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https://www.readbyqxmd.com/read/28221788/substituted-2-aminopyrimidines-selective-for-%C3%AE-7-nicotinic-acetylcholine-receptor-activation-and-association-with-acetylcholine-binding-proteins
#1
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/28216123/ablation-of-the-auditory-cortex-results-in-changes-in-the-expression-of-neurotransmission-related-mrnas-in-the-cochlea
#2
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/28212459/structural-studies-of-nicotinoids-cotinine-vs-nicotine
#3
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/28202387/varenicline-enhances-oxidized-ldl-uptake-by-increasing-expression-of-lox-1-and-cd36-scavenger-receptors-through-%C3%AE-7-nachr-in-macrophages
#4
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
#5
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
#6
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
#7
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/28187919/dopamine-d3-and-acetylcholine-nicotinic-receptor-heteromerization-in-midbrain-dopamine-neurons-relevance-for-neuroplasticity
#8
Leonardo Bontempi, Paola Savoia, Federica Bono, Chiara Fiorentini, Cristina Missale
Activation of nicotinic acetylcholine receptors (nAChR) promotes the morphological remodeling of cultured dopamine (DA) neurons, an effect requiring functional DA D3 receptors (D3R). The aim of this study was to investigate the mechanisms mediating D3R-nAChR cross-talk in the modulation of DA neuron structural plasticity. By using bioluminescence resonance energy transfer(2) (BRET(2)) and proximity ligation assay (PLA), evidence for the existence of D3R-nAChR heteromers has been obtained. In particular, BRET(2) showed that the D3R directly and specifically interacts with the β2 subunit of the nAChR...
February 7, 2017: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28187830/lack-of-cross-resistance-between-neonicotinoids-and-sulfoxaflor-in-field-strains-of-q-biotype-of-whitefly-bemisia-tabaci-from-eastern-china
#9
Wenlong Wang, Shaoli Wang, Guangjie Han, Yuzhou Du, Jianjun Wang
Control of Bemisia tabaci has depended primarily and heavily on insecticides, especially neonicotinoids. The novel sulfoximine insecticide sulfoxaflor exhibits high potency against a broad range of sap-feeding insect species, including those resistant to neonicotinoids. The resistance levels of Q-biotype B. tabaci field strains collected from 8 locations in eastern China to neonicotinoids and sulfoxaflor were investigated, and single nucleotide polymorphisms (SNPs) of nicotinic acetylcholine receptor β1 subunit gene (Btβ1) were detected...
March 2017: Pesticide Biochemistry and Physiology
https://www.readbyqxmd.com/read/28177213/characterization-of-optically-and-electrically-evoked-dopamine-release-in-striatal-slices-from-digenic-knock-in-mice-with-dat-driven-expression-of-channelrhodopsin
#10
Brian O'Neill, Jyoti C Patel, Margaret E Rice
Fast-scan cyclic voltammetry (FCV) is an established method to monitor increases in extracellular dopamine (DA) concentration ([DA]o) in the striatum, which is densely innervated by DA axons. Ex vivo brain slice preparations provide an opportunity to identify endogenous modulators of DA release. For these experiments, local electrical stimulation is often used to elicit release of DA, as well as other transmitters, in the striatal microcircuitry; changes in evoked increases in [DA]o after application of a pharmacological agent (e...
February 15, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28176635/modes-of-action-resistance-and-toxicity-of-insecticides-targeting-nicotinic-acetylcholine-receptors
#11
Makoto Ihara, Steven D Buckingham, Kazuhiko Matsuda, David B Sattelle
Nicotinic acetylcholine receptors (nAChRs) are members of the cys-loop superfamily of ligand-gated ion channels (cys-loop LGICs) and mediate fast cholinergic synaptic transmission in the nervous system of insects. The completion of many insect genome projects has greatly enhanced our understanding of the individual subunits that make up nAChR gene families from an insect genetic model organism (Drosophila melanogaster), crop pests, disease vectors and beneficial (pollinator) species. In addition to considerable insect nAChR subunit diversity, individual subunits can be subject to alternative splicing and RNA editing and these post-transcriptional modifications can add significantly to the diversity of nAChR receptor subtypes...
February 6, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28176016/choline-induces-opposite-changes-in-pyramidal-neuron-excitability-and-synaptic-transmission-through-a-nicotinic-receptor-independent-process-in-hippocampal-slices
#12
E Albiñana, J G Luengo, A M Baraibar, M D Muñoz, L Gandía, J M Solís, J M Hernández-Guijo
Choline is present at cholinergic synapses as a product of acetylcholine degradation. In addition, it is considered a selective agonist for α5 and α7 nicotinic acetylcholine receptors (nAChRs). In this study, we determined how choline affects action potentials and excitatory synaptic transmission using extracellular and intracellular recording techniques in CA1 area of hippocampal slices obtained from both mice and rats. Choline caused a reversible depression of evoked field excitatory postsynaptic potentials (fEPSPs) in a concentration-dependent manner that was not affected by α7 nAChR antagonists...
February 8, 2017: Pflügers Archiv: European Journal of Physiology
https://www.readbyqxmd.com/read/28169167/design-and-synthesis-of-a-novel-series-of-4-heteroarylamino-1-azaspiro-oxazole-5-3-bicyclo-2-2-2-octanes-as-%C3%AE-7-nicotinic-receptor-agonists-2-development-of-4-heteroaryl-sar
#13
Christiana Iwuagwu, Dalton King, Ivar M McDonald, James Cook, F Christopher Zusi, Matthew D Hill, Robert A Mate, Haiquan Fang, Ronald Knox, Lizbeth Gallagher, Debra Post-Munson Amy Easton, Regina Miller, Yulia Benitex, Judy Siuciak, Nicholas Lodge, Robert Zaczek, Daniel Morgan, Linda Bristow, John E Macor, Richard E Olson
Quinuclidine-containing spirooxazolines, as described in the previous report in this series, were demonstrated to have utility as α7 nicotinic acetylcholine receptor (α7 nAChR) partial agonists. In this work, the SAR of this chemotype was expanded to include an array of diazine heterocyclic substitutions. Many of the heterocyclic analogs were potent partial agonists of the α7 receptor, selective against other nicotinic receptors and the serotinergic 5HT3A receptor. (1'S,3'R,4'S)-N-(6-phenylpyrimidin-4-yl)-4H-1'-azaspiro[oxazole-5,3'-bicyclo[2...
January 20, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28168926/stimulation-of-nicotinic-acetylcholine-alpha7-receptors-rescue-schizophrenia-like-cognitive-impairments-in-rats
#14
Agnieszka Potasiewicz, Agnieszka Nikiforuk, Małgorzata Hołuj, Piotr Popik
Alpha7 nicotinic acetylcholine receptor (α7 nAChR) dysfunction plays an important role in schizophrenia. Positive allosteric modulators of α7 nAChR have emerged as a promising therapeutic approach to manage cognitive deficits that are inadequately treated in schizophrenic patients. The aim of the present study was to evaluate the ability of type I (CCMI) and type II (PNU120596) α7 nAChR positive allosteric modulators to counteract MK-801-induced cognitive and sensorimotor gating deficits. The activity of these compounds was compared with the action of the α7 nAChR agonist A582941...
February 2017: Journal of Psychopharmacology
https://www.readbyqxmd.com/read/28161246/partial-agonism-at-the-%C3%AE-7-nicotinic-acetylcholine-receptor-improves-attention-impulsive-action-and-vigilance-in-low-attentive-rats
#15
Andrew Hayward, Lisa Adamson, Joanna C Neill
Inattention is a disabling symptom in conditions such as schizophrenia and attention deficit/hyperactivity disorder. Nicotine can improve attention and vigilance, but is unsuitable for clinical use due to abuse liability. Genetic knockout of the α7 nicotinic acetylcholine receptor (nAChR) induces attention deficits therefore selective agonism may improve attention, without the abuse liability associated with nicotine. The α7 nAChR partial agonist encenicline (formerly EVP-6124) enhances memory in rodents and humans...
February 1, 2017: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28155595/cholinergic-anti-inflammatory-pathway-and-stroke
#16
Kamil Duris, Jolana Lipkova, Michal Jurajda
Stroke is devastating cerebrovascular event which is responsible for 6.7 million deaths each year worldwide. Inflammation plays an important role in the pathophysiology of stroke. Targeting inflammation after stroke is highly actual topic for both experimental and clinical research. Cholinergic anti-inflammatory pathway (CHAIP) is a physiological mechanism by which central nervous system regulates immune response and controls inflammation. Vagus nerve, spleen and α7 nicotinic acetylcholine receptor (α7 nAChR) are the main components of CHAIP...
February 1, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/28153524/cellular-protein-and-mrna-expression-of-%C3%AE-1-nicotinic-acetylcholine-receptor-nachr-subunit-in-brain-skeletal-muscle-and-placenta
#17
Atqiya Aishah, Tina Hinton, Rita Machaalani
The β1 nicotinic acetylcholine receptor (nAChR) subunit is a muscle type subunit of this family and as such, is found predominantly in muscle. Recent reports document its expression in other tissues and cell lines including adrenal glands, carcinomas, lung and brain. However, the majority of studies were of tissue lysates, thus the cellular distribution was not determined. This study aimed to determine the cellular distribution of the β1 nAChR subunit in the brain, at both the mRNA and protein levels, using non-radioactive in situ hybridization (ISH) and immunohistochemistry (IHC), respectively, and to compare it to two muscle tissue types, skeletal and placenta...
January 30, 2017: International Journal of Developmental Neuroscience
https://www.readbyqxmd.com/read/28147247/evidence-of-brdu-positive-retinal-neurons-after-application-of-an-alpha7-nicotinic-acetylcholine-receptor-agonist
#18
Mark K Webster, Cynthia A Cooley-Themm, Joseph D Barnett, Harrison B Bach, Jessica M Vainner, Sarah E Webster, Cindy L Linn
Irreversible vision loss due to disease or age is responsible for a reduced quality of life. The experiments in this study test the hypothesis that the α7 nicotinic acetylcholine receptor agonist, PNU-282987, leads to the generation of retinal neurons in an adult mammalian retina in the absence of retinal injury or exogenous growth factors. Using antibodies against BrdU, retinal ganglion cells, progenitor cells and Müller glia, the results of this study demonstrate that multiple types of retinal cells and neurons are generated after eye drop application of PNU-282987 in adult Long Evans rats in a dose-dependent manner...
January 29, 2017: Neuroscience
https://www.readbyqxmd.com/read/28134524/monod-wyman-changeux-analysis-of-ligand-gated-ion-channel-mutants
#19
Tal Einav, Rob Phillips
We present a framework for computing the gating properties of ligand-gated ion channel mutants using the Monod-Wyman-Changeux (MWC) model of allostery. We derive simple analytic formulas for key functional properties such as the leakiness, dynamic range, half-maximal effective concentration ([EC50]), and effective Hill coefficient, and explore the full spectrum of phenotypes that are accessible through mutations. Specifically, we consider mutations in the channel pore of nicotinic acetylcholine receptor (nAChR) and the ligand binding domain of a cyclic nucleotide-gated (CNG) ion channel, demonstrating how each mutation can be characterized as only affecting a subset of the biophysical parameters...
January 30, 2017: Journal of Physical Chemistry. B
https://www.readbyqxmd.com/read/28131622/perinatal-nicotine-treatment-induces-transient-increases-in-nacho-protein-levels-in-the-rat-frontal-cortex
#20
Franziska Wichern, Majbrit M Jensen, Ditte Z Christensen, Jens D Mikkelsen, Marjorie C Gondré-Lewis, Morten S Thomsen
The nicotinic acetylcholine receptor (nAChR) regulator chaperone (NACHO) was recently identified as an important regulator of nAChR maturation and surface expression. Here we show that NACHO levels decrease during early postnatal development in rats. This decrease occurs earlier and to a greater degree in the frontal cortex (FC) compared with the hippocampus (HIP). We further show that rats exposed to nicotine during pre- and postnatal development exhibit significantly higher NACHO levels in the FC at postnatal day (PND) 21, but not at PND60...
January 25, 2017: Neuroscience
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