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https://www.readbyqxmd.com/read/28225493/acetylcholinesterase-inhibitor-treatment-alleviated-cognitive-impairment-caused-by-delayed-encephalopathy-due-to-carbon-monoxide-poisoning-two-case-reports-and-a-review-of-the-literature
#1
Kumi Yanagiha, Kazuhiro Ishii, Akira Tamaoka
INTRODUCTION: Delayed encephalopathy due to carbon monoxide (CO) poisoning can even occur in patients with mild symptoms of acute CO poisoning. Some cases taking conventional hyperbaric oxygen (HBO) therapy or steroid-pulse therapy may be insufficient, and AchEI may be effective. PATIENT CONCERNS AND DIAGNOSES: We report two cases of delayed encephalopathy after acute CO poisoning involving two women aged 69 (Case 1) and 60 years (Case 2) whose cognitive function improved with acetylcholinesterase inhibitor (AchEI) treatment...
February 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/28223528/inhibition-of-%C3%AE-9%C3%AE-10-nicotinic-acetylcholine-receptors-prevents-chemotherapy-induced-neuropathic-pain
#2
Haylie K Romero, Sean B Christensen, Lorenzo Di Cesare Mannelli, Joanna Gajewiak, Renuka Ramachandra, Keith S Elmslie, Douglas E Vetter, Carla Ghelardini, Shawn P Iadonato, Jose L Mercado, Baldomera M Olivera, J Michael McIntosh
Opioids are first-line drugs for moderate to severe acute pain and cancer pain. However, these medications are associated with severe side effects, and whether they are efficacious in treatment of chronic nonmalignant pain remains controversial. Medications that act through alternative molecular mechanisms are critically needed. Antagonists of α9α10 nicotinic acetylcholine receptors (nAChRs) have been proposed as an important nonopioid mechanism based on studies demonstrating prevention of neuropathology after trauma-induced nerve injury...
February 21, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28223265/use-of-a-novel-artificial-intelligence-platform-on-mobile-devices-to-assess-dosing-compliance-in-a-phase-2-clinical-trial-in-subjects-with-schizophrenia
#3
Earle E Bain, Laura Shafner, David P Walling, Ahmed A Othman, Christy Chuang-Stein, John Hinkle, Adam Hanina
BACKGROUND: Accurately monitoring and collecting drug adherence data can allow for better understanding and interpretation of the outcomes of clinical trials. Most clinical trials use a combination of pill counts and self-reported data to measure drug adherence, despite the drawbacks of relying on these types of indirect measures. It is assumed that doses are taken, but the exact timing of these events is often incomplete and imprecise. OBJECTIVE: The objective of this pilot study was to evaluate the use of a novel artificial intelligence (AI) platform (AiCure) on mobile devices for measuring medication adherence, compared with modified directly observed therapy (mDOT) in a substudy of a Phase 2 trial of the α7 nicotinic receptor agonist (ABT-126) in subjects with schizophrenia...
February 21, 2017: JMIR MHealth and UHealth
https://www.readbyqxmd.com/read/28222901/pharmacotherapy-in-smoking-cessation-corticotropin-releasing-factor-receptors-as-emerging-intervention-targets
#4
REVIEW
Ioannis Sotiriou, Kleanthi Chalkiadaki, Christos Nikolaidis, Kyriaki Sidiropoulou, Ekaterini Chatzaki
Smoking represents perhaps the single most important health risk factor and a global contributor to mortality that can unquestionably be prevented. Smoking is responsible for many diseases, including various types of cancer, chronic obstructive pulmonary disease, coronary heart disease, peripheral vascular disease and peptic ulcer, while it adversely affects fetal formation and development. Since smoking habit duration is a critical factor for mortality, the goal of treatment should be its timely cessation and relapse prevention...
February 14, 2017: Neuropeptides
https://www.readbyqxmd.com/read/28221788/substituted-2-aminopyrimidines-selective-for-%C3%AE-7-nicotinic-acetylcholine-receptor-activation-and-association-with-acetylcholine-binding-proteins
#5
Katarzyna Kaczanowska, Gisela Andrea Camacho Hernandez, Larissa Bendiks, Larissa Kohs, Jose Manuel Cornejo Bravo, Michal Harel, M G Finn, Palmer Taylor
Through studies with ligand binding to the acetylcholine binding protein (AChBP), we previously identified a series of 4,6 substituted 2-aminopyrimidines that associate with this soluble surrogate of the nicotinic acetylcholine receptor (nAChR) in a cooperative fashion, not seen for classical nicotinic agonists and antagonists. To examine receptor interactions of this structural family on ligand-gated ion channels, we employed HEK cells transfected with cDNA's encoding three requisite receptor subtypes: α7-nAChR, α4β2-nAChR and a serotonin receptor (5-HT3AR), along with a fluorescent reporter...
February 21, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28219984/motor-neurons-tune-premotor-activity-in-a-vertebrate-central-pattern-generator
#6
Kristy J Lawton, Wick M Perry, Ayako Yamaguchi, Erik Zornik
Central patterns generators (CPGs) are neural circuits that drive rhythmic motor output without sensory feedback. Vertebrate CPGs are generally believed to operate in a top-down manner in which premotor interneurons activate motor neurons that in turn drive muscles. In contrast, the frog (Xenopus laevis) vocal CPG contains a functionally unexplored neuronal projection from the motor nucleus to the premotor nucleus, indicating a recurrent pathway that may contribute to rhythm generation. In this study we characterized the function of this bottom-up connection...
February 20, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28218274/trapping-of-ivermectin-by-a-pentameric-ligand-gated-ion-channel-upon-open-to-closed-isomerization
#7
Nurit Degani-Katzav, Moshe Klein, Moran Har-Even, Revital Gortler, Ruthi Tobi, Yoav Paas
Ivermectin (IVM) is a broad-spectrum anthelmintic drug used to treat human parasitic diseases like river blindness and lymphatic filariasis. By activating invertebrate pentameric glutamate-gated chloride channels (GluCl receptors; GluClRs), IVM induces sustained chloride influx and long-lasting membrane hyperpolarization that inhibit neural excitation in nematodes. Although IVM activates the C. elegans heteromeric GluClα/β receptor, it cannot activate a homomeric receptor composed of the C. elegans GluClβ subunits...
February 20, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28217868/an-anti-nicotinic-cognitive-challenge-model-using-mecamylamine-in-comparison-with-the-anti-muscarinic-cognitive-challenge-using-scopolamine
#8
A C Baakman, R Alvarez-Jimenez, R Rissmann, E S Klaassen, J Stevens, S C Goulooze, J Burger, E L Swart, J M A van Gerven, G J Groeneveld
INTRODUCTION: The muscarinic acetylcholine receptor antagonist scopolamine is often used for proof-of-pharmacology studies with pro-cognitive compounds. From a pharmacological point of view, it would seem more rational to use a nicotinic rather than a muscarinic anticholinergic challenge to prove pharmacology of a nicotinic acetylcholine receptor agonist. This study aims to characterize a nicotinic anticholinergic challenge model using mecamylamine and to compare it to the scopolamine model...
February 20, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28216123/ablation-of-the-auditory-cortex-results-in-changes-in-the-expression-of-neurotransmission-related-mrnas-in-the-cochlea
#9
Verónica Lamas, José M Juiz, Miguel A Merchán
The auditory cortex (AC) dynamically regulates responses of the Organ of Corti to sound through descending connections to both the medial (MOC) and lateral (LOC) olivocochlear efferent systems. We have recently provided evidence that AC has a reinforcement role in the responses to sound of the auditory brainstem nuclei. In a molecular level, we have shown that descending inputs from AC are needed to regulate the expression of molecules involved in outer hair cell (OHC) electromotility control, such as prestin and the α10 nicotinic acetylcholine receptor (nAchR)...
February 16, 2017: Hearing Research
https://www.readbyqxmd.com/read/28213944/separation-of-hydroxynorketamine-stereoisomers-using-capillary-electrophoresis-with-sulfated-%C3%AE-cyclodextrin-and-highly-sulfated-%C3%AE-cyclodextrin
#10
Friederike A Sandbaumhüter, Regula Theurillat, Wolfgang Thormann
The racemic N-methyl-d-aspartate receptor antagonist ketamine is used in anesthesia, analgesia and the treatment of depressive disorders. It is known that interactions of hydroxylated norketamine metabolites and 5,6-dehydronorketamine (DHNK) with the α7 -nicotinic acetylcholine receptor and the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor are responsible for the antidepressive effects. Ketamine and its first metabolite norketamine are not active on these receptors. As stereoselectivity plays a role in ketamine metabolism, a cationic capillary electrophoresis based method capable of resolving and analyzing the stereoisomers of four hydroxylated norketamine metabolites, norketamine and DHNK was developed...
February 18, 2017: Electrophoresis
https://www.readbyqxmd.com/read/28213446/acetylcholine-release-in-prefrontal-cortex-promotes-gamma-oscillations-and-theta-gamma-coupling-during-cue-detection
#11
W M Howe, H J Gritton, N Lusk, Erik A Roberts, Vaughn L Hetrick, Joshua D Berke, Martin Sarter
The capacity for using external cues to guide behavior ("cue detection") constitutes an essential aspect of attention and goal-directed behavior. The cortical cholinergic input system, via phasic increases in prefrontal acetylcholine release, plays an essential role in attention by mediating such cue detection. However, the relationship between cholinergic signaling during cue detection and neural activity dynamics in prefrontal networks remains unclear. Here we combined sub-second measures of cholinergic signaling, neurophysiological recordings, and cholinergic receptor blockade to delineate the cholinergic contributions to prefrontal oscillations during cue detection in rats...
February 17, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28212459/structural-studies-of-nicotinoids-cotinine-vs-nicotine
#12
Iciar Uriarte, Cristóbal Pérez, Elena Caballero-Mancebo, Francisco J Basterretxea, Alberto Lesarri, José A Fernández, Emilio J Cocinero
Nicotinoids are agonists of the acetylcholine receptor (nAChR) and play important biochemical and pharmacological roles. Here we report on the structural and conformational landscape of cotinine, and compare its molecular properties with the nicotine prototype, from which it only differs in the addition of a carbonyl group. The investigation of cotinine included a theoretical survey of the effects of rotamerization of the pyridine moiety, the puckering of the pyrrolidinone ring and the internal rotation of the methyl group...
February 17, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28210782/toll-like-receptor-signaling-and-stages-of-addiction
#13
REVIEW
Fulton T Crews, T Jordan Walter, Leon G Coleman, Ryan P Vetreno
BACKGROUND: Athina Markou and her colleagues discovered persistent changes in adult behavior following adolescent exposure to ethanol or nicotine consistent with increased risk for developing addiction. Building on Dr. Markou's important work and that of others in the field, researchers at the Bowles Center for Alcohol Studies have found that persistent changes in behavior following adolescent stress or alcohol exposure may be linked to induction of immune signaling in brain. AIM: This study aims to illuminate the critical interrelationship of the innate immune system (e...
February 17, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28209997/antisense-mir-132-blockade-via-the-ache-r-splice-variant-mitigates-cortical-inflammation
#14
Nibha Mishra, Lyndon Friedson, Geula Hanin, Uriya Bekenstein, Meshi Volovich, Estelle R Bennett, David S Greenberg, Hermona Soreq
MicroRNA (miR)-132 brain-to-body messages suppress inflammation by targeting acetylcholinesterase (AChE), but the target specificity of 3'-AChE splice variants and the signaling pathways involved remain unknown. Using surface plasmon resonance (SPR), we identified preferential miR-132 targeting of soluble AChE-R over synaptic-bound AChE-S, potentiating miR-132-mediated brain and body cholinergic suppression of pro-inflammatory cytokines. Inversely, bacterial lipopolysaccharide (LPS) reduced multiple miR-132 targets, suppressed AChE-S more than AChE-R and elevated inflammatory hallmarks...
February 17, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28209287/molecular-imaging-of-the-nicotinic-cholinergic-receptor-in-alzheimer-disease
#15
EDITORIAL
Gwenn S Smith
No abstract text is available yet for this article.
January 5, 2017: American Journal of Geriatric Psychiatry
https://www.readbyqxmd.com/read/28202387/varenicline-enhances-oxidized-ldl-uptake-by-increasing-expression-of-lox-1-and-cd36-scavenger-receptors-through-%C3%AE-7-nachr-in-macrophages
#16
Yuki Kanaoka, Mitsuhisa Koga, Keita Sugiyama, Kaoru Ohishi, Yasufumi Kataoka, Atsushi Yamauchi
Varenicline is a widely used and effective drug for smoking cessation. It is a partial agonist of the α4β2 nicotinic acetylcholine receptor (nAChR) and full agonist of α7 nAChR. We have reported that varenicline aggravates formation of atherosclerotic plaques through α7 nAChR in apolipoprotein E knockout mice. However, little is known about its effects on macrophages in atherosclerotic plaques. Here, we ascertained whether varenicline promotes oxidized low-density lipoprotein (oxLDL) uptake in mouse peritoneal macrophages in vitro and clarified its mechanism...
February 12, 2017: Toxicology
https://www.readbyqxmd.com/read/28199738/orthosteric-and-allosteric-potentiation-of-heteromeric-neuronal-nicotinic-acetylcholine-receptors
#17
REVIEW
Jingyi Wang, Jon Lindstrom
Heteromeric nicotinic acetylcholine receptors (nAChRs) were thought to have two orthodox agonist binding sites at two α/β subunit interfaces. Highly selective ligands are hard to achieve by targeting orthodox agonist sites because of high sequence similarity of this binding pocket among different subunits. Recently, unorthodox acetylcholine (ACh) binding sites have been discovered at some α/α and β/α subunit interfaces, such as α4/α4, α5/α4 and β3/α4. Targeting unorthodox sites may yield subtype-selective ligands which are otherwise hard to develop, such as those for (α4β2)2 α5, (α4β2)2 β3 and (α6β2)2 β3 nAChRs...
February 15, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28197544/plasticity-in-brainstem-mechanisms-of-pain-modulation-by-nicotinic-acetylcholine-receptors-in-the-rat
#18
Francis J Jareczek, Stephanie R White, Donna L Hammond
Individuals with chronic pain may be driven to smoke more because the analgesic efficacy of nicotine diminishes. To determine whether persistent pain diminishes the actions of a nicotinic acetylcholine receptor (nAChR) agonist in pain modulatory pathways, we examined the effects of epibatidine in the rostral ventromedial medulla (RVM) of rats with and without inflammatory injury induced by intraplantar injection of complete Freund's adjuvant (CFA). In uninjured rats, epibatidine produced a dose-dependent antinociception that was completely blocked by dihydro-β-erythroidine (DHβE; α4β2 antagonist) and partially blocked by methyllycaconitine (MLA; α7 antagonist)...
January 2017: ENeuro
https://www.readbyqxmd.com/read/28197102/right-cervical-vagotomy-aggravates-viral-myocarditis-in-mice-via-the-cholinergic-anti-inflammatory-pathway
#19
Ge Li-Sha, Chen Xing-Xing, Wu Lian-Pin, Zhou De-Pu, Li Xiao-Wei, Lin Jia-Feng, Li Yue-Chun
The autonomic nervous system dysfunction with increased sympathetic activity and withdrawal of vagal activity may play an important role in the pathogenesis of viral myocarditis. The vagus nerve can modulate the immune response and control inflammation through a 'cholinergic anti-inflammatory pathway' dependent on the α7-nicotinic acetylcholine receptor (α7nAChR). Although the role of β-adrenergic stimulation on viral myocarditis has been investigated in our pervious studies, the direct effect of vagal tone in this setting has not been yet studied...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28196430/first-in-human-trial-of-a-type-i-positive-allosteric-modulator-of-alpha7-nicotinic-acetylcholine-receptors-pharmacokinetics-safety-and-evidence-for-neurocognitive-effect-of-avl-3288
#20
Kelvin W Gee, Ann Olincy, Richard Kanner, Lynn Johnson, Derk Hogenkamp, Josette Harris, Minhtam Tran, Stephen A Edmonds, William Sauer, Ryan Yoshimura, Timothy Johnstone, Robert Freedman
Type I positive allosteric modulators (PAMs) of the alpha7-nicotinic receptor enhance its cholinergic activation while preserving the spatiotemporal features of synaptic transmission and the receptor's characteristic rapid desensitization kinetics. Alpha7-nicotinic receptor agonists have shown promise for improving cognition in schizophrenia, but longer-term trials have been disappointing. Therefore, the type I PAM AVL-3288 was evaluated for safety and preliminary evidence of neurocognitive effect in healthy human subjects...
February 1, 2017: Journal of Psychopharmacology
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