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Anti cholinergics

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https://www.readbyqxmd.com/read/28822039/stimulation-of-nachr%C3%AE-7-receptor-inhibits-tnf-synthesis-and-secretion-in-response-to-lps-treatment-of-mast-cells-by-targeting-erk1-2-and-tace-activation
#1
F Guzmán-Mejía, C López-Rubalcava, C González-Espinosa
The cholinergic anti-inflammatory pathway is recognized as one of the main mechanisms of neuromodulation of the immune system. Activation of the α7 nicotinic acetylcholine receptor (nAchRα7) suppresses cytokine synthesis in distinct immune cells but the molecular mechanisms behind this effect remain to be fully described. Mast cells (MCs) are essential players of allergic reactions and innate immunity responses related to chronic inflammation. Activation of TLR4 receptor in MCs leads to the rapid secretion of pre-synthesized TNF from intracellular pools and to the activation of NFκB, necessary for de novo synthesis of TNF and other cytokines...
August 18, 2017: Journal of Neuroimmune Pharmacology: the Official Journal of the Society on NeuroImmune Pharmacology
https://www.readbyqxmd.com/read/28818494/gts-21-reduces-microvascular-permeability-during-experimental-endotoxemia
#2
Karsten Schmidt, Sukanya Bhakdisongkhram, Florian Uhle, Christoph Philipsenburg, Aleksandar R Zivkovic, Thorsten Brenner, Johann Motsch, Markus A Weigand, Stefan Hofer
INTRODUCTION: No effective pharmacological therapy is currently available to attenuate tissue edema formation due to increased microvascular permeability in sepsis. Cholinergic mediators have been demonstrated to exert anti-inflammatory effects via the α7 nicotinic acetylcholine receptor (α7nAChR) during inflammation. GTS-21, a partial α7nAChR agonist, is an appealing therapeutic substance for sepsis-induced microvascular inflammation due to its demonstrated cholinergic anti-inflammatory properties and its favorable safety profile in clinical trials...
August 14, 2017: Microvascular Research
https://www.readbyqxmd.com/read/28806219/selective-activation-of-basal-forebrain-cholinergic-neurons-attenuates-polymicrobial-sepsis-induced-inflammation-via-the-cholinergic-anti-inflammatory-pathway
#3
Qian Zhai, Dengming Lai, Ping Cui, Rui Zhou, Qixing Chen, Jinchao Hou, Yunting Su, Libiao Pan, Hui Ye, Jing-Wei Zhao, Xiangming Fang
OBJECTIVES: Basal forebrain cholinergic neurons are proposed as a major neuromodulatory system in inflammatory modulation. However, the function of basal forebrain cholinergic neurons in sepsis is unknown, and the neural pathways underlying cholinergic anti-inflammation remain unexplored. DESIGN: Animal research. SETTING: University research laboratory. SUBJECTS: Male wild-type C57BL/6 mice and ChAT-ChR2-EYFP (ChAT) transgenic mice...
August 10, 2017: Critical Care Medicine
https://www.readbyqxmd.com/read/28806057/rational-design-and-multi-biological-profiling-of-novel-donepezil-trolox-hybrids-against-alzheimer-s-disease-with-cholinergic-antioxidant-neuroprotective-and-cognition-enhancing-properties
#4
Pei Cai, Si-Qiang Fang, Xue-Lian Yang, Jia-Jia Wu, Qiao-Hong Liu, Hao Hong, Xiao-Bing Wang, Lingyi Kong
A novel series of donepezil-trolox hybrids were designed, synthesized and evaluated as multifunctional ligands against Alzheimer's disease (AD). Biological assays showed that these derivatives possessed moderate to good inhibitory activities against acetylcholinesterase (AChE) and monoamine oxidase B (MAO-B) as well as remarkable antioxidant effects. The optimal compound 6d exhibited balanced functions with good inhibition against hAChE (IC50 = 0.54 μM) and hMAO-B (IC50 = 4.3 μM), significant antioxidant activity (41...
August 14, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28797614/delayed-varenicline-administration-reduces-inflammation-and-improves-forelimb-use-following-experimental-stroke
#5
Siyi Chen, Laura Bennet, Ailsa L McGregor
BACKGROUND: Pharmacological activation of the cholinergic anti-inflammatory pathway (CAP), specifically by activating α7 nicotinic acetylcholine receptors, has been shown to confer short-term improvements in outcome. Most studies have investigated administration within 24 hours of stroke, and few have investigated drugs approved for use in human patients. We investigated whether delayed administration of varenicline, a high-affinity agonist at α7 nicotinic receptors and an established therapy for nicotine addiction, decreased brain inflammation and improved functional performance in a mouse model of experimental stroke...
August 7, 2017: Journal of Stroke and Cerebrovascular Diseases: the Official Journal of National Stroke Association
https://www.readbyqxmd.com/read/28766689/nicotine-induces-tipe2-upregulation-and-stat3-phosphorylation-contributes-to-cholinergic-anti-inflammatory-effect
#6
Hua Xiu Sui, Shi Zhong Ke, Dan Dan Xu, Nan Nan Lu, Yi Nan Wang, Yue Hua Zhang, Feng Guang Gao
Cholinergic anti-inflammatory pathway has therapeutic effect on inflammation-associated diseases. However, the exact mechanism of nicotine-mediated anti-inflammatory effect is still unclear. TIPE2, a new member of tumor necrosis factor-α-induced protein-8 family, is a negative regulator of immune homeostasis. However, the roles of TIPE2 in cholinergic anti-inflammatory effect are still uncertain. Here, we demonstrated that nicotine exerts its anti-inflammatory effect by TIPE2 upregulation and phosphorylated stat3 mediated the inhibition of NF-κB activation, which was supported by the following evidence: firstly, both nicotine and TIPE2 inhibit pro-inflammatory cytokine release via NF-κB inactivation...
September 2017: International Journal of Oncology
https://www.readbyqxmd.com/read/28766165/chagas-disease-modulation-of-the-inflammatory-response-by-acetylcholinesterase-in-hematological-cells-and-brain-tissue
#7
Aniélen D Silva, Nathieli B Bottari, Guilherme M do Carmo, Matheus D Baldissera, Carine F Souza, Vanessa S Machado, Vera M Morsch, Maria Rosa C Schetinger, Ricardo E Mendes, Silvia G Monteiro, Aleksandro S Da Silva
Chagas disease is an acute or chronic illness that causes severe inflammatory response, and consequently, it may activate the inflammatory cholinergic pathway, which is regulated by cholinesterases, including the acetylcholinesterase. This enzyme is responsible for the regulation of acetylcholine levels, an anti-inflammatory molecule linked to the inflammatory response during parasitic diseases. Thus, the aim of this study was to investigate whether Trypanosoma cruzi infection can alter the activity of acetylcholinesterase and acetylcholine levels in mice, and whether these alterations are linked to the inflammatory cholinergic signaling pathway...
August 1, 2017: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/28751232/omalizumab-treatment-in-chronic-inducible-urticaria-a-systematic-review-of-published-evidence
#8
Marcus Maurer, Martin Metz, Randolf Brehler, Uwe Hillen, Thilo Jakob, Vera Mahler, Claudia Pföhler, Petra Staubach, Regina Treudler, Bettina Wedi, Markus Magerl
BACKGROUND: Omalizumab, a recombinant anti-IgE antibody, effectively treats chronic spontaneous urticaria. Evidence is lacking in chronic inducible urticarias (CIndUs), which are frequently H1-antihistamine resistant. OBJECTIVE: We aimed to determine, from the current published literature, the strength of evidence for omalizumab efficacy and safety in the treatment of CIndUs. METHODS: We performed a PubMed® search to identify evidence on omalizumab use in the following nine CIndU subtypes: symptomatic dermographism, cold urticaria, delayed pressure urticaria, solar urticaria, heat urticaria, vibratory angioedema, cholinergic urticaria, contact urticaria and aquagenic urticaria...
July 24, 2017: Journal of Allergy and Clinical Immunology
https://www.readbyqxmd.com/read/28749416/anti-oxidative-stress-activity-is-essential-for-amanita-caesarea-mediated-neuroprotection-on-glutamate-induced-apoptotic-ht22-cells-and-an-alzheimer-s-disease-mouse-model
#9
Zhiping Li, Xia Chen, Wenqian Lu, Shun Zhang, Xin Guan, Zeyu Li, Di Wang
Amanita caesarea, an edible mushroom found mainly in Asia and southern Europe, has been reported to show good antioxidative activities. In the present study, the neuroprotective effects of A. caesarea aqueous extract (AC) were determined in an l-glutamic acid (l-Glu) induced HT22 cell apoptosis model, and in a d-galactose (d-gal) and AlCl₃-developed experimental Alzheimer's disease (AD) mouse model. In 25 mM of l-Glu-damaged HT22 cells, a 3-h pretreatment with AC strongly improved cell viability, reduced the proportion of apoptotic cells, restored mitochondrial function, inhibited the over-production of intracellular reactive oxygen species (ROS) and Ca(2+), and suppressed the high expression levels of cleaved-caspase-3, calpain 1, apoptosis-inducing factor (AIF) and Bax...
July 27, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28724203/huprine-x-attenuates-the-neurotoxicity-induced-by-kainic-acid-especially-brain-inflammation
#10
J Relat, B Pérez, P Camps, D Muñoz-Torrero, A Badia, M V Clos
Huprine X (HX) is a synthetic anticholinesterasic compound that exerts a potent inhibitory action on acetylcholinesterase (AChE) activity, an agonist effect on cholinergic receptors, neuroprotective activity in different neurotoxicity models in vivo and in vitro and cognition enhancing effects in non-transgenic (C57BL/6) and transgenic (3xTg-AD, APPswe) mice. In the present study, we assessed the ability of HX (0.8 mg/kg, 21 days) to prevent the damage induced by kainic acid (KA; 28 mg/kg) regarding apoptosis, glia reactivity and neurogenesis in mouse brain...
July 19, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28720101/drug-candidates-in-clinical-trials-for-alzheimer-s-disease
#11
REVIEW
Shih-Ya Hung, Wen-Mei Fu
Alzheimer's disease (AD) is a major form of senile dementia, characterized by progressive memory and neuronal loss combined with cognitive impairment. AD is the most common neurodegenerative disease worldwide, affecting one-fifth of those aged over 85 years. Recent therapeutic approaches have been strongly influenced by five neuropathological hallmarks of AD: acetylcholine deficiency, glutamate excitotoxicity, extracellular deposition of amyloid-β (Aβ plague), formation of intraneuronal neurofibrillary tangles (NTFs), and neuroinflammation...
July 19, 2017: Journal of Biomedical Science
https://www.readbyqxmd.com/read/28704107/asthma-medication-use-among-adults-with-current-asthma-by-work-related-asthma-status-asthma-call-back-survey-29-states-2012-2013
#12
Katelynn E Dodd, Jacek M Mazurek
OBJECTIVE: Asthma severity is defined as the intensity of treatment required to achieve good control of asthma symptoms. Studies have shown that work-related asthma (WRA) can be associated with poorer asthma control and more severe symptoms than non-WRA. Associations between asthma medications and WRA status were assessed using data from the 2012-2013 Asthma Call-back Survey among ever-employed adults (≥18 years) with current asthma from 29 states. METHODS: Persons with WRA had been told by a physician that their asthma was work-related...
July 13, 2017: Journal of Asthma: Official Journal of the Association for the Care of Asthma
https://www.readbyqxmd.com/read/28702935/vitamin-d3-attenuates-cognitive-deficits-and-neuroinflammatory-responses-in-icv-stz-induced-sporadic-alzheimer-s-disease
#13
P Yamini, R S Ray, Kanwaljit Chopra
Alzheimer's disease (AD) is a progressive neurodegenerative disorder characterized by intracellular neurofibrillary tangles and extracellular Aβ deposition. Growing experimental evidence indicate diverse biological effects of vitamin D3 including antioxidant, neuroprotective, anti-inflammatory and cardiovascular benefits. However, the underlying neuroprotective mechanism of vitamin D3 is still largely elusive. Therefore, the present study was aimed to investigate the neuroprotective effects of vitamin D3 on ICV-STZ induced sporadic AD...
July 12, 2017: Inflammopharmacology
https://www.readbyqxmd.com/read/28699699/involvement-of-cholinergic-and-adenosinergic-systems-on-the-branchial-immune-response-of-experimentally-infected-silver-catfish-with-streptococcus-agalactiae
#14
M D Baldissera, C F Souza, P H Doleski, K L S Moreira, M L da Veiga, M I U M da Rocha, R C V Santos, B Baldisserotto
It has been recognized that the cholinergic and adenosinergic systems have an essential role in immune and inflammatory responses during bacterial fish pathogens, such as the enzymes acetylcholinesterase (AChE) and adenosine deaminase (ADA), which are responsible for catalysis of the anti-inflammatory molecules acetylcholine (ACh) and adenosine (Ado) respectively. Thus, the aim of this study was to investigate the involvement of the cholinergic and adenosinergic systems on the immune response and inflammatory process in gills of experimentally infected Rhamdia quelen with Streptococcus agalactiae...
July 12, 2017: Journal of Fish Diseases
https://www.readbyqxmd.com/read/28687927/the-distribution-of-cholinergic-neurons-and-their-co-localization-with-fmrfamide-in-central-and-peripheral-neurons-of-the-spider-cupiennius-salei
#15
Ruth Fabian-Fine, Carly M Anderson, Molly A Roush, Jessica A G Johnson, Hongxia Liu, Andrew S French, Päivi H Torkkeli
The spider Cupiennius salei is a well-established model for investigating information processing in arthropod sensory systems. Immunohistochemistry has shown that several neurotransmitters exist in the C. salei nervous system, including GABA, glutamate, histamine, octopamine and FMRFamide, while electrophysiology has found functional roles for some of these transmitters. There is also evidence that acetylcholine (ACh) is present in some C. salei neurons but information about the distribution of cholinergic neurons in spider nervous systems is limited...
July 7, 2017: Cell and Tissue Research
https://www.readbyqxmd.com/read/28687462/the-effect-of-tiotropium-in-combination-with-olodaterol-on-house-dust-mite-induced-allergic-airway-disease
#16
Gerrit John-Schuster, Stan de Kleijn, Yolanda van Wijck, Veerle Kremer, Hermelijn H Smits, Michael P Pieper, Pieter S Hiemstra, Christian Taube
One of the major goals of asthma therapy is to maintain asthma control and prevent acute exacerbations. Long-acting bronchodilators are regularly used for the treatment of asthma patients and in clinical studies the anti-cholinergic tiotropium has recently been shown to reduce exacerbations in patients with asthma. So far it is unclear how tiotropium exerts this effect. For this purpose, we designed an allergen-driven rechallenge model of allergic airway inflammation in mice, to assess the effectiveness of tiotropium and the long-acting β-2 adrenoceptor agonist olodaterol on allergen-induced exacerbations of airway disease...
August 2017: Pulmonary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/28685687/modulators-of-acetylcholinesterase-activity-from-alzheimer-s-disease-to-anti-cancer-drugs
#17
Tamara Lazarević-Pašti, Andreja Leskovac, Tatjana Momić, Sandra Petrović, Vesna Vasić
BACKGROUND: Acetylcholinesterase (AChE) is involved in the termination of impulse transmission by rapid hydrolysis of the neurotransmitter acetylcholine in numerous cholinergic pathways in the central and peripheral nervous systems. The enzyme inactivation leads to acetylcholine accumulation, hyperstimulation of nicotinic and muscarinic receptors, and disrupted neurotransmission. Hence, acetylcholinesterase inhibitors, interacting with the enzyme as their primary target, are applied as relevant drugs for different neurodegenerative diseases (such as Alzheimer's and Parkinson's) as well as toxins...
July 5, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28673740/forebrain-knock-out-of-torsina-reduces-striatal-free-water-and-impairs-whole-brain-functional-connectivity-in-a-symptomatic-mouse-model-of-dyt1-dystonia
#18
Jesse C DeSimone, Samuel S Pappas, Marcelo Febo, Roxana G Burciu, Priyank Shukla, Luis M Colon-Perez, William T Dauer, David E Vaillancourt
Multiple lines of evidence implicate striatal dysfunction in the pathogenesis of dystonia, including in DYT1, a common inherited form of the disease. The impact of striatal dysfunction on connected motor circuits and their interaction with other brain regions is poorly understood. Conditional knock-out (cKO) of the DYT1 protein torsinA from forebrain cholinergic and GABAergic neurons creates a symptomatic model that recapitulates many characteristics of DYT1 dystonia, including the developmental onset of overt twisting movements that are responsive to antimuscarinic drugs...
October 2017: Neurobiology of Disease
https://www.readbyqxmd.com/read/28660314/nicotine-chewing-gum-for-the-prevention-of-postoperative-ileus-after-colorectal-surgery-a-multicenter-double-blind-randomised-controlled-pilot-study
#19
Daniël P V Lambrichts, Geesien S A Boersema, Buket Tas, Zhouqiao Wu, Wietske W Vrijland, Gert-Jan Kleinrensink, Johannes Jeekel, Johan F Lange, Anand G Menon
PURPOSE: When postoperative ileus is not resolved after 5 days or recurs after resolution, prolonged POI (PPOI) is diagnosed. PPOI increases discomfort, morbidity and hospitalisation length, and is mainly caused by an inflammatory response following intestinal manipulation. This response can be weakened by targeting the cholinergic anti-inflammatory pathway, with nicotine as essential regulator. Chewing gum, already known to stimulate gastrointestinal motility itself, combined with nicotine is hypothesised to improve gastrointestinal recovery and prevent PPOI...
June 28, 2017: International Journal of Colorectal Disease
https://www.readbyqxmd.com/read/28651185/treatment-of-neurocognitive-symptoms-in-unipolar-depression-a-systematic-review-and-future-perspectives
#20
REVIEW
E Salagre, B Solé, Y Tomioka, B S Fernandes, D Hidalgo-Mazzei, M Garriga, E Jimenez, J Sanchez-Moreno, E Vieta, I Grande
BACKGROUND: Cognitive symptoms in Major Depressive Disorder (MDD) are persistent and commonly entail neurocognitive impairment and a decline in quality of life. This systematic review gathers the current scientific evidence on therapeutic strategies for neuropsychological impairment in MDD. METHOD: A systematic search on PubMed, PsycINFO and Clinicaltrials.gov was carried out on December 2016 according to PRISMA using Boolean terms to identify interventions for the treatment of cognitive dysfunction in MDD...
October 15, 2017: Journal of Affective Disorders
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