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https://www.readbyqxmd.com/read/28445782/the-immunohistochemical-distribution-of-the-gabaa-receptor-%C3%AE-1-%C3%AE-2-%C3%AE-3-%C3%AE-2-3-and-%C3%AE-2-subunits-in-the-human-thalamus
#1
H J Waldvogel, M Munkle, W van Roon-Mom, H Mohler, R L M Faull
The GABAA receptor is the most abundant inhibitory receptor in the human brain and is assembled from a variety of different subunit subtypes which determines their pharmacology and physiology. To determine which GABAA receptor subunit proteins are found in the human thalamus we investigated the distribution of five major GABAA receptor subunits α1, α2, α3, β2,3 and γ2 using immunohistochemical techniques. The α1-, β2,3- and γ2- subunits which combine to form a benzodiazepine sensitive GABAA receptor showed the most intense levels of staining and were the most common subunits found throughout the human thalamus especially in the ventral and posterior nuclear groups...
April 23, 2017: Journal of Chemical Neuroanatomy
https://www.readbyqxmd.com/read/28442546/modeled-structural-basis-for-the-recognition-of-%C3%AE-2-3-sialyllactose-by-soluble-klotho
#2
Jon D Wright, Sung-Wan An, Jian Xie, Joonho Yoon, Nicole Nischan, Jennifer J Kohler, Noelynn Oliver, Carmay Lim, Chou-Long Huang
Soluble Klotho (sKlotho) is the shed ectodomain of antiaging membrane Klotho that contains 2 extracellular domains KL1 and KL2, each of which shares sequence homology to glycosyl hydrolases. sKlotho elicits pleiotropic cellular responses with a poorly understood mechanism of actions. Notably, in injury settings, sKlotho confers cardiac and renal protection by down-regulating calcium-permeable transient receptor potential canonical type isoform 6 (TRPC6) channels in cardiomyocytes and glomerular podocytes. Inhibition of PI3K-dependent exocytosis of TRPC6 is thought to be the underlying mechanism, and recent studies showed that sKlotho interacts with α2-3-sialyllactose-containing gangliosides enriched in lipid rafts to inhibit raft-dependent PI3K signaling...
April 25, 2017: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/28442369/further-evaluation-of-the-potential-anxiolytic-activity-of-imidazo-1-5-a-1-4-diazepin-agents-selective-for-%C3%AE-2-3-containing-gabaa-receptors
#3
J M Witkin, R Cerne, M Wakulchik, J S, S D Gleason, T M Jones, G Li, L A Arnold, Jun-Xu Li, J M Schkeryantz, K R Methuku, J M Cook, M M Poe
Positive allosteric modulators of GABAA receptors transduce a host of beneficial effects including anxiolytic actions. We have recently shown that bioavailability and anxiolytic-like activity can be improved by eliminating the ester functionality in imidazo[1,5-a][1,4]diazepines. In the present series of experiments, we further substantiate the value of heterocyle replacement of the ester for potential treatment of anxiety. None of the three esters was active in a Vogel conflict test in rats that detects anxiolytic drugs like diazepam...
April 22, 2017: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/28441717/dexmedetomidine-relieves-formaldehyde-induced-pain-in-rats-through-both-%C3%AE-2-adrenoceptor-and-imidazoline-receptor
#4
Hong Zhang, Xiang Yan, De-Gui Wang, Yu-Fang Leng, Zhan-Hai Wan, Yong-Qiang Liu, Yan Zhang
Dexmedetomidine (DEX) is a highly selective α2 adrenergic receptor agonist. In this study, we investigated the analgesic effect and the underlying mechanisms of DEX on inflammatory visceral pain in rats. Twenty-five male Sprague Dawley (SD) rats were randomly divided into 5 groups, including control, sham, low dose DEX, medium dose DEX and high dose DEX group. Pain was induced with 10% formalin and scored every 15min till 2 h-post the induction. Hematoxylin-eosin (HE) staining was used to evaluate the toxicity of DEX on spinal cord neurons...
April 21, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28438532/kinetic-properties-and-adrenergic-control-of-trek-2-like-channels-in-rat-medial-prefrontal-cortex-mpfc-pyramidal-neurons
#5
W Ładno, M Gawlak, P Szulczyk, E Nurowska
TREK-2-like channels were identified on the basis of electrophysiological and pharmacological tests performed on freshly isolated and enzymatically/mechanically dispersed pyramidal neurons of the rat medial prefrontal cortex (mPFC). Single-channel currents were recorded in cell-attached configuration and the impact of adrenergic receptors (α1, α2, β) stimulation on spontaneously appearing TREK-2-like channel activity was tested. The obtained results indicate that noradrenaline decreases the mean open probability of TREK-2-like channel currents by activation of β1 but not of α1- and α2-adrenergic receptors...
April 21, 2017: Brain Research
https://www.readbyqxmd.com/read/28433788/regulation-of-human-nucleus-pulposus-cells-by-peptide-coupled-substrates
#6
Devin T Bridgen, Bailey V Fearing, Liufang Jing, Johannah Sanchez-Adams, Megan C Cohan, Farshid Guilak, Jun Chen, Lori A Setton
Nucleus pulposus (NP) cells are derived from the notochord and differ from neighboring cells of the intervertebral disc in phenotypic marker expression and morphology. Adult human NP cells lose this phenotype and morphology with age in a pattern that contributes to progressive disc degeneration and pathology. Select laminin-mimetic peptide ligands and substrate stiffnesses were examined for their ability to regulate human NP cell phenotype and biosynthesis through the expression of NP-specific markers aggrecan, N-cadherin, collagen types I and II, and GLUT1...
April 19, 2017: Acta Biomaterialia
https://www.readbyqxmd.com/read/28429853/molecular-cloning-of-mda5-phylogenetic-analysis-of-rig-i-like-receptors-rlrs-and-differential-gene-expression-of-rlrs-interferons-and-proinflammatory-cytokines-after-in%C3%A2-vitro-challenge-with-ipnv-isav-and-sav-in-the-salmonid-cell-line-to
#7
I-K G Nerbøvik, M A Solheim, H Ø Eggestøl, A Rønneseth, R A Jakobsen, H I Wergeland, G T Haugland
The RIG-I receptors RIG-I, MDA5 and LGP2 are involved in viral recognition, and they have different ligand specificity and recognize different viruses. Activation of RIG-I-like receptors (RLRs) leads to production of cytokines essential for antiviral immunity. In fish, most research has focused on interferons, and less is known about the production of proinflammatory cytokines during viral infections. In this study, we have cloned the full-length MDA5 sequence in Atlantic salmon, and compared it with RIG-I and LGP2...
April 21, 2017: Journal of Fish Diseases
https://www.readbyqxmd.com/read/28425829/effects-of-dexmedetomidine-versus-midazolam-for-premedication-in-paediatric-anaesthesia-with-sevoflurane-a-meta-analysis
#8
Ji-Feng Feng, Xiao-Xia Wang, Yan-Yan Lu, Deng-Ge Pang, Wei Peng, Jian-Lan Mo
Background Dexmedetomidine (DEX), an α2-adrenergic receptor agonist, produces ideal sedation and early postoperative recovery for premedication in paediatric surgery, reducing preoperative anxiety and facilitating smooth induction of anaesthesia. We performed a meta-analysis to compare the effects of DEX and midazolam (MDZ) in paediatric anaesthesia with sevoflurane. Methods PubMed, Ovid, Web of Science, and Public Health Management Corporation were searched through December 2016 for randomized controlled trials (RCTs) that compared DEX and MDZ in children undergoing sevoflurane anaesthesia...
January 1, 2017: Journal of International Medical Research
https://www.readbyqxmd.com/read/28424537/awake-craniotomy-anesthetic-management-using-dexmedetomidine-propofol-and-remifentanil
#9
Andrea Prontera, Stefano Baroni, Andrea Marudi, Franco Valzania, Alberto Feletti, Francesca Benuzzi, Elisabetta Bertellini, Giacomo Pavesi
INTRODUCTION: Awake craniotomy allows continuous monitoring of patients' neurological functions during open surgery. Anesthesiologists have to sedate patients in a way so that they are compliant throughout the whole surgical procedure, nevertheless maintaining adequate analgesia and anxiolysis. Currently, the use of α2-receptor agonist dexmedetomidine as the primary hypnotic-sedative medication is increasing. METHODS: Nine patients undergoing awake craniotomy were treated with refined monitored anesthesia care (MAC) protocol consisting of a combination of local anesthesia without scalp block, low-dose infusion of dexmedetomidine, propofol, and remifentanil, without the need of airways management...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28424212/pdgf-receptor-%C3%AE-uses-akt-mtorc1-signaling-node-to-promote-high-glucose-induced-renal-proximal-tubular-cell-collagen-i-%C3%AE-2-expression
#10
Falguni Das, Nandini Ghosh-Choudhury, Balachandar Venkatesan, Balakuntalam S Kasinath, Goutam Ghosh Choudhury
Increased expression of PDGF receptor-β (PDGFRβ) has been shown in the diabetic renal proximal tubules. The core molecular network used by high glucose to induce proximal tubular epithelial cell collagen I (α2) expression is poorly understood. We hypothesized that activation of PDGFRβ by high glucose increases collagen I (α2) production via Akt/mTORC1 signaling pathway in proximal tubular epithelial cells. Using biochemical and molecular biological techniques, we investigated this hypothesis. We show that high glucose increases activating phosphorylation of the PDGFRβ, resulting in the phosphorylation of the phosphatidylinositol 3 kinase...
April 19, 2017: American Journal of Physiology. Renal Physiology
https://www.readbyqxmd.com/read/28423672/%C3%AE-2-3-sialyltransferase-type-i-regulates-migration-and-peritoneal-dissemination-of-ovarian-cancer-cells
#11
Kuo-Chang Wen, Pi-Lin Sung, Shie-Liang Hsieh, Yu-Ting Chou, Oscar Kuang-Sheng Lee, Cheng-Wen Wu, Peng-Hui Wang
Epithelial ovarian cancer (EOC) has the highest mortality rate among gynecologic cancers due to advanced stage presentation, peritoneal dissemination, and refractory ascites at diagnosis. We investigated the role of α2,3-sialyltransferase type I (ST3GalI) by analyzing human ovarian cancer datasets and human EOC tissue arrays. We found that high expression of ST3GalI was associated with advanced stage EOC. Transwell migration and cell invasion assays showed that high ST3GalI expression enhanced migration of EOC cells...
March 7, 2017: Oncotarget
https://www.readbyqxmd.com/read/28409931/1-4-18-f-fluorobenzyl-4-tetrahydrofuran-2-yl-methyl-piperazine-a-novel-suitable-radioligand-with-low-lipophilicity-for-imaging-sigma-1-receptors-in-the-brain
#12
Yingfang He, Fang Xie, Jiajun Ye, Winnie Deuther-Conrad, Bixiao Cui, Liang Wang, Jie Lu, Jörg Steinbach, Peter Brust, Yiyun Huang, Jie Lu, Hongmei Jia
We have designed and synthesized novel piperazine compounds with low lipophilicity as σ1 receptor ligands. 1-(4-Fluorobenzyl)-4-((tetrahydrofuran-2-yl)methyl)piperazine (10) possessed low nanomolar σ1 receptor affinity and high selectivity toward the vesicular acetylcholine transporter (>2000-fold), σ2 receptors (52-fold), adenosine A2A, adrenergic α2, cannabinoid CB1, dopamine D1, D2L, γ-aminobutyric acid A (GABAA), NMDA, melatonin MT1, MT2 and serotonin 5-HT1 receptors. The corresponding radiotracer [(18)F]10 demonstrated high brain uptake and extremely high brain-to-blood ratios in biodistribution studies in mice...
April 14, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28405526/anti-vegfr2-interferon-%C3%AE-2-regulates-the-tumor-microenvironment-and-exhibits-potent-antitumor-efficacy-against-colorectal-cancer
#13
Zhaoting Li, Yijia Zhu, Chenchen Li, Ryan Trinh, Xueyan Ren, Fumou Sun, Youfu Wang, Pengzhao Shang, Tong Wang, Min Wang, Sherie L Morrison, Juan Zhang
Interferon-α (IFNα) has multiple antitumor effects including direct antitumor toxicity and the ability to potently stimulate both innate and adaptive immunity. However, its clinical applications in the treatment of malignancies have been limited because of short half-life and serious adverse reactions when attempting to deliver therapeutically effective doses. To address these issues, we fused IFNα2a to the anti-vascular endothelial growth factor and receptor 2 (VEGFR2) antibody JZA00 with the goal of targeting it to the tumor microenvironment where it can stimulate the antitumor immune response...
2017: Oncoimmunology
https://www.readbyqxmd.com/read/28402881/stability-and-conformation-of-a-chemoreceptor-hamp-domain-chimera-correlates-with-signaling-properties
#14
Nattakan Sukomon, Joanne Widom, Peter P Borbat, Jack H Freed, Brian R Crane
HAMP domains are dimeric, four-helix bundles that transduce conformational signals in bacterial receptors. Genetic studies of the Escherichia coli serine receptor (Tsr) provide an opportunity to understand HAMP conformational behavior in terms of functional output. To increase its stability, the Tsr HAMP domain was spliced into a poly-HAMP unit from the Pseudomonas aeruginosa Aer2 receptor. Within the chimera, the Tsr HAMP undergoes a thermal melting transition at a temperature much lower than that of the Aer2 HAMP domains...
April 11, 2017: Biophysical Journal
https://www.readbyqxmd.com/read/28400591/pathogenicity-and-transmission-of-a-swine-influenza-a-h6n6-virus
#15
Hailiang Sun, Bryan S Kaplan, Minhui Guan, Guihong Zhang, Jianqiang Ye, Li-Ping Long, Sherry Blackmon, Chun-Kai Yang, Meng-Jung Chiang, Hang Xie, Nan Zhao, Jim Cooley, David F Smith, Ming Liao, Carol Cardona, Lei Li, George Peng Wang, Richard Webby, Xiu-Feng Wan
Subtype H6 influenza A viruses (IAVs) are commonly detected in wild birds and domestic poultry and can infect humans. In 2010, a H6N6 virus emerged in southern China, and since then, it has caused sporadic infections among swine. We show that this virus binds to α2,6-linked and α2,3-linked sialic acids. Mutations at residues 222 (alanine to valine) and 228 (glycine to serine) of the virus hemagglutinin (HA) affected its receptor-binding properties. Experiments showed that the virus has limited transmissibility between ferrets through direct contact or through inhalation of infectious aerosolized droplets...
April 12, 2017: Emerging Microbes & Infections
https://www.readbyqxmd.com/read/28393207/rna-interference-mediated-silencing-of-ppgalnac-t1-and-ppgalnac-t2-inhibits-invasion-and-increases-chemosensitivity-potentially-by-reducing-terminal-%C3%AE-2-3-sialylation-and-mmp14-expression-in-triple%C3%A2-negative-breast-cancer-cells
#16
Hao Qiu, Xu Xu, Min Liu, Zerong Wang, Yaqin Yuan, Chunliang Liu, Lan Xu, Shiliang Wu
Glycopeptide-preferring polypeptide N-acetylgalactosamine transferase (ppGalNAc‑T) is a key enzyme that initiates the formation of the first GalNAc monosaccharide to polypeptides at Thr/Ser residues by O‑linked glycosylation. In order to investigate the effects of ppGalNAc‑T1 and ppGalNAc‑T2 on the initiation of O‑glycosylation, siRNA‑ppGalNAc‑T1 (si‑T1) and siRNA‑ppGalNAc‑T2 (si‑T2) were transfected into highly‑invasive estrogen receptor‑negative MDA‑MB‑231 cells to inhibit O‑glycosylation...
April 7, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28387936/the-plasticity-of-descending-controls-in-pain-translational-probing
#17
Kirsty Bannister, A H Dickenson
Descending controls, comprising pathways that originate in midbrain and brainstem regions and project onto the spinal cord, have long been recognized as key links in the multiple neural networks that interact to produce the overall pain experience. There is clear evidence from preclinical and clinical studies that both peripheral and central sensitisation play important roles in determining the level of pain perceived. Much emphasis has been put on spinal cord mechanisms in central excitability, but it now becoming clear that spinal hyperexcitability can be regulated by descending pathways from the brain that originate from predominantly noradrenergic and serotonergic systems...
April 7, 2017: Journal of Physiology
https://www.readbyqxmd.com/read/28386114/avian-and-human-influenza-virus-compatible-sialic-acid-receptors-in-little-brown-bats
#18
Shubhada K Chothe, Gitanjali Bhushan, Ruth H Nissly, Yin-Ting Yeh, Justin Brown, Gregory Turner, Jenny Fisher, Brent J Sewall, DeeAnn M Reeder, Mauricio Terrones, Bhushan M Jayarao, Suresh V Kuchipudi
Influenza A viruses (IAVs) continue to threaten animal and human health globally. Bats are asymptomatic reservoirs for many zoonotic viruses. Recent reports of two novel IAVs in fruit bats and serological evidence of avian influenza virus (AIV) H9 infection in frugivorous bats raise questions about the role of bats in IAV epidemiology. IAVs bind to sialic acid (SA) receptors on host cells, and it is widely believed that hosts expressing both SA α2,3-Gal and SA α2,6-Gal receptors could facilitate genetic reassortment of avian and human IAVs...
April 6, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28382197/attention-deficit-hyperactivity-disorder-medication-use-factors-involved-in-prescribing-safety-aspects-and-outcomes
#19
REVIEW
Jose Martinez-Raga, Amparo Ferreros, Carlos Knecht, Raquel de Alvaro, Eloisa Carabal
While treatment of patients with attention-deficit hyperactivity disorder (ADHD) is based on a multimodal approach that combines medication with specific psychological interventions, pharmacotherapy alone is generally considered an essential and cost-effective element. This paper aims to comprehensively and critically review factors involved in prescribing and medication use in individuals diagnosed with ADHD, focusing on the difficulties facing patients with ADHD seeking treatment, as well as the safety and tolerability aspects of ADHD pharmacotherapies, with particular attention on the cardiovascular adverse events and the potential risk of misuse or diversion of ADHD medications...
March 2017: Therapeutic Advances in Drug Safety
https://www.readbyqxmd.com/read/28365836/abuse-related-effects-of-subtype-selective-gabaa-receptor-positive-allosteric-modulators-in-an-assay-of-intracranial-self-stimulation-in-rats
#20
Kathryn L Schwienteck, Guanguan Li, Michael M Poe, James M Cook, Matthew L Banks, S Stevens Negus
RATIONALE: GABAA positive allosteric modulators (GABAA PAMs), such as diazepam and zolpidem, are used clinically for anxiety and insomnia, but abuse liability is a concern. Novel GABAA PAMS may have lower abuse liability while retaining clinical utility. OBJECTIVE: The present study compared abuse-related effects of the non-selective GABAA PAM diazepam, the α1-selective GABAA PAM zolpidem, and three novel GABAA PAMs (JY-XHe-053, XHe-II-053, and HZ-166) using intracranial self-stimulation (ICSS) in rats...
April 1, 2017: Psychopharmacology
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