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https://www.readbyqxmd.com/read/29328482/cytisine-induces-endoplasmic-reticulum-stress-caused-by-calcium-overload-in-hepg2-cells
#1
Lei Yu, Bo Jiang, Zhifeng Chen, Xin Wang, Dongxue Shang, Xiaopo Zhang, Yongxue Sun, Jinghui Yang, Yubin Ji
Cytisine, a quinolizidine alkaloid, is one of the major bioactive components found in the small tree Sophora Alopecuraides L., and is a traditional Chinese medicine that is used for treating hepatitis and liver cancer. In the 1960s, quinolizidine alkaloids were reported to exhibit inhibitory effects on tumour cell proliferation in several types of cancer cells. However, few studies have investigated the effect of cytisine on liver cancer. Our team confirmed that cytisine induced apoptosis in HepG2 cells via a mitochondrial pathway...
January 8, 2018: Oncology Reports
https://www.readbyqxmd.com/read/29326174/muscle-nicotinic-acetylcholine-receptors-may-mediate-trans-synaptic-signaling-at-the-mouse-neuromuscular-junction
#2
Xueyong Wang, J Michael McIntosh, Mark M Rich
Block of neurotransmitter receptors at the neuromuscular junction (NMJ) has been shown to trigger upregulation of the number of synaptic vesicles released (quantal content, QC), a response termed homeostatic synaptic plasticity. The mechanism underlying this plasticity is not known. Here, we used selective toxins to demonstrate that block of α1-containing nicotinic acetylcholine receptors (nAChRs) at the neuromuscular junction of male and female mice, triggers the upregulation of QC. Reduction of current flow through nAChRs, induced by drugs with antagonist activity, demonstrated that reduction in synaptic current per se does not trigger upregulation of QC...
January 11, 2018: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/29324040/neonicotinoids-and-other-insect-nicotinic-receptor-competitive-modulators-progress-and-prospects
#3
John E Casida
Neonicotinoids (neonics) are remarkably effective as plant systemics to control sucking insects and for flea control on dogs and cats. The nitroimines imidacloprid, clothianidin, thiamethoxam, and dinotefuran are the leaders among the seven commercial neonics that also include the nitromethylene nitenpyram, the nitromethylene-derived cycloxaprid, and the cyanoimines acetamiprid and thiacloprid. Honey bees are highly sensitive to the nitroimines and nitromethylenes, but the cyanoimines are less toxic. All neonics are nicotinic acetylcholine receptor (nAChR) agonists with a common mode of action, target-site cross-resistance, and much higher potency on insect than mammalian nAChRs at defined binding sites...
January 7, 2018: Annual Review of Entomology
https://www.readbyqxmd.com/read/29321522/accelerated-proteomic-visualization-of-individual-predatory-venoms-of-conus-purpurascens-reveals-separately-evolved-predation-evoked-venom-cabals
#4
S W A Himaya, Frank Marí, Richard J Lewis
Cone snail venoms have separately evolved for predation and defense. Despite remarkable inter- and intra-species variability, defined sets of synergistic venom peptides (cabals) are considered essential for prey capture by cone snails. To better understand the role of predatory cabals in cone snails, we used a high-throughput proteomic data mining and visualisation approach. Using this approach, the relationship between the predatory venom peptides from nine C. purpurascens was systematically analysed. Surprisingly, potentially synergistic levels of κ-PVIIA and δ-PVIA were only identified in five of nine specimens...
January 10, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29316656/azemiopsin-a-selective-peptide-antagonist-of-muscle-nicotinic-acetylcholine-receptor-preclinical-evaluation-as-a-local-muscle-relaxant
#5
Irina V Shelukhina, Maxim N Zhmak, Alexander V Lobanov, Igor A Ivanov, Alexandra I Garifulina, Irina N Kravchenko, Ekaterina A Rasskazova, Margarita A Salmova, Elena A Tukhovskaya, Vladimir A Rykov, Gulsara A Slashcheva, Natalya S Egorova, Inessa S Muzyka, Victor I Tsetlin, Yuri N Utkin
Azemiopsin (Az), a linear peptide from the Azemiops feae viper venom, contains no disulfide bonds, is a high-affinity and selective inhibitor of nicotinic acetylcholine receptor (nAChR) of muscle type and may be considered as potentially applicable nondepolarizing muscle relaxant. In this study, we investigated its preclinical profile in regard to in vitro and in vivo efficacy, acute and chronic toxicity, pharmacokinetics, allergenic capacity, immunotoxicity and mutagenic potency. The peptide effectively inhibited (IC50 ~ 19 nM) calcium response of muscle nAChR evoked by 30 μM (EC100) acetylcholine but was less potent (IC50 ~ 3 μM) at α7 nAChR activated by 10 μM (EC50) acetylcholine and had a low affinity to α4β2 and α3-containing nAChR, as well as to GABAA or 5HT₃ receptors...
January 7, 2018: Toxins
https://www.readbyqxmd.com/read/29316361/effects-of-serum-enzyme-thiol-and-forced-degradation-on-the-stabilities-of-%C3%AE-o-conotoxin-gexiva-1-2-and-gexiva-1-4
#6
Shurun Yu, Yong Wu, Pan Xu, Shuai Wang, Dongting Zhangsun, Sulan Luo
αO-conotoxin GeXIVA, which is a potent antagonist of α9α10 nicotinic acetylcholine receptor (nAChR), is of great interest as a potential analgesic for chronic neuropathic pain. It has three isomers, of which both GeXIVA[1,2] and GeXIVA[1,4] showed similar low nanomolar IC50 s in potent blocking rat α9α10 nAChRs. Here, we first reported stabilities of GeXIVA[1,2] and GeXIVA[1,4] in various biochemical circumstances, including human serum, enzymatic degradation and thiol, which would be the key factors to affect stabilities of the two isomers in vivo...
January 9, 2018: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/29306322/curcumin-attenuates-collagen-induced-inflammatory-response-through-the-gut-brain-axis
#7
Yannong Dou, Jinque Luo, Xin Wu, Zhifeng Wei, Bei Tong, Juntao Yu, Ting Wang, Xinyu Zhang, Yan Yang, Xusheng Yuan, Peng Zhao, Yufeng Xia, Huijuan Hu, Yue Dai
BACKGROUND: Previous studies have demonstrated that oral administration of curcumin exhibited an anti-arthritic effect despite its poor bioavailability. The present study aimed to explore whether the gut-brain axis is involved in the therapeutic effect of curcumin. METHODS: The collagen-induced arthritis (CIA) rat model was induced by immunization with an emulsion of collagen II and complete Freund's adjuvant. Sympathetic and parasympathetic tones were measured by electrocardiographic recordings...
January 6, 2018: Journal of Neuroinflammation
https://www.readbyqxmd.com/read/29305920/nicotinic-acetylcholine-receptor-nachr-mediated-dopamine-release-in-larval-drosophila-melanogaster
#8
Poojan Pyakurel, Mimi Shin, B Jill Venton
Acetylcholine is an excitatory neurotransmitter in the central nervous system of insects and the nicotinic acetylcholine receptor (nAChR) is a target for neonicotinoid insecticides. Functional insect nAChRs are difficult to express in host cells, and hence difficult to study. In mammals, acetylcholine and nicotine evoke dopamine release, but the extent to which this mechanism is conserved in insects is unknown. In intact larval ventral nerve cords (VNCs), we studied dopamine evoked by acetylcholine, nicotine, or neonicotinoids...
January 3, 2018: Neurochemistry International
https://www.readbyqxmd.com/read/29305655/chrfam7a-gene-expression-in-schizophrenia-clinical-correlates-and-the-effect-of-antipsychotic-treatment
#9
Sunil V Kalmady, Rimjhim Agrawal, Deepthi Venugopal, Venkataram Shivakumar, Anekal C Amaresha, Sri Mahavir Agarwal, Manjula Subbanna, Ashwini Rajasekaran, Janardhanan C Narayanaswamy, Monojit Debnath, Ganesan Venkatasubramanian
Earlier studies have implicated CHRNA7, coding α-7 nicotinic acetylcholine receptor (α7 nAChR), and its partially duplicated chimeric gene CHRFAM7A in schizophrenia. However, the relationship between the alterations in peripheral gene expression of CHRFAM7A and severity of clinical symptoms has not been examined. Furthermore, potential influence of the antipsychotic medication on CHRFAM7A expression in drug-naive or drug-free schizophrenia is an unexplored area. CHRFAM7A gene expression in lymphocytes was analyzed in 90 antipsychotic-naïve or free schizophrenia patients using TaqMan-based quantitative RT-PCR...
January 5, 2018: Journal of Neural Transmission
https://www.readbyqxmd.com/read/29302769/imidacloprid-impedes-mitochondrial-function-and-induces-oxidative-stress-in-cotton-bollworm-helicoverpa-armigera-larvae-hubner-noctuidae
#10
Bharat Nareshkumar, Shaik Mohammad Akbar, Hari Chand Sharma, Senigala K Jayalakshmi, Kuruba Sreeramulu
Neonicotinoids have high agonistic affinity to insect nicotinic acetylcholine receptors (nAChR) and are frequently used as insecticides against most devastating lepidopteran insect pests. Imidacloprid influenced dose-dependent decline in the state III and IV respiration, respiration control index (RCI), and P/O ratios, in vitro and in vivo. The bioassay indicated its LD50 value to be 531.24 μM. The insecticide exhibited a dose-dependent inhibition on F0F1-ATPase and complex IV activity. At 600 μM, the insecticide inhibited 83...
January 5, 2018: Journal of Bioenergetics and Biomembranes
https://www.readbyqxmd.com/read/29299690/%C3%AE-5-nachr-modulation-of-the-prefrontal-cortex-makes-attention-resilient
#11
William M Howe, Julie L Brooks, Patrick L Tierney, Jincheng Pang, Amie Rossi, Damon Young, Keith Dlugolenski, Ed Guillmette, Marc Roy, Katherine Hales, Rouba Kozak
A loss-of-function polymorphism in the α5 nicotinic acetylcholine receptor (nAChR) subunit gene has been linked to both drug abuse and schizophrenia. The α5 nAChR subunit is strategically positioned in the prefrontal cortex (PFC), where a loss-of-function in this subunit may contribute to cognitive disruptions in both disorders. However, the specific contribution of α5 to PFC-dependent cognitive functions has yet to be illustrated. In the present studies, we used RNA interference to knockdown the α5 nAChR subunit in the PFC of adult rats...
January 3, 2018: Brain Structure & Function
https://www.readbyqxmd.com/read/29298898/a-triad-of-residues-is-functionally-transferrable-between-5-ht3-serotonin-receptors-and-nicotinic-acetylcholine-receptors
#12
Richard Mosesso, Dennis A Dougherty
Cys-loop receptors are pentameric ligand-gated ion channels that facilitate communication within the nervous system. Upon neurotransmitter binding, these receptors undergo an allosteric activation mechanism connecting the binding event to the membrane-spanning channel pore, which expands to conduct ions. Some of the earliest steps in this activation mechanism are carried out by residues proximal to the binding site, the relative positioning of which may reflect functional differences among members of the Cys-loop family of receptors...
January 3, 2018: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/29277577/coronaridine-congeners-modulate-mitochondrial-%C3%AE-3%C3%AE-4-nicotinic-acetylcholine-receptors-with-different-potency-and-through-distinct-intra-mitochondrial-pathways
#13
Hugo R Arias, Olena Lykhmus, Kateryna Uspenska, Maryna Skok
In contrast to plasma membrane-expressed nicotinic acetylcholine receptors (nAChRs), mitochondrial nAChRs function in an ion-independent manner by triggering intra-mitochondrial kinases that regulate the release of cytochrome c (Cyt c), an important step in cellular apoptosis. The aim of this study is to determine the structural requirements for mitochondrial α3β4* nAChR activation by measuring the modulatory effects of two noncompetitive antagonists of these receptors, (+)-catharanthine and (±)-18-methoxycoronaridine [(±)-18-MC], on Cyt c release from wild-type and α7-/- mice mitochondria...
December 22, 2017: Neurochemistry International
https://www.readbyqxmd.com/read/29277457/development-of-fluorescence-imaging-probes-for-nicotinic-acetylcholine-%C3%AE-4%C3%AE-2%C3%A2-receptors
#14
Gurleen K Samra, Irakli Intskirveli, Anitha P Govind, Christopher Liang, Ronit Lazar, William N Green, Raju Metherate, Jogeshwar Mukherjee
Nicotinic acetylcholine α4β2∗ receptors (nAChRs) are implicated in various neurodegenerative diseases and smoking addiction. Imaging of brain high-affinity α4β2∗ nAChRs at the cellular and subcellular levels would greatly enhance our understanding of their functional role. Since better resolution could be achieved with fluorescent probes, using our previously developed positron emission tomography (PET) imaging agent [18F]nifrolidine, we report here design, synthesis and evaluation of two fluorescent probes, nifrodansyl and nifrofam for imaging α4β2∗ nAChRs...
December 17, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29276477/cholinergic-modulation-of-cortical-microcircuits-is-layer-specific-evidence-from-rodent-monkey-and-human-brain
#15
REVIEW
Joshua Obermayer, Matthijs B Verhoog, Antonio Luchicchi, Huibert D Mansvelder
Acetylcholine (ACh) signaling shapes neuronal circuit development and underlies specific aspects of cognitive functions and behaviors, including attention, learning, memory and motivation. During behavior, activation of muscarinic and nicotinic acetylcholine receptors (mAChRs and nAChRs) by ACh alters the activation state of neurons, and neuronal circuits most likely process information differently with elevated levels of ACh. In several brain regions, ACh has been shown to alter synaptic strength as well. By changing the rules for synaptic plasticity, ACh can have prolonged effects on and rearrange connectivity between neurons that outlasts its presence...
2017: Frontiers in Neural Circuits
https://www.readbyqxmd.com/read/29273965/effects-of-%C3%AE-7-nicotinic-receptor-activation-on-cell-survival-in-rat-organotypic-hippocampal-slice-cultures
#16
Denise F Happ, R Andrew Tasker
Glutamatergic signaling via N-methyl-D-aspartate receptors (NMDARs) is important for physiological functioning, but can also induce cell death via excitotoxic mechanisms in many neuropathological diseases, such as stroke. Altering the cellular response to excitotoxic insults by modulating the downstream effects of NMDAR activation represents a promising therapeutic approach. For example, α7 nicotinic acetylcholine receptors (α7 nAChRs) signaling has been shown to be able to change NMDA-induced neurotoxicity in some models...
December 22, 2017: Neurotoxicity Research
https://www.readbyqxmd.com/read/29261717/probing-the-putative-%C3%AE-7-nachr-nmdar-complex-in-human-and-murine-cortex-and-hippocampus-different-degrees-of-complex-formation-in-healthy-and-alzheimer-brain-tissue
#17
Mohamed R Elnagar, Anne Byriel Walls, Gouda K Helal, Farid M Hamada, Morten Skøtt Thomsen, Anders A Jensen
α7 nicotinic acetylcholine receptors (nAChRs) and N-methyl-D-aspartate receptors (NMDARs) are key mediators of central cholinergic and glutamatergic neurotransmission, respectively. In addition to numerous well-established functional interactions between α7 nAChRs and NMDARs, the two receptors have been proposed to form a multimeric complex, and in the present study we have investigated this putative α7 nAChR/NMDAR assembly in human and murine brain tissues. By α-bungarotoxin (BGT) affinity purification, α7 and NMDAR subunits were co-purified from human and murine cortical and hippocampal homogenates, substantiating the notion that the receptors are parts of a multimeric complex in the human and rodent brain...
2017: PloS One
https://www.readbyqxmd.com/read/29261656/nicotinic-alpha-7-receptor-agonists-evp-6124-and-bms-933043-attenuate-scopolamine-induced-deficits-in-visuo-spatial-paired-associates-learning
#18
Michael R Weed, Joseph Polino, Laura Signor, Mark Bookbinder, Deborah Keavy, Yulia Benitex, Daniel G Morgan, Dalton King, John E Macor, Robert Zaczek, Richard Olson, Linda J Bristow
Agonists at the nicotinic acetylcholine alpha 7 receptor (nAChR α7) subtype have the potential to treat cognitive deficits in patients with Alzheimer's disease (AD) or schizophrenia. Visuo-spatial paired associates learning (vsPAL) is a task that has been shown to reliably predict conversion from mild cognitive impairment to AD in humans and can also be performed by nonhuman primates. Reversal of scopolamine-induced impairment of vsPAL performance may represent a translational approach for the development of nAChR α7 agonists...
2017: PloS One
https://www.readbyqxmd.com/read/29248596/the-wonderland-of-neuronal-nicotinic-acetylcholine-receptors
#19
REVIEW
Daniel Bertrand, A V Terry
Nearly 30 years of experimental evidence supports the argument that ligands of nicotinic acetylcholine receptors (nAChRs) have potential as therapeutic agents. However, as in the famous Lewis Carroll novel "Alice in Wonderland", there have been many unexpected adventures along the pathway of development, and few nAChR ligands have been approved for any clinical condition to date with the exception of nicotine dependence. The recent failures of nAChR ligands in AD and schizophrenia clinical trials have reduced enthusiasm for this therapeutic strategy and many pharmaceutical companies have now abandoned this field of research...
December 14, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/29248576/counteracting-desensitization-of-human-%C3%AE-7-nicotinic-acetylcholine-receptors-with-bispyridinium-compounds-as-an-approach-against-organophosphorus-poisoning
#20
Corinna Scheffel, Karin V Niessen, Sebastian Rappenglück, Klaus T Wanner, Horst Thiermann, Franz Worek, Thomas Seeger
Irreversible inhibition of acetylcholinesterase (AChE) resulting in accumulation of acetylcholine and overstimulation of muscarinic and nicotinic receptors accounts for the acute toxicity of organophosphorus compounds (OP). Accordingly, the mainstay pharmacotherapy against poisoning by OP comprises the competitive muscarinic acetylcholine receptor antagonist atropine to treat muscarinic effects and, in addition, oximes to reactivate inhibited AChE. A therapeutic gap still remains in the treatment of desensitized nicotinic acetylcholine receptors following OP exposure...
December 14, 2017: Toxicology Letters
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