, little is known about mechanisms of protection against MeHg neurotoxicity. We found that resveratrol (10µM) and ascorbic acid (200µM) protected MeHg-induced cell death in primary cultures of cortical neurons...
July 31, 2018: Neurotoxicology
David Brieger, John Amerena, John R Attia, Beata Bajorek, Kim H Chan, Cia Connell, Ben Freedman, Caleb Ferguson, Tanya Hall, Haris M Haqqani, Jeroen Hendriks, Charlotte M Hespe, Joseph Hung, Jonathan M Kalman, Prashanthan Sanders, John Worthington, Tristan Yan, Nicholas A Zwar
Atrial fibrillation (AF) is increasing in prevalence and is associated with significant morbidity and mortality. The optimal diagnostic and treatment strategies for AF are continually evolving and care for patients requires confidence in integrating these new developments into practice. These clinical practice guidelines will assist Australian practitioners in the diagnosis and management of adult patients with AF. Main recommendations: These guidelines provide advice on the standardised assessment and management of patients with atrial fibrillation regarding: screening, prevention and diagnostic work-up; acute and chronic arrhythmia management with antiarrhythmic therapy and percutaneous and surgical ablative therapies; stroke prevention and optimal use of anticoagulants; and integrated multidisciplinary care...
August 2, 2018: Medical Journal of Australia
Sang Eun Park, Ji Hoon Song, Chansik Hong, Dong Eun Kim, Jee-Won Sul, Tae-Youn Kim, Bo-Ra Seo, Insuk So, Sang-Yeob Kim, Dong-Jun Bae, Mi-Ha Park, Hye Min Lim, In-Jeoung Baek, Antonio Riccio, Joo-Yong Lee, Woo Hyun Shim, Bumwoo Park, Jae-Young Koh, Jung Jin Hwang
Oxidative stress is a key mediator of neuronal death in acute brain injuries, such as epilepsy, trauma, and stroke. Although it is accompanied by diverse cellular changes, increases in levels of intracellular zinc ion (Zn2+ ) and calcium ion (Ca2+ ) may play a critical causative role in oxidative neuronal death. However, the mechanistic link between Zn2+ and Ca2+ dyshomeostasis in neurons during oxidative stress is not well-understood. Here, we show that the exposure of cortical neurons to H2 O2 led to a zinc-triggered calcium influx, which resulted in neuronal death...
July 31, 2018: Molecular Neurobiology
Xiaoyan Zhang, Junyu Wei, Yifan Huang, Wenbiao Shen, Xin Chen, Chungui Lu, Nana Su, Jin Cui
Our previous studies showed that hydrogen-rich water (HRW) promoted the biosynthesis of anthocyanin under UV-A in radish. However, molecular mechanism involved in the regulation of the anthocyanin biosynthesis is still unclear. In this study, the role of calcium (Ca2+ ) in HRW-promoted anthocyanin biosynthesis in radish sprouts hypocotyls under UV-A was investigated. The results showed that a positive effect of HRW on the content of cytosolic calcium and anthocyanin accumulation, mimicking the effects of induced CaCl2 ...
2018: Frontiers in Plant Science
Thomas Dahl Nissen, Christina Brock, Jens Lykkesfeldt, Erik Lindström, Leif Hultin
BACKGROUND: Cerebral evoked potentials (CEP) induced by colorectal distension (CRD) in conscious rats provides a novel method in studies of visceral sensitivity. The aim of this study was to explore the pharmacological effect on CEP of compounds known to reduce the visceromotor response to CRD. METHODS: Epidural electrodes were chronically implanted in eight female Sprague-Dawley rats. Evoked potentials were elicited by colorectal rapid balloon distensions (100 ms, 80 mmHg) and the effect of WIN55 (cannabinoid CB receptor agonist), clonidine (adrenergic α2 receptor agonist), MPEP (mGluR5 receptor antagonist), pregabalin (ligand of α2 δ subunits in voltage-gated calcium channels) and baclofen (GABA-B receptor agonist) on amplitudes and latency of CEP were determined...
July 27, 2018: Neuropharmacology
Diego Castro Musial, Regiane Miranda-Ferreira, Juan Fernando Padin, Juan Alberto Arranz-Tagarro, Alberto J Parra-Vitela, Aron Jurkiewicz, Antonio Garcia Garcia, Neide Hyppolito Jurkiewicz
Diabetes mellitus and hypertension are diseases that have are strongly correlated. A major factor in this correlation is the renin-angiotensin system (RAS), with the peptide angiotensin II being a key component. This study analyzed the impact of AT1R (Angiotensin Type 1 receptor) and AT2R (Angiotension Type 2 receptor) in atrial function. MAIN METHODS: to perform the experiments, Wistar Kyoto rats (WKY), Diabetic streptozotocin-induced (WKY) and Spontaneously Hypertensive Rats (SHR) were used, and stimulation of cardiovascular function was done by means of the following drugs: angiotensin II, novokinin and the antagonists losartan and PD123177...
July 30, 2018: Clinical and Experimental Pharmacology & Physiology
Tania Kamal, Taryn N Green, James I Hearn, Emma C Josefsson, Marie-Christine Morel-Kopp, Christopher M Ward, Matthew J During, Maggie L Kalev-Zylinska
<AbstractText Label="Background" NlmCategory="UNASSIGNED"> N -methyl-d-aspartate receptors (NMDARs) contribute calcium influx in megakaryocytic cells but their roles remain unclear; both pro- and anti-differentiating effects have been shown in different contexts. Objectives: The aim of this study was to clarify NMDAR contribution to megakaryocytic differentiation in both normal and leukemic cells. Methods: Meg-01, Set-2, and K-562 leukemic cell lines were differentiated using phorbol-12-myristate-13-acetate (PMA, 10 nmol L-1 ) or valproic acid (VPA, 500 μmol L-1 )...
January 2018: Research and Practice in Thrombosis and Haemostasis
Yue Dai, Yi Cheng, Brent Fedirchuk, Larry M Jordan, Junhao Chu
Cat lumbar motoneurons display changes in membrane properties during fictive locomotion. These changes include reduction of input resistance and afterhyperpolarization, hyperpolarization of voltage threshold and voltage-dependent excitation of the motoneurons. The state-dependent alteration of membrane properties lead to dramatic changes in frequency-current (F-I) relationship. The mechanism underlying these changes remains unknown. Using a motoneuron model combined with electrophysiological data, we investigated the channel mechanisms underlying the regulation of motoneuronal excitability and motor output...
July 25, 2018: Journal of Neurophysiology
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