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https://www.readbyqxmd.com/read/28337332/bms-933043-a-selective-%C3%AE-7-nachr-partial-agonist-for-the-treatment-of-cognitive-deficits-associated-with-schizophrenia
#1
Dalton King, Christiana Iwuagwu, Jim Cook, Ivar M McDonald, Robert Mate, F Christopher Zusi, Matthew D Hill, Haiquan Fang, Rulin Zhao, Bei Wang, Amy E Easton, Regina Miller, Debra Post-Munson, Ronald J Knox, Lizbeth Gallagher, Ryan Westphal, Thaddeus Molski, Jingsong Fan, Wendy Clarke, Yulia Benitex, Kimberley A Lentz, Rex Denton, Daniel Morgan, Robert Zaczek, Nicholas J Lodge, Linda J Bristow, John E Macor, Richard E Olson
The therapeutic treatment of negative symptoms and cognitive dysfunction associated with schizophrenia is a significant unmet medical need. Preclinical literature indicates that α7 neuronal nicotinic acetylcholine (nACh) receptor agonists may provide an effective approach to treating cognitive dysfunction in schizophrenia. We report herein the discovery and evaluation of 1c (BMS-933043), a novel and potent α7 nACh receptor partial agonist with high selectivity against other nicotinic acetylcholine receptor subtypes (>100-fold) and the 5-HT3A receptor (>300-fold)...
March 9, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28332590/nicotine-enhances-alcohol-intake-and-dopaminergic-responses-through-%C3%AE-2-and-%C3%AE-4-nicotinic-acetylcholine-receptors
#2
Stefania Tolu, Fabio Marti, Carole Morel, Carole Perrier, Nicolas Torquet, Stephanie Pons, Renaud de Beaurepaire, Philippe Faure
Alcohol and nicotine are the most widely co-abused drugs. Both modify the activity of dopaminergic (DA) neurons of the Ventral Tegmental Area (VTA) and lead to an increase in DA release in the Nucleus Accumbens, thereby affecting the reward system. Evidences support the hypothesis that distinct nicotinic acetylcholine receptors (nAChRs), the molecular target of acetylcholine (ACh) and exogenous nicotine, are also in addition implicated in the response to alcohol. The precise molecular and neuronal substrates of this interaction are however not well understood...
March 23, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28326551/cyclic-imine-toxins-from-dinoflagellates-a-growing-family-of-potent-antagonists-of-the-nicotinic-acetylcholine-receptors
#3
REVIEW
Jordi Molgó, Pascale Marchot, Rómulo Aráoz, Evelyne Benoit, Bogdan I Iorga, Armen Zakarian, Palmer Taylor, Yves Bourne, Denis Servent
We present an overview of the toxicological profile of the fast-acting, lipophilic macrocyclic imine toxins, an emerging family of organic compounds associated with algal blooms, shellfish contamination and neurotoxicity. Worldwide, shellfish contamination incidents are expanding; therefore, the significance of these toxins for the shellfish food industry deserves further study. Emphasis is directed to the dinoflagellate species involved in their production, their chemical structures, and their specific mode of interaction with their principal natural molecular targets, the nicotinic acetylcholine receptors, or with the soluble acetylcholine-binding protein, used as a surrogate receptor model...
March 21, 2017: Journal of Neurochemistry
https://www.readbyqxmd.com/read/28321180/multiple-kinases-involved-in-the-nicotinic-modulation-of-gamma-oscillations-in-the-rat-hippocampal-ca3-area
#4
JianGang Wang, XiaoLong He, Fangli Guo, XiangLin Cheng, Yali Wang, XiaoFang Wang, ZhiWei Feng, Martin Vreugdenhil, ChengBiao Lu
Neuronal synchronization at gamma band frequency (20-80 Hz, γ oscillations) is closely associated with higher brain function, such as learning, memory and attention. Nicotinic acetylcholine receptors (nAChRs) are highly expressed in the hippocampus, and modulate hippocampal γ oscillations, but the intracellular mechanism underlying such modulation remains elusive. We explored multiple kinases by which nicotine can modulate γ oscillations induced by kainate in rat hippocampal area CA3 in vitro. We found that inhibitors of cyclic AMP dependent kinase (protein kinase A, PKA), protein kinase C (PKC), N-methyl-D-aspartate receptor (NMDA) receptors, Phosphoinositide 3-kinase (PI3K) and extracellular signal-related kinases (ERK), each individually could prevent the γ oscillation-enhancing effect of 1 μM nicotine, whereas none of them affected baseline γ oscillation strength...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/28319594/long-term-cardiovascular-autonomic-and-clinical-changes-after-immunoglobulin-g-immunoadsorption-therapy-in-autoimmune-autonomic-ganglionopathy
#5
Franca Barbic, Franca Dipaola, Francesca Andreetta, Enrico Brunetta, Laura Dalla Vecchia, Renato Mantegazza, Raffaello Furlan, Carlo Antozzi
A 63-year-old male was diagnosed with autoimmune autonomic ganglionopathy based on the finding of plasma antibodies to the nicotinic acetylcholine receptor (nAChR) of autonomic ganglia. He complained of mouth and eye dryness, dysphagia, severe constipation, erectile dysfunction, urgency, frequent urination, habitual orthostatic syncope and presyncope. A remarkable symptomatic orthostatic hypotension without changes in heart rate was present. We here describe the 3-year time course of the changes in spectral indices of cardiovascular autonomic control LF/HF and LFSAP, dysautonomia symptoms intensity and anti-nAChR antibodies following repetitive selective immunoadsorptions...
March 17, 2017: Journal of Hypertension
https://www.readbyqxmd.com/read/28315314/nicotine-promotes-cholangiocarcinoma-growth-in-xenograft-mice
#6
Allyson K Martínez, Kendal Jensen, Chad Hall, April O'Brien, Laurent Ehrlich, Tori White, Fanyin Meng, Tianhao Zhou, John Greene, Francesca Bernuzzi, Pietro Invernizzi, David E Dostal, Terry Lairmore, Gianfranco Alpini, Shannon Glaser
Nicotine, the main addictive substance in tobacco, is known to play a role in the development and/or progression of a number of malignant tumors. However, nicotine's involvement in the pathogenesis of cholangiocarcinoma is controversial. Therefore, we studied the effects of nicotine on the growth of cholangiocarcinoma cells in vitro and the progression of cholangiocarcinoma in a mouse xenograft model. The predominant subunit responsible for nicotine-mediated proliferation in normal and cancer cells, the α7 nicotinic acetylcholine receptor (α7-nAChR), was more highly expressed in human cholangiocarcinoma cell lines compared with normal human cholangiocytes...
March 14, 2017: American Journal of Pathology
https://www.readbyqxmd.com/read/28302458/the-effects-of-dexmedetomidine-pretreatment-on-the-pro-and-anti-inflammation-systems-after-spinal-cord-injury-in-rats
#7
Hui Rong, Zhibin Zhao, Jiying Feng, Yishan Lei, Hao Wu, Rao Sun, Zuoxia Zhang, Bailing Hou, Wei Zhang, YuE Sun, Xiaoping Gu, Zhengliang Ma, Yue Liu
Excessive inflammatory responses play important roles in the aggravation of secondary damage to an injured spinal cord. Dexmedetomidine (DEX), a selective α2-adrenoceptor agonist, has recently been implied to be neuroprotective in clinical anesthesia, but the underlying mechanism is elusive. As signaling through Toll-like receptor 4 (TLR4) and nicotinic receptors (nAChRs, notably α7nAChR) play important roles in the pro- and anti-inflammation systems in the central nervous system, respectively, this study investigated whether and how they were modulated by DEX pretreatment in a rat model of spinal cord compression...
March 14, 2017: Brain, Behavior, and Immunity
https://www.readbyqxmd.com/read/28302035/translational-multimodality-neuroimaging
#8
Sushil K Sharma
Recently high-resolution, noninvasive, multimodality in-vivo molecular imaging with PET, SPECT, CT and MRI, employing fusion algorithms has revolutionized personalized medicine. However, specific radiopharmaceuticals (RPs) for the accurate diagnosis and effective treatment of progressive neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, drug addiction, and other cognitive impairments still remain in developmental phase. Currently, multimodality fusion neuroimaging is utilized for the determination of: pharmacokinetics and pre-clinical development of radiopharmaceuticals (RPs); in-vivo monitoring of stem cell transplantation therapy; nicotinic acetylcholine receptors (nAChRs) investigations; and regional cerebral blood flow and glucose metabolism in cognitively-impaired subjects employing noninvasive microPET and nano-SPECT imaging...
March 15, 2017: Current Drug Targets
https://www.readbyqxmd.com/read/28298165/high-throughput-patch-clamp-screening-in-human-%C3%AE-6-containing-nicotinic-acetylcholine-receptors
#9
Lucas C Armstrong, Glenn E Kirsch, Nikolai B Fedorov, Caiyun Wu, Yuri A Kuryshev, Abby L Sewell, Zhiqi Liu, Arianne L Motter, Carmine S Leggett, Michael S Orr
Nicotine, the addictive component of tobacco products, is an agonist at nicotinic acetylcholine receptors (nAChRs) in the brain. The subtypes of nAChR are defined by their α- and β-subunit composition. The α6β2β3 nAChR subtype is expressed in terminals of dopaminergic neurons that project to the nucleus accumbens and striatum and modulate dopamine release in brain regions involved in nicotine addiction. Although subtype-dependent selectivity of nicotine is well documented, subtype-selective profiles of other tobacco product constituents are largely unknown and could be essential for understanding the addiction-related neurological effects of tobacco products...
March 1, 2017: SLAS Discov
https://www.readbyqxmd.com/read/28294298/proteins-and-chemical-chaperones-involved-in-neuronal-nicotinic-receptor-expression-and-function-an-update
#10
REVIEW
Arianna Crespi, Sara Francesca Colombo, Cecilia Gotti
Neuronal nicotinic acetylcholine receptors (nAChRs) are a family of acetylcholine-(ACh) gated cation channels and their homeostasis or proteostasis is essential for the correct physiology of the central and peripheral nervous systems. The proteostasis network regulates the folding, assembly, degradation and trafficking of nAChRs in order to ensure their efficient functional cell surface expression. However, as nAChRs are multisubunit, multispan, integral membrane proteins, the folding and assembly is a very inefficient process, and only a small portion of subunits can form functional pentamers...
March 13, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28293176/muscarinic-receptors-are-responsible-for-the-cholinergic-modulation-of-projection-neurons-in-the-song-production-brain-nucleus-ra-of-zebra-finches
#11
Wei Meng, Songhua Wang, Lihua Yao, Nan Zhang, Dongfeng Li
Songbirds are a useful model for the study of learned vocal behavior in vertebrates. The robust nucleus of the arcopallium (RA) is a premotor nucleus in the vocal motor pathway. It receives excitatory synaptic inputs from the anterior forebrain pathway. RA also receives cholinergic inputs from the ventral paleostriatum of the basal forebrain. Our previous study showed that carbachol, a non-selective cholinergic receptor agonist, modulates the electrophysiology of RA projection neurons (PNs), indicating that cholinergic modulation of RA may play an important role in song production...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/28283678/deficiency-of-%C3%AE-7-nicotinic-acetylcholine-receptor-attenuates-bleomycin-induced-lung-fibrosis-in-mice
#12
Peiyu Sun, Ling Li, Caiqi Zhao, Mengyao Pan, Zhikang Qian, Xiao Su
α7 nicotinic acetylcholine receptor (α7 nAChR, coded by Chrna7) is indispensible in dampening proinflammatory responses. However, whether α7 nAChR would play a role in regulating bleomycin (BLM)-induced lung fibrosis is less investigated. Here, we intratracheally challenged wildtype and Chrna7(-/-) mice with BLM to elicit lung fibrosis. Taken advantage of this model, we measured body weight loss, lung fibrogenic genes (Acta2, Col1a1, Fsp1, and Fstl1), histology, Masson's trichrome staining, hydroxyproline levels, and expression of α-SMA at protein levels in the BLM-challenged lung for evaluating severity of lung fibrosis...
March 6, 2017: Molecular Medicine
https://www.readbyqxmd.com/read/28279662/in%C3%A2-vivo-interactions-between-%C3%AE-7-nicotinic-acetylcholine-receptor-and-nuclear-peroxisome-proliferator-activated-receptor-%C3%AE-implication-for-nicotine-dependence
#13
Asti Jackson, Deniz Bagdas, Pretal P Muldoon, Aron H Lichtman, F Ivy Carroll, Mark Greenwald, Michael F Miles, M Imad Damaj
Chronic tobacco use dramatically increases health burdens and financial costs. Limitations of current smoking cessation therapies indicate the need for improved molecular targets. The main addictive component of tobacco, nicotine, exerts its dependency effects via nicotinic acetylcholine receptors (nAChRs). Activation of the homomeric α7 nAChR reduces nicotine's rewarding properties in conditioned place preference (CPP) test and i.v. self-administration models, but the mechanism underlying these effects is unknown...
March 7, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28273388/enhanced-transport-of-plant-produced-rabies-single-chain-antibody-rvg-peptide-fusion-protein-across-an-in-cellulo-blood-brain-barrier-device
#14
Waranyoo Phoolcharoen, Christophe Prehaud, Craig J van Dolleweerd, Leonard Both, Anaelle da Costa, Monique Lafon, Julian K-C Ma
The biomedical applications of antibody engineering are developing rapidly and have been expanded to plant expression platforms. In the present study, we have generated a novel antibody molecule in planta for targeted delivery across the blood-brain barrier (BBB). Rabies virus (RABV) is a neurotropic virus for which there is no effective treatment after entry into the central nervous system (CNS). This study investigated the use of a RABV glycoprotein peptide sequence to assist delivery of a rabies neutralising single-chain antibody (ScFv) across an in cellulo model of human BBB...
March 8, 2017: Plant Biotechnology Journal
https://www.readbyqxmd.com/read/28268112/taking-varenicline-for-smoking-cessation-a-rare-cause-of-pulmonary-thromboembolism-with-infarction
#15
Sun Hwa Lee, Seong Jong Yun, Seokyong Ryu, Seung Won Choi, Hye Jin Kim, Tae Kyug Kang, Sung Chan Oh, Suk Jin Cho
Varenicline (Champix®, Chantix®) is a partial agonist of the α4β2 nicotinic acetylcholine receptor (nAChR) and a full agonist of the α7 nAChR. It has been used for smoking cessation since 2006. Varenicline has been associated with adverse cardiovascular (CV) events, including myocardial infarction, which may be caused by activation of the α7 nAChR receptor that in turn stimulates parasympathetic output from the brainstem to the heart, release of catecholamines, and has a prothrombotic effect. However, among the adverse CV events, the issue related to the varenicline-induced pulmonary thromboembolism (PTE) has not being addressed...
February 28, 2017: American Journal of Emergency Medicine
https://www.readbyqxmd.com/read/28264149/hippocampal-%C3%AE-7-nicotinic-acetylcholine-receptors-contribute-to-modulation-of-depression-like-behavior-in-c57bl-6%C3%A2-j-mice
#16
Yann S Mineur, Tenna N Mose, Sam Blakeman, Marina R Picciotto
BACKGROUND AND PURPOSE: Clinical studies have identified links between cholinergic signaling and depression in human subjects. Increased cholinergic signaling in hippocampus also increases behaviors related to anxiety and depression in mice, which can be reversed by acetylcholine receptor antagonists. EXPERIMENTAL APPROACH: Since the α7 subunit of the nicotinic acetylcholine receptor (nAChR) is highly expressed in hippocampus, we determined whether blocking α7 nAChRs could reverse effects of increased ACh signaling in anxiety- and depression-related behaviors in mice...
March 6, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28259598/tropisetron-sensitizes-%C3%AE-7-containing-nicotinic-receptors-to-low-levels-of-acetylcholine-in%C3%A2-vitro-and-improves-memory-related-task-performance-in-young-and-aged-animals
#17
Patrick M Callahan, Daniel Bertrand, Sonia Bertrand, Marc R Plagenhoef, Alvin V Terry
Tropisetron, a 5-HT3 receptor antagonist commonly prescribed for chemotherapy-induced nausea and vomiting also exhibits high affinity, partial agonist activity at α7 nicotinic acetylcholine receptors (α7 nAChRs). α7 nAChRs are considered viable therapeutic targets for neuropsychiatric disorders such as Alzheimer's disease (AD). Here we further explored the nAChR pharmacology of tropisetron to include the homomeric α7 nAChR and recently characterized heteromeric α7β2 nAChR (1:10 ratio) and we evaluated its cognitive effects in young and aged animals...
March 1, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28243714/nicotine-withdrawal-induced-inattention-is-absent-in-alpha7-nachr-knockout-mice
#18
K K Higa, A Grim, M E Kamenski, J van Enkhuizen, X Zhou, K Li, J C Naviaux, L Wang, R K Naviaux, M A Geyer, A Markou, J W Young
RATIONALE: Smoking is the leading cause of preventable death in the USA, but quit attempts result in withdrawal-induced cognitive dysfunction and predicts relapse. Greater understanding of the neural mechanism(s) underlying these cognitive deficits is required to develop targeted treatments to aid quit attempts. OBJECTIVES: We examined nicotine withdrawal-induced inattention in mice lacking the α7 nicotinic acetylcholine receptor (nAChR) using the five-choice continuous performance test (5C-CPT)...
February 28, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28241318/the-nicotinic-cholinergic-pathway-contributes-to-retinal-neovascularization-in-a-mouse-model-of-retinopathy-of-prematurity
#19
Sean F Hackett, Christopher Seidel, Sheena Abraham, Rishi Chadha, Seth D Fortmann, Peter A Campochiaro, John P Cooke
Purpose: To investigate the role of nicotinic acetylcholine receptors (nAChRs) in retinal vascular development and ischemia-induced retinal neovascularization (NV). Methods: The expression of nAChR subtypes and VEGF signaling pathway components was assessed in mice with and without oxygen-induced ischemic retinopathy by comparing expression levels at postnatal day (P) 14 and P17 in mice exposed to 75% oxygen from P7 to P12 and returned to room air versus mice pups that were exposed to ambient oxygen levels during the same period...
February 1, 2017: Investigative Ophthalmology & Visual Science
https://www.readbyqxmd.com/read/28240351/a-time-to-listen-perinatal-smoking-affects-the-development-of-temporal-sound-processing
#20
Barbara J Morley, Richard A Felix
It has been known for more than 30 years that the α7 nicotinic acetylcholine receptor (nAChR) is widely expressed in the mammalian brain and is very heavily expressed in the auditory brainstem, where it is developmentally regulated. Peak expression usually occurs at about postnatal day 10 (P10) in rodents, coincident with the maturation of glutamatergic excitatory synapses. The importance of the developmental regulation and the association with excitatory synapses, however, has remained elusive. This article is protected by copyright...
February 27, 2017: Journal of Physiology
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