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https://www.readbyqxmd.com/read/28651369/reduced-thalamus-volume-may-reflect-nicotine-severity-in-young-male-smokers
#1
Dahua Yu, Kai Yuan, Jiadong Cheng, Yanyan Guan, Yangding Li, Yanzhi Bi, Jinquan Zhai, Lin Luo, Bo Liu, Ting Xue, Xiaoqi Lu
Introduction: Nicotine acts as an agonist at presynaptic nicotinic acetylcholine receptors (nAChRs) and to facilitate synaptic release of several neurotransmitters including dopamine and glutamate. The thalamus has the highest density of nAChRs in the brain, which may make this area be more vulnerable to the addictive effects of nicotine. However, the volume of thalamus abnormalities and the association with smoking behaviors in young smokers remains unknown. Methods: Thirty-six young male smokers and 36 age-, gender- and education-matched nonsmokers participated in current study...
June 23, 2017: Nicotine & Tobacco Research: Official Journal of the Society for Research on Nicotine and Tobacco
https://www.readbyqxmd.com/read/28648825/differential-control-of-dopaminergic-excitability-and-locomotion-by-cholinergic-inputs-in-mouse-substantia-nigra
#2
Jasem Estakhr, Danya Abazari, Kaitlyn Frisby, J Michael McIntosh, Raad Nashmi
Understanding how dopaminergic (DA) neurons of the substantia nigra pars compacta (SNc) govern movements requires a detailed knowledge of how different neurotransmitter systems modulate DA neuronal excitability. We report a heterogeneity of electrophysiological properties between medial and lateral SNc neurons modulated by cholinergic neurotransmission. Lateral DA neurons received mainly excitatory (nicotinic or glutamatergic) mediated cholinergic neurotransmission. Medial DA neurons received predominantly GABAergic currents mediated by presynaptic nicotinic receptors or biphasic GABAergic and nicotinic neurotransmission conveyed by GABA and ACh corelease, which inhibited DA neurons...
June 20, 2017: Current Biology: CB
https://www.readbyqxmd.com/read/28647281/serotonergic-modulation-of-nicotine-induced-kinetic-tremor-in-mice
#3
Naofumi Kunisawa, Higor A Iha, Yuji Nomura, Misaki Onishi, Nami Matsubara, Saki Shimizu, Yukihiro Ohno
We previously demonstrated that nicotine elicited kinetic tremor by elevating the neural activity of the inferior olive via α7 nicotinic acetylcholine (nACh) receptors. Since α7 nACh receptors reportedly facilitate synaptic monoamine release, we explored the role of 5-HT receptors in induction and/or modulation of nicotine tremor. Treatment of mice with nicotine induced kinetic tremor that normally appeared during movement. The 5-HT1A agonist, 8-hydroxydipropylaminotetraline (8-OH-DPAT), significantly enhanced nicotine-induced tremor and the action of 8-OH-DPAT was antagonized by WAY-100135 (5-HT1A antagonist)...
June 9, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28646714/synthetic-cathinones-and-stereochemistry-s-enantiomer-of-mephedrone-reduces-anxiety-and-depressant-like-effects-in-cocaine-or-mdpv-abstinent-rats
#4
Helene L Philogene-Khalid, Callum Hicks, Allen B Reitz, Lee-Yuan Liu-Chen, Scott M Rawls
BACKGROUND AND PURPOSE: The neuropharmacological profile of the synthetic cathinone mephedrone (MEPH) is influenced by stereochemistry. Both MEPH enantiomers are monoamine transporter substrates, but R-MEPH is primarily responsible for rewarding effects of MEPH as it produces greater locomotor activation and intracranial self-stimulation than S-MEPH. S-MEPH is a 50-fold more potent 5-HT releaser than R-MEPH and does not place preference in rats. MEPH is also structurally similar to the cathinone derivative bupropion, an antidepressant and smoking cessation medication, suggesting MEPH has therapeutic and addictive properties...
June 13, 2017: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/28644870/effects-of-nicotine-on-corneal-wound-healing-following-acute-alkali-burn
#5
Jong Won Kim, Chae Woong Lim, Bumseok Kim
Epidemiological studies have indicated that smoking is a pivotal risk factor for the progression of several chronic diseases. Nicotine, the addictive component of cigarettes, has powerful pathophysiological properties in the body. Although the effects of cigarette smoking on corneal re-epithelialization have been studied, the effects of nicotine on corneal wound healing-related neovascularization and fibrosis have not been fully demonstrated. The aim of this study was to evaluate the effects of chronic administration of nicotine on corneal wound healing following acute insult induced by an alkali burn...
2017: PloS One
https://www.readbyqxmd.com/read/28642492/segregation-of-glutamatergic-and-cholinergic-transmission-at-the-mixed-motoneuron-renshaw-cell-synapse
#6
Boris Lamotte d'Incamps, Gardave S Bhumbra, Joshua D Foster, Marco Beato, Philippe Ascher
In neonatal mice motoneurons excite Renshaw cells by releasing both acetylcholine (ACh) and glutamate. These two neurotransmitters activate two types of nicotinic receptors (nAChRs) (the homomeric α7 receptors and the heteromeric α*ß* receptors) as well as the two types of glutamate receptors (GluRs) (AMPARs and NMDARs). Using paired recordings, we confirm that a single motoneuron can release both transmitters on a single post-synaptic Renshaw cell. We then show that co-transmission is preserved in adult animals...
June 22, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28641950/cholinergic-signaling-plasticity-maintains-viscerosensory-responses-during-aspiculuris-tetraptera-infection-in-mice-small-intestine
#7
Egina C Villalobos-Hernández, Carlos Barajas-López, Elizabeth A Martínez-Salazar, Roberto C Salgado-Delgado, Marcela Miranda-Morales
Intestinal parasites alter gastrointestinal (GI) functions like the cholinergic function. Aspiculuris tetraptera is a pinworm frequently observed in laboratory facilities, which infests the mice cecum and proximal colon. However, little is known about the impact of this infection on the GI sensitivity. Here, we investigated possible changes in spontaneous mesenteric nerve activity and on the mechanosensitivity function of worm-free regions of naturally infected mice with A. tetraptera. Infection increased the basal firing of mesenteric afferent nerves in jejunum...
June 3, 2017: Autonomic Neuroscience: Basic & Clinical
https://www.readbyqxmd.com/read/28638646/crystal-structure-of-4-4-bis-3-piperidin-1-yl-prop-1-yn-1-yl-1-1-biphen-yl
#8
Anqi Walbaum, E Kim Fifer, Sean Parkin, Peter A Crooks
The title compound, C28H32N2, (I), is one of a second generation of compounds designed and synthesized based on a very potent and selective α9α10 nicotinic acetyl-choline receptor antagonist ZZ161C {1,1'-[[1,1'-biphen-yl]-4,4'-diylbis(prop-2-yne-3,1-di-yl)]bis-(3,4-di-methyl-pyridin-1-ium) bromide}, which has shown analgesic effects in a chemotherapy-induced neuropathy animal model. Compound (I) was synthesized by the reaction of 4,4'-bis-(3-bromo-prop-1-yn-1-yl)-1,1'-biphenyl with piperidine at room temperature in aceto-nitrile...
June 1, 2017: Acta Crystallographica. Section E, Crystallographic Communications
https://www.readbyqxmd.com/read/28632446/multitarget-drug-design-strategy-in-alzheimer-s-disease-focus-on-cholinergic-transmission-and-amyloid-%C3%AE-aggregation
#9
Elena Simoni, Manuela Bartolini, Izuddin F Abu, Alix Blockley, Cecilia Gotti, Giovanni Bottegoni, Roberta Caporaso, Christian Bergamini, Vincenza Andrisano, Andrea Cavalli, Ian R Mellor, Anna Minarini, Michela Rosini
AIM: Alzheimer pathogenesis has been associated with a network of processes working simultaneously and synergistically. Over time, much interest has been focused on cholinergic transmission and its mutual interconnections with other active players of the disease. Besides the cholinesterase mainstay, the multifaceted interplay between nicotinic receptors and amyloid is actually considered to have a central role in neuroprotection. Thus, the multitarget drug-design strategy has emerged as a chance to face the disease network...
June 20, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28631100/co-modulation-of-an-allosteric-modulator-of-nicotinic-receptor-cholinesterase-inhibitor-galantamine-and-a-5-ht4-receptor-agonist-rs-67333-effect-on-scopolamine-induced-memory-deficit-in-the-mouse
#10
Thomas Freret, Véronique Lelong-Boulouard, Pierre Lecouflet, Katia Hamidouche, François Dauphin, Michel Boulouard
AIM: It is widely assumed that the upcoming therapeutics for Alzheimer's disease will require to act on more than one target to be effective. We investigated here whether a combination of the nicotinic receptor allosteric modulator/cholinesterase inhibitor galantamine can act synergistically with the type 4 serotonin receptor (5-HT4R) partial agonist, RS-67333, to counterbalance deficits in short- and long-term memory. To select sub-efficacious doses of both drugs, dose-response studies were first performed on the scopolamine-induced deficits of spontaneous alternation in the Y-maze task and of acquisition and retrieval processes in a passive avoidance task...
June 19, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28630263/determination-of-the-residues-in-the-extracellular-domain-of-the-nicotinic-%C3%AE-subunit-required-for-the-actions-of-physostigmine-on-neuronal-nicotinic-receptors
#11
Xiaochun Jin, Allison L Germann, Daniel J Shin, Gustav Akk, Joseph H Steinbach
Physostigmine can potentiate and inhibit neuronal nicotinic receptors, in addition to inhibiting the activity of acetylcholinesterase. We found that receptors containing 3 copies of the α2 subunit are inhibited by low concentrations of physostigmine in contrast to receptors containing 3 copies of the α4 subunit that are potentiated. We exploited this observation to determine regions required for the actions of physostigmine. Chimeric constructs of the α2 and α4 subunits located two regions in the extracellular amino-terminal domain of the subunit: the E loop (a loop of the transmitter-binding domain) and a region closer to the amino-terminus that collectively could completely determine the different effects of physostigmine...
June 19, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/28626386/minimal-effects-of-age-and-exposure-to-a-noisy-environment-on-hearing-in-alpha9-nicotinic-receptor-knockout-mice
#12
Amanda M Lauer
Studies have suggested a role of weakened medial olivocochlear (OC) efferent feedback in accelerated hearing loss and increased susceptibility to noise. The present study investigated the progression of hearing loss with age and exposure to a noisy environment in medial OC-deficient mice. Alpha9 nicotinic acetylcholine receptor knockout (α9KO) and wild types were screened for hearing loss using auditory brainstem responses. α9KO mice housed in a quiet environment did not show increased hearing loss compared to wild types in young adulthood and middle age...
2017: Frontiers in Neuroscience
https://www.readbyqxmd.com/read/28625505/bioequivalence-study-of-a-new-fixed-dose-combination-tablet-containing-s-amlodipine-nicotinate-and-olmesartan-medoxomil-in-healthy-korean-male-subjects
#13
Mi Jin Oh, Hyun Hwan Hwang, Hyun Gyu Kim, Geun Hyeog Lee, Yun-Seok Cho, Sun Young Lee, Soo Yeon Kang, Kyung Hee Cho, Yun Young Lee, Yun Jeong Lee, Choon-Gon Jang, Seok-Yong Lee
PURPOSE: A fixed-dose combination (FDC) pill of amlodipine (relatively old calcium channel blocker as dihydropyridine) and olmesartan (relatively new angiotensin II receptor blocker) is used for hypertension that is not adequately controlled with a single-formulation drug. Because the FDC is a one-pill formulation, and amlodipine and olmesartan have different mechanisms of action, it is expected to improve patients' medication compliance and have an increased blood pressure-lowering efficacy...
June 15, 2017: Clinical Therapeutics
https://www.readbyqxmd.com/read/28625139/targeting-cholinergic-system-to-modulate-liver-injury
#14
Ravirajsinh N Jadeja, Vikrant P Rachakonda, Sandeep Khurana
Over the past few decades, evidence accumulated to indicate that parasympathetic innervation regulates liver injury and regeneration. Liver derives its parasympathetic input via vagus nerve. In animal models, vagus nerve stimulation and transection are frequently used to determine the impact of parasympathetic input on liver injury responses. Such strategies provide limited understanding of post-neuronal mechanisms involved in regulation of liver injury. The hepatic branch of vagus nerve releases acetylcholine (ACh), which activates muscarinic and nicotinic receptors in hepatocytes as well as non-parenchymal cells to modulate cellular functions...
June 18, 2017: Current Drug Targets
https://www.readbyqxmd.com/read/28623170/nicotinic-acetylcholine-receptor-inhibitors-derived-from-snake-and-snail-venoms
#15
REVIEW
Sebastien Dutertre, Annette Nicke, Victor Tsetlin
The nicotinic acetylcholine receptor (nAChR) represents the prototype of ligand-gated ion channels. It is vital for neuromuscular transmission and an important regulator of neurotransmission. A variety of toxic compounds derived from diverse species target this receptor and have been of elemental importance in basic and applied research. They enabled milestone discoveries in pharmacology and biochemistry ranging from the original formulation of the receptor concept, the first isolation and structural analysis of a receptor protein (the nAChR) to the identification, localization, and differentiation of its diverse subtypes and their validation as a target for therapeutic intervention...
June 13, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28623168/access-to-nicotine-in-drinking-water-reduces-weight-gain-without-changing-caloric-intake-on-high-fat-diet-in-male-c57bl-6j-mice
#16
Cali A Calarco, Somin Lee, Marina R Picciotto
Nicotine and tobacco use is associated with lower body weight, and many smokers report concerns about weight. In animal studies, nicotine reduces weight gain, reduces food consumption, and alters energy expenditure, but these effects vary with duration and route of nicotine administration. Previous studies have used standardized nicotine doses, however, in this study, male and female mice had free access to nicotine drinking water for 30 days while fed either a high fat diet (HFD) or chow, allowing animals to titrate their nicotine intake...
June 13, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28620379/neuroimmune-interactions-in-schizophrenia-focus-on-vagus-nerve-stimulation-and-activation-of-the-alpha-7-nicotinic-acetylcholine-receptor
#17
REVIEW
Fabiana Maria das Graças Corsi-Zuelli, Fernanda Brognara, Gustavo Fernando da Silva Quirino, Carlos Hiroji Hiroki, Rafael Sobrano Fais, Cristina Marta Del-Ben, Luis Ulloa, Helio Cesar Salgado, Alexandre Kanashiro, Camila Marcelino Loureiro
Schizophrenia is one of the most debilitating mental disorders and is aggravated by the lack of efficacious treatment. Although its etiology is unclear, epidemiological studies indicate that infection and inflammation during development induces behavioral, morphological, neurochemical, and cognitive impairments, increasing the risk of developing schizophrenia. The inflammatory hypothesis of schizophrenia is also supported by clinical studies demonstrating systemic inflammation and microglia activation in schizophrenic patients...
2017: Frontiers in Immunology
https://www.readbyqxmd.com/read/28617431/nicotine-protects-rat-hypoglossal-motoneurons-from-excitotoxic-death-via-downregulation-of-connexin-36
#18
Silvia Corsini, Maria Tortora, Rossana Rauti, Andrea Nistri
Motoneuron disease including amyotrophic lateral sclerosis may be due, at an early stage, to deficit in the extracellular clearance of the excitatory transmitter glutamate. A model of glutamate-mediated excitotoxic cell death based on pharmacological inhibition of its uptake was used to investigate how activation of neuronal nicotinic receptors by nicotine may protect motoneurons. Hypoglossal motoneurons (HMs) in neonatal rat brainstem slices were exposed to the glutamate uptake blocker DL-threo-β-benzyloxyaspartate (TBOA) that evoked large Ca(2+) transients time locked among nearby HMs, whose number fell by about 30% 4 h later...
June 15, 2017: Cell Death & Disease
https://www.readbyqxmd.com/read/28616862/loops-d-e-and-g-in-the-drosophila-d%C3%AE-1-subunit-contribute-to-high-neonicotinoid-sensitivity-of-d%C3%AE-1-chicken-%C3%AE-2-nicotinic-acetylcholine-receptor
#19
Makoto Ihara, Mai Hikida, Hiroyuki Matsushita, Kyosuke Yamanaka, Yuya Kishimoto, Kazuki Kubo, Shun Watanabe, Mifumi Sakamoto, Koutaro Matsui, Akihiro Yamaguchi, Daiki Okuhara, Shogo Furutani, David B Sattelle, Kazuhiko Matsuda
BACKGROUND AND PURPOSE: Neonicotinoid insecticides interact with the orthosteric site formed at subunit interfaces of insect nicotinic acetylcholine receptors (insect nACh receptors). However, their interactions with the orthosteric sites at α-non α and α-α subunit interfaces remain poorly understood. The aim of this study was to elucidate the mechanism of neonicotinoid actions using the Drosophila Dα1-chicken β2 hybrid nACh receptor. EXPERIMENTAL APPROACH: Computer models of the (Dα1)3 (β2)2 nACh receptor in complex with imidacloprid and thiacloprid were generated...
June 14, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28615326/prenatal-nicotinic-exposure-prolongs-superior-laryngeal-c-fiber-mediated-apnea-and-bradycardia-through-enhancing-neuronal-trpv1-expression-and-excitation
#20
Xiuping Gao, Lei Zhao, Jianguo Zhuang, Na Zang, Fadi Xu
Maternal cigarette smoke, including prenatal nicotinic exposure (PNE), is responsible for sudden infant death syndrome (SIDS). The fatal events of SIDS are characterized by severe bradycardia and life-threatening apneas. Although activation of transient receptor potential vanilloid 1 (TRPV1) of superior laryngeal C-fibers (SLCFs) could induce bradycardia and apnea and has been implicated in SIDS pathogenesis, how PNE affects the SLCF-mediated cardiorespiratory responses remains unexplored. Here, we tested the hypothesis that PNE would aggravate the SLCF-mediated apnea and bradycardia via up-regulating TRPV1 expression and excitation of laryngeal C-neurons in the nodose/jugular (N/J) ganglia...
June 14, 2017: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
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