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https://www.readbyqxmd.com/read/29784663/involvement-of-nicotinic-receptor-subtypes-in-behavioral-effects-of-nicotinic-drugs-in-squirrel-monkeys
#1
Sarah Louise Withey, Michelle R Doyle, Jack Bergman, Rajeev I Desai
Evidence suggests that the α4β2, but not the α7, subtype of nicotinic acetylcholine receptor (nAChR) plays a key role in mediating the behavioral effects of nicotine and related drugs. However, the importance of other nAChR subtypes remains unclear. The present studies were conducted to examine the involvement of nAChR subtypes by determining the effects of selected nicotinic agonists and antagonists in squirrel monkeys: a) responding for food-reinforcement; or b) discriminating the nicotinic agonist (+)-epibatidine (0...
May 21, 2018: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29779223/gene-editing-vectors-for-studying-nicotinic-acetylcholine-receptors-in-cholinergic-transmission
#2
Can Peng, Yijin Yan, Veronica J Kim, Staci E Engle, Jennifer N Berry, J Michael McIntosh, Rachael L Neve, Ryan M Drenan
Nicotinic acetylcholine receptors (nAChRs), prototype members of the cys-loop ligand gated ion channel family, are key mediators of cholinergic transmission in the central nervous system. Despite their importance, technical gaps exist in our ability to dissect the function of individual subunits in the brain. To overcome these barriers, we designed CRISPR/Cas9 small guide RNA sequences (sgRNAs) for production of loss-of-function alleles in mouse nAChR genes. These sgRNAs were validated in vitro via deep sequencing...
May 19, 2018: European Journal of Neuroscience
https://www.readbyqxmd.com/read/29778945/self-administration-of-the-synthetic-cathinone-mpdv-enhances-reward-function-via-a-nicotinic-receptor-dependent-mechanism
#3
Jean R Geste, Marjory Pompilus, Marcelo Febo, Adriaan W Bruijnzeel
Methylenedioxypyrovalerone (MDPV) is an addictive synthetic drug with severe side effects. Previous studies have shown that MDPV has positive reinforcing properties. However, little is known about the effect of MDPV self-administration on the state of the brain reward system and the neuronal mechanisms by which MDPV mediates its effects. The goal of the present studies was to determine the effect of MDPV self-administration on reward function and the role of cholinergic neurotransmission in the reinforcing effects of MDPV...
May 9, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29775454/in-vivo-and-in-vitro-studies-of-cry5b-and-nicotinic-acetylcholine-receptor-agonist-anthelmintics-reveal-a-powerful-and-unique-combination-therapy-against-intestinal-nematode-parasites
#4
Yan Hu, Melanie Miller, Bo Zhang, Thanh-Thanh Nguyen, Martin K Nielsen, Raffi V Aroian
BACKGROUND: The soil-transmitted nematodes (STNs) or helminths (hookworms, whipworms, large roundworms) infect the intestines of ~1.5 billion of the poorest peoples and are leading causes of morbidity worldwide. Only one class of anthelmintic or anti-nematode drugs, the benzimidazoles, is currently used in mass drug administrations, which is a dangerous situation. New anti-nematode drugs are urgently needed. Bacillus thuringiensis crystal protein Cry5B is a powerful, promising new candidate...
May 18, 2018: PLoS Neglected Tropical Diseases
https://www.readbyqxmd.com/read/29772664/the-cholinergic-anti-inflammatory-response-and-the-role-of-macrophages-in-hiv-induced-inflammation
#5
REVIEW
Manuel Delgado-Vélez, José A Lasalde-Dominicci
Macrophages are phagocytic immune cells that protect the body from foreign invaders and actively support the immune response by releasing anti- and proinflammatory cytokines. A seminal finding revolutionized the way macrophages are seen. The expression of the neuronal alpha7 nicotinic acetylcholine receptor (α7-nAChR) in macrophages led to the establishment of the cholinergic anti-inflammatory response (CAR) in which the activation of this receptor inactivates macrophage production of proinflammatory cytokines...
May 16, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29770521/nicotine-mediated-neuroprotection-of-rat-spinal-networks-against-excitotoxicity
#6
Jaspreet Kaur, Rossana Rauti, Andrea Nistri
Activation of neuronal nicotinic acetylcholine receptors (nAChRs) by nicotine is reported to protect brain neurons from glutamate excitotoxicity. We inquired whether a similar phenomenon can occur in the rat isolated spinal cord (or spinal slice culture) challenged by a transient (1 h) application of kainate (a powerful glutamate receptor agonist) to induce excitotoxicity mimicking spinal injury in vitro. We recorded spinal reflexes and fictive locomotion generated by the locomotor central pattern generator before and 24 h after applying kainate...
May 16, 2018: European Journal of Neuroscience
https://www.readbyqxmd.com/read/29768467/alpha-7-nicotinic-receptors-attenuate-neurite-development-through-calcium-activation-of-calpain-at-the-growth-cone
#7
Justin R King, Nadine Kabbani
The α7 nicotinic acetylcholine receptor (nAChR) is a ligand-gated ion channel that plays an important role in cellular calcium signaling contributing to synaptic development and plasticity, and is a key drug target for the treatment of neurodegenerative conditions such as Alzheimer's disease. Here we show that α7 nAChR mediated calcium signals in differentiating PC12 cells activate the proteolytic enzyme calpain leading to spectrin breakdown, microtubule retraction, and attenuation in neurite growth. Imaging in growth cones confirms that α7 activation decreases EB3 comet motility in a calcium dependent manner as demonstrated by the ability of α7 nAChR, ryanodine, or IP3 receptor antagonists to block the effect of α7 nAChR on growth...
2018: PloS One
https://www.readbyqxmd.com/read/29759142/heterogeneity-of-auto-antibodies-against-nachr-in-myasthenic-serum-and-their-pathogenic-roles-in-experimental-autoimmune-myasthenia-gravis
#8
Ryuichi Nakamura, Tomohiro Makino, Takeshi Hanada, Maki Terakawa, Kazuhiro Nagahira, Jyoji Yamate, Hirokazu Shiraishi, Masakatsu Motomura
Many myasthenia gravis (MG) patients have auto-antibodies against the nicotinic acetylcholine receptor (nAChR), and monoclonal antibodies against the main immunogenic region (MIR) of nAChR can induce experimental autoimmune MG (EAMG). We investigated whether Fab fragment of MIR antibody (Fab35) could block the pathogenicity of polyclonal antibodies. Fab35 partially inhibited nAChR downmodulation, blocked EAMG serum-induced binding of polyclonal antibodies and complement deposition in vitro. Moreover, Fab35 did not ameliorate the EAMG serum-induced EAMG phenotype in rats...
July 15, 2018: Journal of Neuroimmunology
https://www.readbyqxmd.com/read/29753712/focc%C3%AE-6-a-truncated-nachr-subunit-positively-correlates-with-spinosad-resistance-in-the-western-flower-thrips-frankliniella-occidentalis-pergande
#9
Yanran Wan, Guangdi Yuan, Bingqing He, Baoyun Xu, Wen Xie, Shaoli Wang, Youjun Zhang, Qingjun Wu, Xuguo Zhou
Nicotinic acetylcholine receptors (nAChRs), a molecular target for spinosyns and neonicotinoids, mediate rapid cholinergic transmission in insect central nervous system by binding acetylcholine. Previous studies have shown that mutations in nAChRs contribute to the high level of resistance to these two classes of insecticides. In this study, we identified nine nAChR subunits from a transcriptome of the western flower thrips, Frankliniella occidentalis, including α1-7, β1, and β2. Exon 4 of α4 and exons 3 and 8 of α6 each have two splicing variants, respectively...
May 10, 2018: Insect Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/29751234/pyridinyl-and-pyridazinyl-3-6-diazabicyclo-3-1-1-heptane-anilines-novel-selective-ligands-with-subnanomolar-affinity-for-%C3%AE-4-%C3%AE-2-nach-receptors
#10
Francesco Deligia, Gabriele Murineddu, Cecilia Gotti, Giulio Ragusa, Francesca Fasoli, Miriam Sciaccaluga, Simona Plutino, Sergio Fucile, Giovanni Loriga, Battistina Asproni, Gerard A Pinna
The cholinergic pathways in the central nervous system (CNS) of animals and humans are important for cognitive and behavioural functions. Until a few years ago, it was thought that the key molecules transducing the cholinergic message were the metabotropic muscarinic receptors, but it is now known that ionotropic neuronal nicotinic receptors (nAChRs) are also involved. Based on recent studies, we prepared a small library of novel 3-substituted-3,6-diazabicyclo [3.1.1]heptanes, whose binding activity and functionality have been assayed...
April 17, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29748129/the-sarco-endo-plasmic-reticulum-calcium-atpase-sca-1-regulates-the-caenorhabditis-elegans-nicotinic-acetylcholine-receptor-acr-16
#11
Ashley A Martin, Janet E Richmond
Nicotinic acetylcholine receptors (nAChR) are present in many excitable tissues and are found both pre and post-synaptically. Through their non-specific cationic permeability, these nAChRs have excitatory roles in neurotransmission, neuromodulation, synaptic plasticity, and neuroprotection. Thus, nAChR mislocalization or functional deficits are associated with many neurological disease states. Therefore identifying the mechanisms that regulate nAChR expression and function will inform our understanding of normal as well as pathological physiological conditions and offer avenues for potential therapeutic advances...
February 24, 2018: Cell Calcium
https://www.readbyqxmd.com/read/29746088/structure-activity-studies-reveal-the-molecular-basis-for-gabab-receptor-mediated-inhibition-of-high-voltage-activated-calcium-channels-by-%C3%AE-conotoxin-vc1-1
#12
Mahsa Sadeghi, Bodil B Carstens, Brid P Callaghan, James T Daniel, Han Shen Tae, Tracey O'Donnell, Joel Castro, Stuart M Brierley, David J Adams, David J Craik, Richard J Clark
α-Conotoxins are disulfide-bonded peptides from cone snail venoms and are characterized by their affinity for nicotinic acetylcholine receptors (nAChR). Several α-conotoxins with distinct selectivity for nAChR subtypes have been identified as potent analgesics in animal models of chronic pain. However, a number of α-conotoxins have been shown to inhibit N-type calcium channel currents in rodent dissociated dorsal root ganglion (DRG) neurons via activation of G protein-coupled GABAB receptors (GABABR). Therefore it is unclear whether activation of GABABR or inhibition of α9α10 nAChRs is the analgesic mechanism...
May 10, 2018: ACS Chemical Biology
https://www.readbyqxmd.com/read/29743034/glial-cell-line-derived-neurotrophic-factor-gdnf-attenuates-the-peripheral-neuromuscular-dysfunction-without-inhibiting-the-activation-of-spinal-microglia-monocyte
#13
Fei Xie, Fan Zhang, Su Min, Jingyuan Chen, Jun Yang, Xin Wang
BACKGROUND: Peripheral neuromuscular dysfunctions were found in elderly individuals, and spinal microglia/monocyte plays an important role on this process. This study aims to test whether the glial cell line-derived neurotrophic factor (GDNF) could attenuate age-related neuromuscular dysfunction by inhibiting the activation of spinal microglia/monocyte. METHODS: Male Sprague-Dawley rats were divided into an adult group and an aged group. The aged rats were intrathecally injected with normal saline (NS) and GDNF...
May 9, 2018: BMC Geriatrics
https://www.readbyqxmd.com/read/29739869/synaptic-release-of-acetylcholine-rapidly-suppresses-cortical-activity-by-recruiting-muscarinic-receptors-in-layer-4
#14
Rajan Dasgupta, Frederik Seibt, Michael Beierlein
Cholinergic afferents from the basal forebrain (BF) can influence cortical activity on rapid time scales, enabling sensory information processing and exploratory behavior. However, our understanding of how synaptically released acetylcholine (ACh) influences cellular targets in distinct cortical layers remains incomplete. Previous studies have shown that rapid changes in cortical dynamics induced by phasic BF activity can be mediated by the activation of nicotinic ACh receptors (nAChRs) expressed in distinct types of GABAergic interneurons...
May 8, 2018: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/29735728/the-nicotinic-acetylcholine-receptor-a-typical-allosteric-machine
#15
REVIEW
Jean-Pierre Changeux
The concept of allosteric interaction was initially proposed to account for the inhibitory feedback mechanism mediated by bacterial regulatory enzymes. In contrast with the classical mechanism of competitive, steric, interaction between ligands for a common site, allosteric interactions take place between topographically distinct sites and are mediated by a discrete and reversible conformational change of the protein. The concept was soon extended to membrane receptors for neurotransmitters and shown to apply to the signal transduction process which, in the case of the acetylcholine nicotinic receptor (nAChR), links the ACh binding site to the ion channel...
June 19, 2018: Philosophical Transactions of the Royal Society of London. Series B, Biological Sciences
https://www.readbyqxmd.com/read/29733889/adenosine-promotes-endplate-nachr-channel-activity-in-adult-mouse-skeletal-muscle-fibres-via-low-affinity-p1-receptors
#16
Annalisa Bernareggi, Elisa Ren, Arthur Giniatullin, Elisa Luin, Marina Sciancalepore, Rashid Giniatullin, Paola Lorenzon
Adenosine is a powerful modulator of skeletal neuromuscular transmission, operating via inhibitory or facilitatory purinergic-type P1 receptors. To date, studies have been focused mainly on the effect of adenosine on presynaptic P1 receptors controlling transmitter release. In this study, using two-microelectrode voltage clamp and single channel patch-clamp recording techniques, we have explored potential postsynaptic targets of adenosine and their modulatory effect on nicotinic acetylcholine receptor (nAChR)-mediated synaptic responses in adult mouse skeletal muscle fibres in vitro...
May 4, 2018: Neuroscience
https://www.readbyqxmd.com/read/29733583/molecular-determinants-conferring-the-stoichiometric-dependent-activity-of-%C3%AE-conotoxins-at-the-human-%C3%AE-9%C3%AE-10-nicotinic-acetylcholine-receptor-subtype
#17
Rilei Yu, Han-Shen Tae, Nargis Tabassum, Juan Shi, Tao Jiang, David J Adams
α9α10 Nicotinic acetylcholine receptors (nAChRs) putatively exist at different stoichiometries. We systematically investigated the molecular determinants of α-conotoxins Vc1.1, RgIA#, and PeIA inhibition at hypothetical stoichiometries of the human α9α10 nAChR. Our results suggest that only Vc1.1 exhibits stoichiometric-dependent inhibition at the α9α10 nAChR. The hydrogen bond between N154 of α9 and D11 of Vc1.1 at the α9(+)-α9(-) interface is responsible for the stoichiometric-dependent potency of Vc1...
May 7, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29732929/drug-development-for-alzheimer-s-disease-review
#18
Kejing Lao, Naichun Ji, Xiaohua Zhang, Wenwei Qiao, Zhishu Tang, Xingchun Gou
Alzheimer's disease (AD) is a chronic neurodegenerative disease, which is considered one of the most intractable medical problems with heavy social and economic costs. The current drugs for AD, including acetylcholinesterase inhibitors (AChEIs) and memantine, a NMDA receptor antagonist, only temporarily ameliorate cognitive decline, but are unable to stop or reverse the progression of dementia. This paper reviewed the recent advance in AD drug development. The drug discovery programs under clinical trials targeting cholinergic system, α7 nicotinic acetylcholine receptors (nAChRs), N-methyl-D-aspartate receptor (NMDAR), β-secretase, γ-secretase modulators, tau, inflammatory mediators and glucagon-like peptide-1 (GLP-1) were discussed...
May 7, 2018: Journal of Drug Targeting
https://www.readbyqxmd.com/read/29730150/neurotoxicity-fingerprinting-of-venoms-using-on-line-microfluidic-achbp-profiling
#19
Julien Slagboom, Reka A Otvos, Fernanda C Cardoso, Janaki Iyer, Jeroen C Visser, Bjorn R van Doodewaerd, Ryan J R McCleary, Wilfried M A Niessen, Govert W Somsen, Richard J Lewis, R Manjunatha Kini, August B Smit, Nicholas R Casewell, Jeroen Kool
Venoms from snakes are rich sources of highly active proteins with potent affinity towards a variety of enzymes and receptors. Of the many distinct toxicities caused by envenomation, neurotoxicity plays an important role in the paralysis of prey by snakes as well as by venomous sea snails and insects. In order to improve the analytical discovery component of venom toxicity profiling, this paper describes the implementation of microfluidic high-resolution screening (HRS) to obtain neurotoxicity fingerprints from venoms that facilitates identification of the neurotoxic components of envenomation...
May 3, 2018: Toxicon: Official Journal of the International Society on Toxinology
https://www.readbyqxmd.com/read/29724797/stoichiometry-of-the-heteromeric-nicotinic-receptors-of-the-renshaw-cell
#20
Boris Lamotte d'Incamps, Tamara Zorbaz, Dominika Dingova, Eric Krejci, Philippe Ascher
Neuronal nicotinic acetylcholine receptors (nAChRs) are pentamers built from a variety of subunits. Some are homomeric assemblies of α subunits, others heteromeric assemblies of α and β subunits which can adopt two stoichiometries (2α:3β or 3α:2β). There is evidence for the presence of heteromeric nAChRs with the two stoichiometries in the CNS, but it has not yet been possible to identify them at a given synapse. The 2α:3β receptors are highly sensitive to agonists, whereas the 3α:2β stoichiometric variants, initially described as low sensitivity receptors, are in fact activated by low and high concentrations of ACh...
May 3, 2018: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
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