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https://www.readbyqxmd.com/read/29146291/development-of-ms-binding-assays-targeting-the-binding-site-of-mb327-at-the-nicotinic-acetylcholine-receptor
#1
S Sichler, G Höfner, S Rappenglück, T Wein, K V Niessen, T Seeger, F Worek, H Thiermann, F F Paintner, K T Wanner
The bispyridinium compound MB327 has been shown previously to have a positive pharmacological effect against poisoning with organophosphorous compounds (OPCs). The mechanism by which it exerts its therapeutic effect seems to be directly mediated by the nicotinic acetylcholine receptor (nAChR). In the present study, the development of mass spectrometry based binding assays (MS Binding Assays) for characterization of the binding site of MB327 at the nAChR from Torpedo californica is described. MS Binding Assays follow the principle of radioligand binding assays, but do not, in contrast to the latter, require a radiolabeled reporter ligand, as the readout is in this case based on mass spectrometric detection...
November 13, 2017: Toxicology Letters
https://www.readbyqxmd.com/read/29131336/molecular-function-of-%C3%AE-7-nicotinic-receptors-as-drug-targets
#2
Cecilia Bouzat, Matías Lasala, Beatriz Elizabeth Nielsen, Jeremías Corradi, María Del Carmen Esandi
Nicotinic acetylcholine receptors (nAChR) are pentameric ligand-gated ion channels involved in many physiological and pathological processes. In vertebrates, there are seventeen different nAChR subunits that combine to yield a variety of receptors with different pharmacology, function, and localization. The homomeric α7 receptor is one of the most abundant nAChRs in the nervous system and it is also present in non-neuronal cells. It plays important roles in cognition, memory, pain, neuroprotection, and inflammation...
November 13, 2017: Journal of Physiology
https://www.readbyqxmd.com/read/29129316/functional-consequences-of-chrna7-copy-number-alterations-in-induced-pluripotent-stem-cells-and-neural-progenitor-cells
#3
Madelyn A Gillentine, Jiani Yin, Aleksandar Bajic, Ping Zhang, Steven Cummock, Jean J Kim, Christian P Schaaf
Copy-number variants (CNVs) of chromosome 15q13.3 manifest clinically as neuropsychiatric disorders with variable expressivity. CHRNA7, encoding for the α7 nicotinic acetylcholine receptor (nAChR), has been suggested as a candidate gene for the phenotypes observed. Here, we used induced pluripotent stem cells (iPSCs) and neural progenitor cells (NPCs) derived from individuals with heterozygous 15q13.3 deletions and heterozygous 15q13.3 duplications to investigate the CHRNA7-dependent molecular consequences of the respective CNVs...
November 4, 2017: American Journal of Human Genetics
https://www.readbyqxmd.com/read/29118361/behavioral-changes-after-nicotine-challenge-are-associated-with-%C3%AE-7-nicotinic-acetylcholine-receptor-stimulated-glutamate-release-in-the-rat-dorsal-striatum
#4
In Soo Ryu, Jieun Kim, Su Yeon Seo, Ju Hwan Yang, Jeong Hwan Oh, Dong Kun Lee, Hyun-Wook Cho, Seong Shoon Yoon, Joung-Wook Seo, Suchan Chang, Hee Young Kim, Insop Shim, Eun Sang Choe
Neurochemical alterations associated with behavioral responses induced by re-exposure to nicotine have not been sufficiently characterized in the dorsal striatum. Herein, we report on changes in glutamate concentrations in the rat dorsal striatum associated with behavioral alterations after nicotine challenge. Nicotine challenge (0.4 mg/kg/day, subcutaneous) significantly increased extracellular glutamate concentrations up to the level observed with repeated nicotine administration. This increase occurred in parallel with an increase in behavioral changes in locomotor and rearing activities...
November 8, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29117550/microrna-regulation-of-nachr-expression-and-nicotine-dependent-behavior-in-c-%C3%A2-elegans
#5
Manish Rauthan, Jianke Gong, Jinzhi Liu, Zhaoyu Li, Seth A Wescott, Jianfeng Liu, X Z Shawn Xu
Chronic exposure to nicotine upregulates nicotinic acetylcholine receptors (nAChRs), and such upregulation is critical for the development of nicotine dependence in humans and animal models. However, how nicotine upregulates nAChRs is not well understood. Here, we identify a key role for microRNA in regulating nicotine-dependent behavior by modulating nAChR expression in C. elegans. We show that the nAChR gene acr-19 and alg-1, a key Argonaute-family member in the microRNA machinery, are specifically required for nicotine withdrawal response following chronic nicotine treatment...
November 7, 2017: Cell Reports
https://www.readbyqxmd.com/read/29117258/lung-epithelial-response-to-cigarette-smoke-and-modulation-by-the-nicotinic-alpha-7-receptor
#6
Lorise C Gahring, Elizabeth J Myers, Diane M Dunn, Robert B Weiss, Scott W Rogers
Cigarette smoking (CS) is a principal contributor to a spectrum of devastating lung diseases whose occurrence and severity may vary between individuals and not appear for decades after prolonged use. One explanation for the variability and delay in disease onset is that nicotine, the addictive component of CS, acts through the ionotropic nicotinic acetylcholine receptor (nAChR) alpha7 (α7) to modulate anti-inflammatory protection. In this study we measured the impact α7 signaling has on the mouse distal lung response to side-stream CS exposure for mice of the control genotype (α7G) and those in which the α7-receptor signaling mechanisms are restricted by point mutation (α7E260A:G)...
2017: PloS One
https://www.readbyqxmd.com/read/29114204/acute-ethanol-administration-upregulates-synaptic-%C3%AE-4-subunit-of-neuronal-nicotinic-acetylcholine-receptors-within-the-nucleus-accumbens-and-amygdala
#7
Josephine R Tarren, Henry A Lester, Arnauld Belmer, Selena E Bartlett
Alcohol and nicotine are two of the most frequently abused drugs, with their comorbidity well described. Previous data show that chronic exposure to nicotine upregulates high-affinity nicotinic acetylcholine receptors (nAChRs) in several brain areas. Effects of ethanol on specific brain nAChR subtypes within the mesolimbic dopaminergic (DA) pathway may be a key element in the comorbidity of ethanol and nicotine. However, it is unknown how alcohol affects the abundance of these receptor proteins. In the present study, we measured the effect of acute binge ethanol on nAChR α4 subunit levels in the prefrontal cortex (PFC), nucleus accumbens (NAc), ventral tegmental area (VTA), and amygdala (Amg) by western blot analysis using a knock-in mouse line, generated with a normally functioning α4 nAChR subunit tagged with yellow fluorescent protein (YFP)...
2017: Frontiers in Molecular Neuroscience
https://www.readbyqxmd.com/read/29114104/bidirectional-regulation-of-aggression-in-mice-by-hippocampal-alpha-7-nicotinic-acetylcholine-receptors
#8
Alan S Lewis, Steven T Pittenger, Yann S Mineur, Dawson Stout, Philip H Smith, Marina R Picciotto
Humans with 15q13.3 microdeletion syndrome (15q13.3DS) are typically hemizygous for CHRNA7, the gene coding for the α7 nicotinic acetylcholine receptor (nAChR), and manifest a variable neuropsychiatric phenotype that frequently includes persistent aggression. In mice, nAChR activation by nicotine is anti-aggressive, or 'serenic', an effect which requires α7 nAChRs and is recapitulated by GTS-21, an α7 nAChR partial agonist. Pharmacotherapies potentiating α7 nAChR signaling have also been shown to reduce aggression in human 15q13...
November 7, 2017: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/29110618/cognitive-effects-of-nicotine-recent-progress
#9
Gerald Valentine, Mehmet Sofuoglu
Cigarette smoking is the main cause of preventable death in developed countries. Given the limited effectiveness of currently available treatments, there is a great need to identify new treatment approaches for tobacco use disorder (TUD). While the direct positive behavioral reinforcing effect of nicotine has historically been considered the primary mechanism driving the development of TUD, accumulating contemporary research suggests that the cognitive-enhancing effects of nicotine may also significantly contribute to the initiation and maintenance of TUD, especially in individuals with pre-existing cognitive deficits...
November 3, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/29105121/evaluation-of-18-f-flubatine-specific-binding-implications-for-reference-region-approaches
#10
Shivani Bhatt, Ansel T Hillmer, Nabeel Nabulsi, David Matuskey, Keunpoong Lim, Shu-Fei Lin, Irina Esterlis, Richard E Carson, Yiyun Huang, Kelly P Cosgrove
We aimed to characterize changes in binding of (-)-[(18) F]Flubatine to α4 β2 *-nicotinic acetylcholine receptors (α4 β2 *-nAChRs) during a tobacco cigarette smoking challenge. Displacement of (-)-[(18) F]Flubatine throughout the brain was quantified as change in (-)-[(18) F]Flubatine distribution volume (VT ), with particular emphasis on regions with low VT . Three tobacco smokers were imaged with positron emission tomography (PET) during a 210-min bolus-plus-constant infusion of (-)-[(18) F]Flubatine...
November 3, 2017: Synapse
https://www.readbyqxmd.com/read/29100122/human-exposure-to-neonicotinoid-insecticides-and-the-evaluation-of-their-potential-toxicity-an-overview
#11
REVIEW
Wenchao Han, Ying Tian, Xiaoming Shen
Neonicotinoid insecticides have become the fastest growing class of insecticides over the past few decades. The insecticidal activity of neonicotinoids is attributed to their agonist action on nicotinic acetylcholine receptors (nAChRs). Because of the special selective action on nAChRs in central nervous system of insects, and versatility in application methods, neonicotinoids are used to protect crops and pets from insect attacks globally. Although neonicotinoids are considered low toxicity to mammals and humans in comparison with traditional insecticides, more and more studies show exposure to neonicotinoids pose potential risk to mammals and even humans...
October 27, 2017: Chemosphere
https://www.readbyqxmd.com/read/29097222/searching-for-putative-binding-sites-of-the-bispyridinium-compound-mb327-in-the-nicotinic-acetylcholine-receptor
#12
Thomas Wein, Georg Höfner, Sebastian Rappenglück, Sonja Sichler, Karin V Niessen, Thomas Seeger, Franz Worek, Horst Thiermann, Klaus T Wanner
Irreversible inhibition of the acetylcholine esterase upon intoxication with organophosphorus compounds leads to an accumulation of acetylcholine in the synaptic cleft and a subsequent desensitization of nicotinic acetylcholine receptors which may ultimately result in respiratory failure. The bispyridinium compound MB327 has been found to restore functional activity of nAChR thus representing a promising starting point for the development of new drugs for the treatment of organophosphate poisoning. In order to optimize the resensitizing effect of MB327 on nAChR, it would be very helpful to know the MB327 specific binding site to apply structure based molecular modeling...
October 30, 2017: Toxicology Letters
https://www.readbyqxmd.com/read/29095106/deletion-of-the-nicotinic-acetylcholine-receptor-subunit-gene-d%C3%AE-1-confers-insecticide-resistance-but-at-what-cost
#13
Jason Somers, Hang Ngoc Bao Luong, Philip Batterham, Trent Perry
Nicotinic acetylcholine receptors (nAChRs) have vital functions in processes of neurotransmission that underpin key behaviors. These pentameric ligand-gated ion channels have been used as targets for insecticides that constitutively activate them, causing the death of insect pests. In examining a knockout of the Dα1 nAChR subunit gene, our study linked this one subunit with multiple traits. We were able to confirm previous work that had identified Dα1 as a target of the neonicotinoid class of insecticides...
November 2, 2017: Fly
https://www.readbyqxmd.com/read/29080744/effect-of-dexmedetomidine-on-rats-with-convulsive-status-epilepticus-and-association-with-activation-of-cholinergic-anti-inflammatory-pathway
#14
Kai-Liang Xu, Xin-Qiu Liu, Yu-Long Yao, Ming-Rong Ye, Yao-Guo Han, Tao Zhang, Gang Chen, Ming Lei
Convulsive status epilepticus (CSE) is a neurological disease with contraction and extension of limbs, leading to damage of hippocampus and cognition. This study aimed to explore the effects of dexmedetomidine (DEX) on the cognitive function and neuroinflammation in CSE rats. All rats were divided into control group, CSE group and DEX group. Morris water maze test was used to measure cognitive function. Acute hippocampal slices were made to detect long-term potentiation (LTP). Immunohistochemistry was used to determine the expression of α7-nicotinic acetylcholine receptor (α7-nAChR) and interleukin-1β (IL-1β)...
November 11, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29074617/organelle-specific-single-molecule-imaging-of-%C3%AE-4%C3%AE-2-nicotinic-receptors-reveals-the-effect-of-nicotine-on-receptor-assembly-and-cell-surface-trafficking
#15
Ashley M Fox-Loe, Faruk H Moonschi, Christopher I Richards
Nicotinic acetylcholine receptors (nAChRs) assemble in the endoplasmic reticulum (ER) and traffic to the cell surface as pentamers composed of alpha and beta subunits. Many nAChR subtypes can assemble with varying subunit ratios, giving rise to multiple stoichiometries exhibiting different subcellular localization and functional properties. In addition to the endogenous neurotransmitter acetylcholine, nicotine also binds and activates nAChRs and influences their trafficking and expression on the cell surface...
October 26, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/29066952/the-sleep-wake-cycle-in-the-nicotinic-alpha-9-acetylcholine-receptor-subunit-knock-out-mice
#16
Natalia Madrid-López, Jorge Estrada, Javier Díaz, Alejandro Bassi, Paul H Délano, Adrián Ocampo-Garcés
There is a neural matrix controlling the sleep-wake cycle (SWC) embedded within high ranking integrative mechanisms in the central nervous system. Nicotinic alpha-9 acetylcholine receptor subunit (alpha-9 nAChR) participate in physiological processes occurring in sensory, endocrine and immune systems. There is a relationship between the SWC architecture, body homeostasis and sensory afferents so that disruption of afferent signaling is expected to affect the temporal organization of sleep and wake states. The analysis of the SWC of 9 nAChR knock-out animals may help to reveal the contribution of alpha-9 nAChR to sleep chronobiological determinants...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/29064842/effect-of-varenicline-on-behavioral-deficits-in-a-rat-model-of-parkinson-s-disease-induced-by-unilateral-6-hydroxydopamine-lesion-of-substantia-nigra
#17
Rüyal Tan, Funda Bölükbaşi Hatip, Öznur Açikalin, Atsushi Yamauchi, Yasufumi Kataoka, Izzettin Hatip-Al-Khatib
Nicotinic acetylcholine receptors (nAChRs) are implicated in the pathogenesis of Parkinson's disease (PD). Varenicline tartrate is a partial agonist at α4β2 and full agonist at α7 neuronal nAChR subunits. A unilateral lesion of the substantia nigra (SN) has been used as a reliable model of PD. This study aimed to investigate the effect of varenicline on locomotor and nonlocomotor behavioral deficits induced by a unilateral lesion of the SN induced by 6-hydroxydopamine (6-OHDA) (8 µg/4 µl). Varenicline (1 mg/kg) was administered to the lesioned rats daily for 2 weeks, which commenced 3 weeks after 6-OHDA administration...
October 23, 2017: Behavioural Pharmacology
https://www.readbyqxmd.com/read/29062606/the-neuroprotective-effect-of-nicotine-in-parkinson-s-disease-models-is-associated-with-inhibiting-parp-1-and-caspase-3-cleavage
#18
Justin Y D Lu, Ping Su, James E M Barber, Joanne E Nash, Anh D Le, Fang Liu, Albert H C Wong
Clinical evidence points to neuroprotective effects of smoking in Parkinson's disease (PD), but the molecular mechanisms remain unclear. We investigated the pharmacological pathways involved in these neuroprotective effects, which could provide novel ideas for developing targeted neuroprotective treatments for PD. We used the ETC complex I inhibitor methylpyridinium ion (MPP(+)) to induce cell death in SH-SY5Y cells as a cellular model for PD and found that nicotine inhibits cell death. Using choline as a nicotinic acetylcholine receptor (nAChR) agonist, we found that nAChR stimulation was sufficient to protect SH-SY5Y cells against cell death from MPP(+)...
2017: PeerJ
https://www.readbyqxmd.com/read/29061702/presynaptic-neuronal-nicotinic-receptors-differentially-shape-select-inputs-to-auditory-thalamus-and-are-negatively-impacted-by-aging
#19
Sarah Y Sottile, Troy A Hackett, Rui Cai, Lynne Ling, Daniel A Llano, Donald M Caspary
Acetylcholine is a potent neuromodulator capable of modifying patterns of acoustic information flow. In auditory cortex, cholinergic systems have been shown to increase salience/gain while suppressing extraneous information. However, the mechanism by which cholinergic circuits shape signal processing in the auditory thalamus (medial geniculate body, MGB) is poorly understood. The present study, in male Fischer Brown Norway rats, seeks to determine the location and function of presynaptic neuronal nicotinic acetylcholine receptors (nAChRs) at the major inputs to MGB and characterize how nAChRs change during aging...
October 23, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/29059422/reversal-of-nicotine-withdrawal-signs-through-positive-allosteric-modulation-of-%C3%AE-4%C3%AE-2-nicotinic-acetylcholine-receptors-in-male-mice
#20
Ayman K Hamouda, Asti Jackson, Deniz Bagdas, M Imad Damaj
Introduction: Nicotine withdrawal symptoms are important factors in determining the relapse rate to tobacco smoking and drugs that diminish these symptoms would potentially have a higher success rate as smoking cessation aids. Unlike FDA-approved smoke cessation aids (nicotine and varenicline) which act as nicotinic acetylcholine receptors (nAChRs) agonists, desformylflustrabromine (dFBr) acts as a nAChR positive allosteric modulator with higher selectivity to the α4β2 nAChR. In animal studies, dFBr was well tolerated and reduced intravenous nicotine self-administration...
August 18, 2017: Nicotine & Tobacco Research: Official Journal of the Society for Research on Nicotine and Tobacco
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