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Cholinergic receptor

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https://www.readbyqxmd.com/read/29150865/enhanced-mu-opioid-receptor-dependent-opioidergic-modulation-of-striatal-cholinergic-transmission-in-dyt1-dystonia
#1
Giulia Ponterio, Annalisa Tassone, Giuseppe Sciamanna, Valentina Vanni, Maria Meringolo, Massimo Santoro, Nicola Biagio Mercuri, Paola Bonsi, Antonio Pisani
BACKGROUND: Mu opioid receptor activation modulates acetylcholine release in the dorsal striatum, an area deeply involved in motor function, habit formation, and reinforcement learning as well as in the pathophysiology of different movement disorders, such as dystonia. Although the role of opioids in drug reward and addiction is well established, their involvement in motor dysfunction remains largely unexplored. METHODS: We used a multidisciplinary approach to investigate the responses to mu activation in 2 mouse models of DYT1 dystonia (Tor1a(+/Δgag) mice, Tor1a(+/-) torsinA null mice, and their respective wild-types)...
November 18, 2017: Movement Disorders: Official Journal of the Movement Disorder Society
https://www.readbyqxmd.com/read/29137938/discovery-of-imidazo-1-2-a-pyridine-based-anthelmintic-targeting-cholinergic-receptors-of-haemonchus-contortus
#2
Jean-Paul Déto Ursul N'Guessan, Pierre-Olivier Delaye, Mélanie Pénichon, Claude L Charvet, Cédric Neveu, Mahama Ouattara, Cécile Enguehard-Gueiffier, Alain Gueiffier, Hassan Allouchi
We report the synthesis of a series of imidazo[1,2-a]pyridine-based molecules as anthelmintic against the livestock parasite Haemonchus contortus. The molecules were tested by using Larval Paralysis Test (LPT), in order to target ionic channels, as most of the prominent marketed anthelminthics present such mechanism of action. The most active compound (5e) displayed paralysis on H. contortus stage 3 larvae until 31.25 µM. Effect of 5e on H. contortus cholinergic receptors (L-AChR1 and 2) was characterized via electrophysiological measurement and a rare antagonist mode of action was unveiled...
November 6, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29129819/nicotinic-acetylcholine-receptor-%C3%AE-7-subunit-improves-energy-homeostasis-and-inhibits-inflammation-in-nonalcoholic-fatty-liver-disease
#3
Dong-Jie Li, Jian Liu, Xia Hua, Hui Fu, Fang Huang, Yi-Bo Fei, Wen-Jie Lu, Fu-Ming Shen, Pei Wang
OBJECTIVE: Nonalcoholic fatty liver disease (NAFLD) is one of the most common liver diseases worldwide; yet, the pathogenesis of the disorder is not completely understood. The nicotinic acetylcholine receptor α7 subunit (α7nAChR) plays an indispensable role in the vagus nerve-regulated cholinergic anti-inflammatory pathway. METHODS: In the present study, we investigated the key role of α7nAChR in NAFLD development. Male wild-type (WT) and α7nAChR knockout (α7nAChR(-/-)) mice were fed a normal chow or a high-fat diet (HFD) for 16 weeks to induce NAFLD...
November 9, 2017: Metabolism: Clinical and Experimental
https://www.readbyqxmd.com/read/29128415/the-p38-mitogen-activated-protein-kinase-regulates-%C3%AE-amyloid-protein-internalization-through-the-%C3%AE-7-nicotinic-acetylcholine-receptor-in-mouse-brain
#4
Kai-Ge Ma, Jia Lv, Wei-Na Yang, Ke-Wei Chang, Xiao-Dan Hu, Li-Li Shi, Wan-Ying Zhai, Hang-Fan Zong, Yi-Hua Qian
Alzheimer's disease (AD) is one of the most devastating neurodegenerative disorders. Intracellular β-amyloid protein (Aβ) is an early event in AD. It induces the formation of amyloid plaques and neuron damage. The α7 nicotinic acetylcholine receptor (α7nAChR) has been suggested to play an important role in Aβ caused cognition. It has high affinity with Aβ and could mediate Aβ internalization in vitro. However, whether in mouse brain the p38 MAPK signaling pathway is involved in the regulation of the α7nAChR mediated Aβ internalization and their role in mitochondria remains little known...
November 9, 2017: Brain Research Bulletin
https://www.readbyqxmd.com/read/29127449/determining-a-threshold-sub-acute-dose-leading-to-minimal-physiological-alterations-following-prolonged-exposure-to-the-nerve-agent-vx-in-rats
#5
E Bloch-Shilderman, I Rabinovitz, I Egoz, G Yacov, N Allon, U Nili
VX, a potent inhibitor of cholinesterase (ChE), is considered as one of the most toxic, persistent and least volatile nerve agents. VX is absorbed in various environmental surfaces and is gradually released long after its initial dispersal. Its toxicity is mainly caused by disrupting central and peripheral cholinergic nervous system activity, leading to potential long-term detrimental effects on health. The primary objective of the present study was to assess the threshold VX dose leading to minimal physiological alterations following prolonged VX exposure...
November 10, 2017: Archives of Toxicology
https://www.readbyqxmd.com/read/29127015/oxotremorine-m-potentiates-nmda-receptors-by-muscarinic-receptor-dependent-and-independent-mechanisms
#6
Ruud Zwart, Hannah Reed, Emanuele Sher
Muscarinic acetylcholine M1 receptors play an important role in synaptic plasticity in the hippocampus and cortex. Potentiation of NMDA receptors as a consequence of muscarinic acetylcholine M1 receptor activation is a crucial event mediating the cholinergic modulation of synaptic plasticity, which is a cellular mechanism for learning and memory. In Alzheimer's disease, the cholinergic input to the hippocampus and cortex is severely degenerated, and agonists or positive allosteric modulators of M1 receptors are therefore thought to be of potential use to treat the deficits in cognitive functions in Alzheimer's disease...
November 7, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29122691/sexually-diergic-hypothalamic-pituitary-adrenal-axis-responses-to-selective-and-non-selective-muscarinic-antagonists-prior-to-cholinergic-stimulation-by-physostigmine-in-rats
#7
Marissa A Smail, Jessica L Soles, Tracy E Karwoski, Robert T Rubin, Michael E Rhodes
Central cholinergic systems regulate the hypothalamic-pituitary-adrenal (HPA) axis differentially in males and females (sexual diergism). We previously investigated the role of muscarinic receptors in this regulation by administering physostigmine (PHYSO), an acetylcholinesterase inhibitor, to male and female rats pretreated with scopolamine (SCOP), a nonselective muscarinic antagonist. SCOP pretreatment enhanced adrenocorticotropic hormone (ACTH) and corticosterone (CORT) responses in both sexes; males had greater ACTH responses while females had greater CORT responses...
November 7, 2017: Brain Research Bulletin
https://www.readbyqxmd.com/read/29120510/in-vitro-characterization-of-gamma-oscillations-in-the-hippocampal-formation-of-the-domestic-chick
#8
Pradeep Dheerendra, Nicholas M Lynch, Joseph Crutwell, Mark O Cunningham, Tom V Smulders
Avian and mammalian brains have evolved independently from each other for about 300 million years. During that time, the hippocampal formation (HF) has diverged in morphology and cyto-architecture, but seems to have conserved much of its function. It is therefore an open question how seemingly different neural organizations can generate the same function. A prominent feature of the mammalian hippocampus is that it generates different neural oscillations, including the gamma rhythm, which plays an important role in memory processing...
November 9, 2017: European Journal of Neuroscience
https://www.readbyqxmd.com/read/29117064/electroacupuncture-pretreatment-attenuates-acute-lung-injury-through-%C3%AE-7-nicotinic-acetylcholine-receptor-mediated-inhibition-of-hmgb1-release-in-rats-after-cardiopulmonary-bypass
#9
Zhankui Wang, Lei Hou, Hao Yang, Jiaxi Ge, Shaocheng Wang, Weitian Tian, Xiangrui Wang, Zhongwei Yang
Acute lung injury is a common complication after cardiopulmonary bypass (CPB). α7 nicotinic acetylcholine receptors (α7nAChR) and α7nAChR-dependent cholinergic signaling are implicated in suppressing the release of high mobility group box 1 (HMGB1) and reducing the inflammatory response. A previous study has shown the electroacupuncture (EA) pretreatment induces tolerance against lung injury. However, the role of EA in CPB is poorly understood. This study employed EA and a rat model of CPB to determine whether EA was associated with CPB-induced lung injury...
November 7, 2017: Shock
https://www.readbyqxmd.com/read/29114569/cholinergic-receptor-alterations-in-the-cerebral-cortex-of-spinal-cord-injured-rat
#10
R Chinthu, T R Anju, C S Paulose
Many areas of the cerebral cortex process sensory information or coordinate motor output necessary for control of movement. Disturbances in cortical cholinergic system can affect locomotor coordination. Spinal cord injury causes severe motor impairment and disturbances in cholinergic signalling can aggravate the situation. Considering the impact of cortical cholinergic firing in locomotion, we focussed the study in understanding the cholinergic alterations in cerebral cortex during spinal cord injury. The gene expression of key enzymes in cholinergic pathway - acetylcholine esterase and choline acetyl transferase showed significant upregulation in the cerebral cortex of spinal cord injured group compared to control with the fold increase in expression of acetylcholine esterase prominently higher than cholineacetyl transferase...
July 2017: Biochemistry and Biophysics Reports
https://www.readbyqxmd.com/read/29113468/hippocampal-cholinergic-neurostimulating-peptide-as-a-possible-modulating-factor-against-glutamatergic-neuronal-disability-by-amyloid-oligomers
#11
Toyohiro Sato, Yoshiaki Ohi, Daisuke Kato, Masayuki Mizuno, Hiroshi Takase, Tetsuko Kanamori, Cesar V Borlongan, Akira Haji, Noriyuki Matsukawa
Despite having pathological changes in the brain associated with Alzheimer's disease (AD), some patients have preserved cognitive function. A recent epidemiological study has shown that diet, exercise, cognitive training, and vascular risk monitoring interventions may reduce cognitive decline in at-risk elderly people in the general population. However, the details of molecular mechanisms underlying this cognitive function preservation are still unknown. Previous reports have demonstrated that enriched environments prevent the impairment of hippocampal long-term potentiation (LTP) through β2-adrenergic signals, when LTP is incompletely suppressed by synthetic amyloid-β (Aβ) oligomers...
September 2017: Cell Transplantation
https://www.readbyqxmd.com/read/29110801/enhanced-electrical-field-stimulated-nitrergic-and-purinergic-vasoreactivity-in-distal-vs-proximal-internal-pudendal-arteries
#12
Michael R Odom, Elena S Pak, David A Brown, Johanna L Hannan
BACKGROUND: The internal pudendal arteries (IPAs) supply blood to the penis and are highly susceptible to vascular remodeling in rodent models of diabetes, hypertension, aging, and chronic kidney disease, thus contributing to erectile dysfunction. Interestingly, vascular remodeling primarily occurs in the distal and not in the proximal IPA, suggesting distinct local physiologic signaling differences within the IPA. AIM: To examine the role of purinergic signaling and neurotransmitter release by electrical field stimulation (EFS) in the regulation of proximal and distal IPA vascular tone...
November 2017: Journal of Sexual Medicine
https://www.readbyqxmd.com/read/29107522/-silent-nmda-synapses-enhance-motion-sensitivity-in-a-mature-retinal-circuit
#13
Santhosh Sethuramanujam, Xiaoyang Yao, Geoff deRosenroll, Kevin L Briggman, Greg D Field, Gautam B Awatramani
Retinal direction-selective ganglion cells (DSGCs) have the remarkable ability to encode motion over a wide range of contrasts, relying on well-coordinated excitation and inhibition (E/I). E/I is orchestrated by a diverse set of glutamatergic bipolar cells that drive DSGCs directly, as well as indirectly through feedforward GABAergic/cholinergic signals mediated by starburst amacrine cells. Determining how direction-selective responses are generated across varied stimulus conditions requires understanding how glutamate, acetylcholine, and GABA signals are precisely coordinated...
October 25, 2017: Neuron
https://www.readbyqxmd.com/read/29107209/phkv-a-toxin-isolated-from-the-spider-venom-induces-antinociception-by-inhibition-of-cholinesterase-activating-cholinergic-system
#14
Flavia Karine Rigo, Mateus Fortes Rossato, Gabriela Trevisan, Samira Dal-Toé De Prá, Rafael Porto Ineu, Mariane Bernardo Duarte, Célio José de Castro Junior, Juliano Ferreira, Marcus Vinicius Gomez
BACKGROUND AND AIMS: Cholinergic agents cause antinociception by mimicking the release of acetylcholine (ACh) from spinal cholinergic nerves. PhKv is a peptide isolated from the venom of the armed spider Phoneutria nigriventer. It has an antiarrythmogenic activity that involves the enhanced release of acetylcholine. The aim of this study was to investigate whether PhKv had an antinociceptive action in mice. METHODS: Male albino Swiss mice (25-35g) were used in this study...
October 26, 2017: Scandinavian Journal of Pain
https://www.readbyqxmd.com/read/29104018/the-influence-of-midazolam-on-heart-rate-arises-from-cardiac-autonomic-tones-alterations-in-burmese-pythons-python-molurus
#15
Ivã Guidini Lopes, Vinicius Araújo Armelin, Victor Hugo da Silva Braga, Luiz Henrique Florindo
The GABAA receptor agonist midazolam is a compound widely used as a tranquilizer and sedative in mammals and reptiles. It is already known that this benzodiazepine produces small to intermediate heart rate (HR) alterations in mammals, however, its influence on reptiles' HR remains unexplored. Thus, the present study sought to verify the effects of midazolam on HR and cardiac modulation in the snake Python molurus. To do so, the snakes' HR, cardiac autonomic tones, and HR variability were evaluated during four different experimental stages...
October 28, 2017: Autonomic Neuroscience: Basic & Clinical
https://www.readbyqxmd.com/read/29101464/gabaa-receptor-a-unique-modulator-of-excitability-ca-2-signaling-and-catecholamine-release-of-rat-chromaffin-cells
#16
REVIEW
Tzitzitlini Alejandre-García, Johanna G Peña-Del Castillo, Arturo Hernández-Cruz
The role of gamma-aminobutyric acid (GABA) in adrenal medulla chromaffin cell (CC) function is just beginning to unfold. GABA is stored in catecholamine (CA)-containing dense core granules and is presumably released together with CA, ATP, and opioids in response to physiological stimuli, playing an autocrine-paracrine role on CCs. The reported paradoxical "dual action" of GABAA-R activation (enhancement of CA secretion and inhibition of synaptically evoked CA release) is only one aspect of GABA's multifaceted actions...
November 3, 2017: Pflügers Archiv: European Journal of Physiology
https://www.readbyqxmd.com/read/29100274/nicotine-induces-ep4-receptor-expression-in-lung-carcinoma-cells-by-acting-on-ap-2%C3%AE-the-intersection-between-cholinergic-and-prostanoid-signaling
#17
Yu Fan, Ke Wang
It was demonstrated that nicotine increased non-small cell lung cancer cell proliferation through nicotinic acetylcholine receptor -mediated signals. However, the detailed mechanism remains incompletely understood. We evaluated whether nicotine increased EP4 receptor expression in lung carcinoma cells by activating on AP-2α. METHODS: The non-small cell lung cancer cells of A549 and H1838 were cultured and treated with EP4 inhibitor AH23848, also with EP4 and control siRNAs. The extracellular signal-regulated kinases inhibitor PD98059, the p38 mitogen-activated protein kinase inhibitor SB239063, the α7 nicotinic acetylcholine receptor inhibitor α-bungarotoxin, the α4 nicotinic acetylcholine receptor inhibitor dihydro-β-erythroidine, the PI3K inhibitor wortmannin, the PKC inhibitor calphostin C, and the PKA inhibitor H89 have been used to evaluate the effects on proliferations...
September 29, 2017: Oncotarget
https://www.readbyqxmd.com/read/29097596/ck2-oppositely-modulates-l-dopa-induced-dyskinesia-via-striatal-projection-neurons-expressing-d1-or-d2-receptors
#18
Marisol Cortés, Lauren Malave, Julia Castello, Marc Flajolet, M Angela Cenci, Eitan Friedman, Heike Rebholz
We have previously shown that casein kinase 2 (CK2) negatively regulates dopamine D1- and adenosine A2a receptor signaling in the striatum. Ablation of CK2 in D1-receptor-positive striatal neurons caused enhanced locomotion and exploration at baseline, whereas CK2 ablation in D2 receptor-positive neurons caused increased locomotion after treatment with A2a antagonist, caffeine. Since both, D1 and A2a receptors, play major roles in the cellular responses to L-DOPA in the striatum, these findings prompted us to examine the impact of CK2 ablation on the effects of L-DOPA treatment in the unilateral 6-OHDA lesioned mouse model of Parkinson's disease...
November 2, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/29092846/bdnf-overexpression-in-bladder-induces-neuronal-changes-to-mediate-bladder-overactivity
#19
Mahendra Kashyap, Subrata Pore, William C de Groat, Christopher Chermansky, Naoki Yoshimura, Pradeep Tyagi
Elevated levels of brain derived neurotrophic factor (BDNF) in urine of overactive bladder (OAB) patients support the association of BDNF with OAB symptoms, but the causality is not known. Here, we investigated the functionality of BDNF overexpression in rat bladder following bladder wall transfection of either BDNF or luciferase transgenes (10µg). A week after transfection, BDNF overexpression in bladder tissue and elevation of urine BDNF levels was observed together with increased transcript of BDNF, its cognate receptors (TrkB & p75NTR) and downstream PLCγ isoforms in bladder...
November 1, 2017: American Journal of Physiology. Renal Physiology
https://www.readbyqxmd.com/read/29089979/therapeutic-potential-of-%C3%AE-7-nicotinic-receptor-agonists-to-regulate-neuroinflammation-in-neurodegenerative-diseases
#20
REVIEW
Laura Foucault-Fruchard, Daniel Antier
Neurodegenerative diseases, such as Alzheimer's, Parkinson's and Huntington's diseases, are all characterized by a component of innate immunity called neuroinflammation. Neuronal loss and neuroinflammation are two phenomena closely linked. Hence, the neuroinflammation is a relevant target for the management of the neurodegenerative diseases given that, to date, there is no treatment to stop neuronal loss. Several studies have investigated the potential effects of activators of alpha 7 nicotinic acetylcholine receptors in animal models of neurodegenerative diseases...
September 2017: Neural Regeneration Research
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