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Anti cholinergics

X M Chen, F Q Li, S Yan, X C Wu, C L Tang
OBJECTIVE: To investigate the anti-inflammation effects by activation of the cholinergic anti-inflammatory pathway and its mechanisms in non-alcoholic steatohepatitis (NASH) model mice. METHODS: 6-week-old male C57BL/6J (B6) mice were randomly divided into four groups: the first group was normal mice, injected with saline; the second group was normal mice, injected with nicotine; the third group was NASH model mice, injected with saline; the fourth group was NASH model mice, injected with nicotine...
October 18, 2016: Beijing da Xue Xue Bao. Yi Xue Ban, Journal of Peking University. Health Sciences
Nathalia M Pinheiro, Fernanda P R Santana, Rafael Ribeiro Almeida, Marina Guerreiro, Milton A Martins, Luciana C Caperuto, Niels O S Câmara, Lislaine A Wensing, Vânia F Prado, Iolanda F L C Tibério, Marco Antônio M Prado, Carla M Prado
Nicotinic α-7 acetylcholine receptor (nAChRα7) is a critical regulator of cholinergic anti-inflammatory actions in several diseases, including acute respiratory distress syndrome (ARDS). Given the potential importance of α7nAChR as a therapeutic target, we evaluated whether PNU-282987, an α7nAChR agonist, is effective in protecting the lung against inflammation. We performed intratracheal instillation of LPS to generate acute lung injury (ALI) in C57BL/6 mice. PNU-282987 treatment, either before or after ALI induction, reduced neutrophil recruitment and IL-1β, TNF-α, IL-6, keratinocyte chemoattractant (KC), and IL-10 cytokine levels in the bronchoalveolar lavage fluid (P < 0...
October 11, 2016: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
Katarina Spilovska, Jan Korabecny, Eugenie Nepovimova, Rafael Dolezal, Eva Mezeiova, Ondrej Soukup, Kamil Kuca
Alzheimer's disease (AD) is a multifactorial neurodegenerative disorder. Several hallmarks such as β-amyloid (Aβ) aggregation underlying amyloid plaque formation, τ-hyperphosphorylation leading to the production of neurofibrillary tangles, and decline in the number of cholinergic neurons appear to be fundamental in the pathophysiology of the disease. Other evidence points also to the involvement of oxidative stress, biometal dyshomeostasis, inflammation, and cell cycle regulatory failure. Taking into account such premises, many attractive targets for the development of anti-AD drugs have emerged...
September 27, 2016: Current Topics in Medicinal Chemistry
Musaddique Hussain, Hafiz Muhammad Waqas, Shahid Masood Raza, Umer Farooq, Muhammad Masood Ahmed, Abdul Majeed
ETHNOPHARMACOLOGICAL RELEVANCE: Seeds of Sisymbrium irio Linn has been used traditionally in different regions of Pakistan for the treatment of gastrointestinal, airways and vascular system ailments. To insight the pharmacological basis, in vitro study was conducted in order to validate its folkloric uses. MATERIAL AND METHODS: 70% aqueous-methanolic extract of seeds from S. irio (Si.MEs) was tested on isolated rabbit aorta, jejunum and trachea strip hanged in tissue bath having physiological solutions aerated with carbogen and their responses were measured and recorded via Power Lab...
September 29, 2016: Journal of Ethnopharmacology
Weixi Liu, Hang Ma, Nicholas A DaSilva, Kenneth N Rose, Shelby L Johnson, Lu Zhang, Chunpeng Wan, Joel A Dain, Navindra P Seeram
Medicinal plants are promising candidates for Alzheimer's disease (AD) research but there is lack of systematic algorithms and procedures to guide their selection and evaluation. Herein, we developed a Neuroprotective Potential Algorithm (NPA) by evaluating twenty-three standardized and chemically characterized Ayurvedic medicinal plant extracts in a panel of bioassays targeting oxidative stress, carbonyl stress, protein glycation, amyloid beta (Aβ) fibrillation, acetylcholinesterase (AChE) inhibition, and neuroinflammation...
September 29, 2016: Neurochemistry International
James Winter, Alexandra R Cook, Dawn H Patient, Stevan R Emmett, John Tattersall, Michael J Shattock
Pre-treatment with reversible acetylcholinesterase (AChE) inhibitors is an effective strategy for reducing lethality following organophosphate nerve agent exposure. AChE inhibition may have unwanted cardiac side effects, which could be negated by adjunctive anti-cholinergic therapy. The aims of the present study were to examine the concentration-dependent effects of physostigmine on cardiac responses to vagus nerve stimulation (VNS), to test whether adjunctive treatment with hyoscine can reverse these effects and to assess the functional interaction and electrophysiological consequences of a combined pre-treatment...
September 28, 2016: Neurotoxicology
Priya Revathikumar, Filip Bergqvist, Srividya Gopalakrishnan, Marina Korotkova, Per-Johan Jakobsson, Jon Lampa, Erwan Le Maître
BACKGROUND: The cholinergic anti-inflammatory pathway (CAP) primarily functions through acetylcholine (ACh)-alpha7 nicotinic acetylcholine receptor (α7nAChR) interaction on macrophages to control peripheral inflammation. Interestingly, ACh can also bind α7nAChRs on microglia resulting in neuroprotective effects. However, ACh effects on astrocytes remain elusive. Here, we investigated the effects of nicotine, an ACh receptor agonist, on the cytokine and cholinesterase production of immunocompetent human astrocytes stimulated with interleukin 1β (IL-1β) in vitro...
September 29, 2016: Journal of Neuroinflammation
Francesco Panza, Davide Seripa, Vincenzo Solfrizzi, Bruno P Imbimbo, Madia Lozupone, Antonio Leo, Rodolfo Sardone, Gaetano Gagliardi, Lucia Lofano, Bianca C Creanza, Paola Bisceglia, Antonio Daniele, Antonello Bellomo, Antonio Greco, Giancarlo Logroscino
Currently available drugs against Alzheimer's disease (AD) target cholinergic and glutamatergic neurotransmissions without affecting the underlying disease process. Putative disease-modifying drugs are in development and target β-amyloid (Aβ) peptide and tau protein, the principal neurophatological hallmarks of the disease. Areas covered: Phase III clinical studies of emerging anti-Aβ drugs for the treatment of AD were searched in US and EU clinical trial registries and in the medical literature until May 2016...
October 6, 2016: Expert Opinion on Emerging Drugs
Preshanta Naicker, Shailendra Anoopkumar-Dukie, Gary D Grant, Justin J Kavanagh
RATIONALE: Acetylcholine is an important neuromodulator in the central nervous system, where it plays a significant role in central functions such as the regulation of movement. OBJECTIVE: This study investigated the pharmacological effects of over-the-counter anticholinergic medications on saccadic and smooth pursuit eye movements, in order to establish the significance of central cholinergic pathways in the control of these centrally regulated oculomotor processes...
September 26, 2016: Psychopharmacology
Sailesh C Harwani, Jason Ratcliff, Fayyaz S Sutterwala, Zuhair K Ballas, David K Meyerholz, Mark W Chapleau, Francois Abboud
RATIONALE: Renal inflammation contributes to the pathophysiology of hypertension. CD161a+ immune cells are dominant in the Spontaneously Hypertensive Rat (SHR) and expand in response to nicotinic cholinergic activation. OBJECTIVE: We aimed to phenotype CD161a+ immune cells in pre-hypertensive SHR following cholinergic activation with nicotine, and determine if these cells are involved in renal inflammation and the development of hypertension. METHODS AND RESULTS: Studies utilized young SHR and Wistar Kyoto (WKY) rats...
September 22, 2016: Circulation Research
Akash Gautam, Renu Wadhwa, Mahendra K Thakur
BACKGROUND: In our earlier study, we have shown the memory enhancing and scopolamine-induced amnesia recovery properties of Ashwagandha leaf extract using behavioral paradigm and expression analysis of synaptic plasticity genes. PURPOSE: However, the exact mechanism through which Ashwagandha demonstrates these effects is still unknown. METHODS: In the present study, we hypothesized that the alcoholic extract of Ashwagandha leaves (i-Extract) possesses cholinergic properties, which in turn inhibit the anti-cholinergic nature of scopolamine...
July 2016: Annals of Neurosciences
Hélio José Coelho Junior, Bruno Bavaresco Gambassi, Tiego Aparecido Diniz, Isabela Maia da Cruz Fernandes, Érico Chagas Caperuto, Marco Carlos Uchida, Fabio Santos Lira, Bruno Rodrigues
Inflammatory markers are increased systematically and locally (e.g., skeletal muscle) in stroke patients. Besides being associated with cardiovascular risk factors, proinflammatory cytokines seem to play a key role in muscle atrophy by regulating the pathways involved in this condition. As such, they may cause severe decrease in muscle strength and power, as well as impairment in cardiorespiratory fitness. On the other hand, physical exercise (PE) has been widely suggested as a powerful tool for treating stroke patients, since PE is able to regenerate, even if partially, physical and cognitive functions...
2016: Mediators of Inflammation
Sekib Sokolovic, Samir Mehmedagic
OBJECTIVE: The goal of this paper was to present the effects of the vagus nerve stimulation (VNS) on a blood pressure (BP) and heart rate (HR) in arterial hypertension patient. DESIGN AND METHOD: The pilot study (SPM-005) was designed to evaluate the eficiancy and safety profile of the neurostimulation of the cholinergic anti-inflammatory pathways using the active implantable device for the vagus nerve stimulation in rheumatoid arthritis patient. We investigated the VNS on the BP and HR in 68 years old female patient with a long-standing arterial hypertension and the lisinopril and hydrochlorothiazide in a therapy...
September 2016: Journal of Hypertension
Shakir D Alsharari, Deniz Bagdas, Hamid I Akbarali, Patraic A Lichtman, Erinn S Raborn, Guy A Cabral, F Ivy Carroll, Elizabeth A McGee, M Imad Damaj
INTRODUCTION: α7 nicotinic acetylcholine receptors (nAChRs) play an important role in vagus nerve-based cholinergic anti-inflammatory effects. This study was designed to assess the role of α7 nAChRs in DSS-induced colitis in male and female mouse. We first compared disease activity and pathogenesis of colitis in α7 knock-out (KO) and wild-type (WT) mice. We then evaluated the effect of several α7 direct and indirect agonists on the severity of disease in the DSS (dextran sodium sulfate)-induced colitis...
September 17, 2016: Nicotine & Tobacco Research: Official Journal of the Society for Research on Nicotine and Tobacco
Michael S Saporito, Eva Zuvich, Amy DiCamillo
Detailed in this unit is a mouse model of overactive bladder and urinary incontinence based on diuretic stress-induced urination. The procedure involves the use of a unique, highly sensitive, and automated urine capturing method to measure urinary latency, frequency, and void volume. Although this method was first described and validated using an anti-muscarinic drug used for treating overactive bladder, subsequent work has shown that effective non-cholinergic agents can be detected. These findings indicate good predictive value for this model regarding the possible clinical utility of test agents as treatments for overactive bladder, regardless of their site of action...
2016: Current Protocols in Pharmacology
Abdul Mannan Baig, H R Ahmad
Acetylcholine affects the target cellular function via muscarinic and nicotinic cholinergic receptors that are seen to exist in humans. Both the cholinergic receptors are G-protein coupled receptors (GPCRs) that perform cardinal functions in humans. Anti-muscarinic drugs, particularly the ones that target M1 subtype (mAChR1), have consistently shown to kill unicellular pathogenic eukaryotes like Acanthamoeba spp. As the M1 receptor subtype has not been reported to be expressed in the above protist, the presence of an ancient form of the M1 muscarinic receptor was inferred...
September 7, 2016: Journal of Receptor and Signal Transduction Research
Zun-Jing Liu, Zhong-Hao Li, Lei Liu, Wen-Xiong Tang, Yu Wang, Ming-Rui Dong, Cheng Xiao
Neuroinflammation is known to have a pivotal role in the pathogenesis of Alzheimer's disease (AD), and curcumin has been reported to have therapeutical effects on AD because of its anti-inflammatory effects. Curcumin is not only a potent PPARγ agonist, but also has neuroprotective effects on cerebral ischemic injury. However, whether PPARγ activated by curcumin is responsible for the anti-neuroinflammation and neuroprotection on AD remains unclear, and needs to be further investigated. Here, using both APP/PS1 transgenic mice and beta-amyloid-induced neuroinflammation in mixed neuronal/glial cultures, we showed that curcumin significantly alleviated spatial memory deficits in APP/PS1 mice and promoted cholinergic neuronal function in vivo and in vitro...
2016: Frontiers in Pharmacology
Virginio Salvi, Claudio Mencacci, Francesco Barone-Adesi
Weight gain and metabolic abnormalities are extensively found in patients taking psychotropic medications. Although mainly antipsychotics have been implicated, also antidepressants carry the potential to induce weight gain, with tricyclics and mirtazapine being associated with the greatest weight gain. It has been suggested that this could be due to the different ability of antidepressants to block adrenergic, cholinergic, and histaminergic postsynaptic receptors. To date, however, the link between antidepressant-induced weight gain and their receptor affinity profile has not been established...
October 2016: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
Hugo F Miranda, Fernando Sierralta, Nicolás Aranda, Viviana Noriega, Juan Carlos Prieto
BACKGROUND: Non-steroidal anti-inflammatory drugs (NSAIDs) may act through others mechanisms, in addition to inhibition of prostaglandin synthesis. These includes cholinergic, NO, serotonergic and opioids pathways. METHODS: The aim of this work was to evaluate the effect of systemic action of (S)-+-ketoprofen (dexketoprofen, DEX) on pain behaviors using the orofacial formalin test in mice and the potential involvement of cholinergic, NO, serotonergic and opioids pathways...
June 25, 2016: Pharmacological Reports: PR
Takaaki Hiragun, Michihiro Hide
For many years, sweat has been recognized as an exacerbation factor in all age groups of atopic dermatitis (AD) and a trigger of cholinergic urticaria (CholU). Recently, we reported the improvement of AD symptoms by spray with tannic acid, which suppresses basophil histamine release by semipurified sweat antigens in vitro, and showering that removes antigens in sweat from the skin surface. We finally identified MGL_1304 secreted by Malassezia globosa as a major histamine-releasing antigen in human sweat. MGL_1304 is detected as a 17-kDa protein in sweat and exhibits almost the highest histamine-release ability from basophils of patients with AD and CholU among antigens derived from Malassezia species...
2016: Current Problems in Dermatology
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