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Physostigmine

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https://www.readbyqxmd.com/read/28500787/corticosterone-primes-the-neuroinflammatory-response-to-gulf-war-illness-relevant-organophosphates-independently-of-acetylcholinesterase-inhibition
#1
Alicia R Locker, Lindsay T Michalovicz, Kimberly A Kelly, Julie V Miller, Diane B Miller, James P O'Callaghan
Gulf War Illness (GWI) is a chronic multi-symptom disorder affecting veterans of the 1991 Gulf War. Among the symptoms of GWI are those associated with sickness behavior, observations suggestive of underlying neuroinflammation. We have shown that exposure of mice to the stress hormone, corticosterone (CORT), and to diisopropyl fluorophosphate (DFP), as a nerve agent mimic, results in marked neuroinflammation, findings consistent with a stress/neuroimmune basis of GWI. Here, we examined the contribution of irreversible and reversible acetylcholinesterase (AChE) inhibitors to neuroinflammation in our mouse model of GWI...
May 13, 2017: Journal of Neurochemistry
https://www.readbyqxmd.com/read/28499986/n-acetylcysteine-treatment-attenuates-the-cognitive-impairment-and-synaptic-plasticity-loss-induced-by-streptozotocin
#2
Michael da Costa, Jamile Bernardi, Lidiane Costa, Tiago Fiuza, Ricardo Brandão, Maria F Ribeiro, Joana D Amaral, Cecília M P Rodrigues, Maria E Pereira
Alzheimer's disease (AD) is a neurodegenerative disorder pathologically characterized by severe neuronal and glial structural changes and progressive cognitive decline. N-acetylcysteine (NAC) is a well-known pharmacological agent with pro-neurogenic properties and neuroprotective effects. In this study, we evaluated NAC protective effects on cognitive impairment and associated pathological markers in a streptozotocin (STZ)-induced sporadic dementia of AD type mice model. Animals were divided into six groups: I) Sham, II) NAC, III) physostigmine (PHY), IV) STZ, V) NAC + STZ and VI) PHY + NAC...
May 9, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28445778/the-impact-of-bilateral-vagotomy-on-the-physostigmine-induced-airway-constriction-in-ferrets
#3
Burim Neziri, Armond Daci, Shaip Krasniqi, Ramadan Sopi, Musa A Haxhiu
Vagal innervations have a great role in the respiratory function and are the main route of signal transmission from respiratory neural centers into the trachea and others conducting airways. We have investigated the role of central mechanisms related to vagal neural pathways and the cholinergic outflow in tracheobronchial smooth muscle tone and lung mechanics parameters. Parameters of lung mechanics such as lung resistance (RL), dynamic compliance (Cdyn) and pressure in bypassed tracheal segment (Ptseg) were measured before and after vagotomy and asphyxia test...
April 23, 2017: Respiratory Physiology & Neurobiology
https://www.readbyqxmd.com/read/28373858/enhanced-cholinergic-activity-improves-cerebral-blood-flow-during-orthostatic-stress
#4
Jorge M Serrador, Roy Freeman
Cerebral blood flow (CBF) and consequently orthostatic tolerance when upright depends on dilation of the cerebral vasculature in the face of reduced perfusion pressure associated with the hydrostatic gradient. However, it is still unclear if cholinergic activation plays a role in this dilation. To determine if enhancing central cholinergic activity with the centrally acting acetylcholinesterase inhibitor, physostigmine would increase CBF when upright compared to the peripherally acting acetylcholinesterase inhibitor, neostigmine, or saline...
2017: Frontiers in Neurology
https://www.readbyqxmd.com/read/28294544/identification-of-acetylcholinesterase-inhibitors-using-homogenous-cell-based-assays-in-quantitative-high-throughput-screening-platforms
#5
Shuaizhang Li, Ruili Huang, Samuel Solomon, Yitong Liu, Bin Zhao, Michael F Santillo, Menghang Xia
Acetylcholinesterase (AChE) is an enzyme responsible for metabolism of acetylcholine, a neurotransmitter associated with muscle movement, cognition, and other neurobiological processes. Inhibition of AChE activity can serve as a therapeutic mechanism, but also cause adverse health effects and neurotoxicity. In order to efficiently identify AChE inhibitors from large compound libraries, homogenous cell-based assays in high-throughput screening platforms are needed. In this study, a fluorescent method using Amplex Red (10-acetyl-3,7-dihydroxyphenoxazine) and the Ellman absorbance method were both developed in a homogenous format using a human neuroblastoma cell line (SH-SY5Y)...
March 14, 2017: Biotechnology Journal
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
#6
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/28238772/assessment-of-anti-cholinesterase-activity-and-cytotoxicity-of-cagaita-eugenia-dysenterica-leaves
#7
Cristian A Gasca, Willian O Castillo, Catarina Satie Takahashi, Christopher W Fagg, Pérola O Magalhães, Yris M Fonseca-Bazzo, Dâmaris Silveira
Eugenia dysenterica ex DC Mart. (Myrtaceae) is a Brazilian tree with pharmacological and biological properties. The aqueous leaf extract, rich in polyphenols, was tested in the human neuroblastoma cell line SH-SY5Y to evaluate its effect on cell viability. The extract and two isolated compounds were also assessed for the potential inhibitory activity on acetylcholinesterase, an enzyme related to Alzheimer's disease. A simple chromatographic method using Sephadex LH-20 was developed to separate catechin and quercetin from the aqueous leaf extract of E...
February 24, 2017: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/27998753/effects-of-intra-hippocampal-microinjection-of-vitamin-b12-on-the-orofacial-pain-and-memory-impairments-induced-by-scopolamine-and-orofacial-pain-in-rats
#8
Amir Erfanparast, Esmaeal Tamaddonfard, Shaghayegh Nemati
In the present study, we investigated the effects of microinjection of vitamin B12 into the hippocampus on the orofacial pain and memory impairments induced by scopolamine and orofacial pain. In ketamine-xylazine anesthetized rats, the right and left sides of the dorsal hippocampus (CA1) were implanted with two guide cannulas. Orofacial pain was induced by subcutaneous injection of formalin (1.5%, 50μl) into the right vibrissa pad, and the durations of face rubbing were recorded at 3-min blocks for 45min. Morris water maze (MWM) was used for evaluation of learning and memory...
December 18, 2016: Physiology & Behavior
https://www.readbyqxmd.com/read/27990564/planarian-cholinesterase-in-vitro-characterization-of-an-evolutionarily-ancient-enzyme-to-study-organophosphorus-pesticide-toxicity-and-reactivation
#9
Danielle Hagstrom, Hideto Hirokawa, Limin Zhang, Zoran Radic, Palmer Taylor, Eva-Maria S Collins
The freshwater planarian Dugesia japonica has recently emerged as an animal model for developmental neurotoxicology and found to be sensitive to organophosphorus (OP) pesticides. While previous activity staining of D. japonica, which possess a discrete cholinergic nervous system, has shown acylthiocholine catalysis, it is unknown whether this is accomplished through an acetylcholinesterase (AChE), butyrylcholinesterase (BChE), or a hybrid esterase and how OP exposure affects esterase activity. Here, we show that the majority of D...
December 18, 2016: Archives of Toxicology
https://www.readbyqxmd.com/read/27895161/the-e-loop-of-the-transmitter-binding-site-is-a-key-determinant-of-the-modulatory-effects-of-physostigmine-on-neuronal-nicotinic-%C3%AE-4%C3%AE-2-receptors
#10
Xiaochun Jin, Megan M McCollum, Allison L Germann, Gustav Akk, Joe Henry Steinbach
Physostigmine is a well known inhibitor of acetylcholinesterase, which can also activate, potentiate, and inhibit acetylcholine receptors, including neuronal nicotinic receptors comprising α4 and β2 subunits. We have found that the two stoichiometric forms of this receptor differ in the effects of physostigmine. The form containing three copies of α4 and two of β2 was potentiated at low concentrations of acetylcholine chloride (ACh) and physostigmine, whereas the form containing two copies of α4 and three of β2 was inhibited...
February 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/27808424/cholinergic-modulation-of-the-parafacial-respiratory-group
#11
Rozlyn C T Boutin, Zaki Alsahafi, Silvia Pagliardini
KEY POINTS: This study investigates the effects of cholinergic transmission on the expiratory oscillator, the parafacial respiratory group (pFRG) in urethane anaesthetized adult rats. Local inhibition of the acetyl cholinesterase enzyme induced activation of expiratory abdominal muscles and active expiration. Local application of the cholinomimetic carbachol elicited recruitment of late expiratory neurons, expiratory abdominal muscle activity and active expiration. This effect was antagonized by local application of the muscarinic antagonists scopolamine, J104129 and 4DAMP...
February 15, 2017: Journal of Physiology
https://www.readbyqxmd.com/read/27799040/optimal-pre-treatment-for-acute-exposure-to-the-organophosphate-dicrotophos
#12
Dietrich Ernst Lorke, Syed M Nurulain, Mohamed Y Hasan, Kamil Kuča, Georg A Petroianu
BACKGROUND: Reversible cholinesterase inhibitors, when given prophylactically before exposure to organophosphates, are able to decrease organophosphate-induced mortality. However, the efficacy of pyridostigmine, the only pre-treatment substance approved by the US Federal Drug Administration, is unsatisfactory. METHODS: In search of a better prophylactic compound, we determined in vivo the protection conferred by five cholinesterase inhibitors (ranitidine, physostigmine, tacrine, K-27 and pyridostigmine), which were administered in equitoxic dosage (1/4 of LD01) 30 minutes before exposure to the organophosphate dicrotophos...
October 27, 2016: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/27773692/pretreatment-and-prophylaxis-against-nerve-agent-poisoning-are-undesirable-behavioral-side-effects-unavoidable
#13
REVIEW
Trond Myhrer, Pål Aas
The threat of chemical warfare agents like nerve agents requires life saving measures of medical pretreatment combined with treatment after exposure. Pretreatment (pyridostigmine) may cause some side effects in a small number of individuals. A comprehensive research on animals has been performed to clarify effects on behavior. The results from these studies are far from unambiguous, since pyridostigmine may produce adverse effects on behavior in animals in relatively high doses, but not in a consistent way...
December 2016: Neuroscience and Biobehavioral Reviews
https://www.readbyqxmd.com/read/27744183/thiadiazolodiazepine-analogues-as-a-new-class-of-neuromuscular-blocking-agents-synthesis-biological-evaluation-and-molecular-modeling-study
#14
Hussein I El-Subbagh, Adel S El-Azab, Ghada S Hassan, Shahenda M El-Messery, Alaa A-M Abdel-Aziz, Kamal E H El-Taher
The synthesis, biological evaluation and molecular modeling study of 6,7-dihydro-[1,3,4] thiadiazolo[3,2-a][1,3]diazepine analogues as new class of neuromuscular blocking agents are described. The new compounds act via competitive mechanism with ACh which could be reversed by the anticholinesterase - Physostigmine. Compounds GS-53 (30) and AAH1 (33) induced dose-dependent neuromuscular blockade with onset time of 3 and 10 min, ED50 0.15 and 0.36 mmol/kg i.p., respectively, in rats. Compound 30 proved to be as twice as potent as 33 with rapid onset and shorter duration (P < 0...
January 27, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27717404/composition-and-cytotoxic-and-antioxidant-activities-of-the-oil-of-piper-aequale-vahl
#15
Joyce Kelly R da Silva, Laine C Pinto, Rommel M R Burbano, Raquel C Montenegro, Eloísa Helena A Andrade, José Guilherme S Maia
BACKGROUND: Piper aequale Vahl is a small shrub that grows in the shadow of large trees in the Carajás National Forest, Municipality of Parauapebas, Para state, Brazil. The local people have used the plant against rheumatism and inflammation. METHODS: The essential oil of the aerial parts was extracted and analyzed by GC and GC-MS. The MTT colorimetric assay was used to measuring the cytotoxic activity of the oil against human cancer lines. The determination of antioxidant activity of the oil was conducted by DPPH radical scavenging assay...
October 7, 2016: Lipids in Health and Disease
https://www.readbyqxmd.com/read/27693445/reversal-of-cardiac-vagal-effects-of-physostigmine-by-adjunctive-muscarinic-blockade
#16
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
https://www.readbyqxmd.com/read/27508961/anti-acetylcholinesterase-activity-of-essential-oils-and-their-major-constituents-from-four-ocimum-species
#17
Mohamed A Farag, Shahira M Ezzat, Maha M Salama, Mariane G Tadros, Rabah A T Serya
Ocimum is a genus of considerable importance in traditional medicine worldwide. The goal of this study was to examine the anti-acetylcholinesterase activity of Ocimum essential oils and to correlate the activity with their chemical profiles using a metabolome based GC-MS approach coupled to chemometrics. Further, molecular docking was adopted to rationalize the activity of some essential oil isolates. Essential oil prepared from the four species O. basilicum, O. africanum, O. americanum, and O. minimum exhibited significant anti-acetylcholinesterase activity with (IC50 0...
November 1, 2016: Zeitschrift Für Naturforschung. C, A Journal of Biosciences
https://www.readbyqxmd.com/read/27445235/in-vivo-neurochemical-evidence-that-delta1-delta2-and-mu2-opioid-receptors-but-not-mu1-opioid-receptors-inhibit-acetylcholine-efflux-in-the-nucleus-accumbens-of-freely-moving-rats
#18
Yuri Kiguchi, Yuri Aono, Yuriko Watanabe, Seiko Yamamoto-Nemoto, Kunihiko Shimizu, Takehiko Shimizu, Yasuhiro Kosuge, John L Waddington, Kumiko Ishige, Yoshihisa Ito, Tadashi Saigusa
Cholinergic neurons in the nucleus accumbens express delta- and mu-opioid receptors that are thought to inhibit neural activity. Delta- and mu-opioid receptors are divided into delta1- and delta2-opioid receptors and mu1- and mu2-opioid receptors, respectively. We analysed the roles of delta- and mu-opioid receptor subtypes in regulating accumbal acetylcholine efflux of freely moving rats using in vivo microdialysis. Other than naloxonazine, given intraperitoneally, delta- and mu-opioid receptor ligands were administered intracerebrally through the dialysis probe...
October 15, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27434299/best-practices-for-intrathecal-baclofen-therapy-troubleshooting
#19
REVIEW
Michael Saulino, David J Anderson, Jennifer Doble, Reza Farid, Fatma Gul, Peter Konrad, Aaron L Boster
INTRODUCTION: Troubleshooting helps optimize intrathecal baclofen (ITB) therapy in cases of underdose, overdose, and infection. METHODS: An expert panel of 21 multidisciplinary physicians currently managing >3200 ITB patients was convened, and using standard methodologies for guideline development, created an organized approach to troubleshooting ITB. They conducted a structured literature search that identified 263 peer-reviewed papers, and used results from an online survey of 42 physicians currently managing at least 25 ITB patients each...
August 2016: Neuromodulation: Journal of the International Neuromodulation Society
https://www.readbyqxmd.com/read/27426839/imaging-of-cerebral-%C3%AE-4%C3%AE-2-nicotinic-acetylcholine-receptors-with-18-f-flubatine-pet-implementation-of-bolus-plus-constant-infusion-and-sensitivity-to-acetylcholine-in-human-brain
#20
A T Hillmer, I Esterlis, J D Gallezot, F Bois, M Q Zheng, N Nabulsi, S F Lin, R L Papke, Y Huang, O Sabri, R E Carson, K P Cosgrove
The positron emission tomography (PET) radioligand (-)-[(18)F]flubatine is specific to α4β2(⁎) nicotinic acetylcholine receptors (nAChRs) and has promise for future investigation of the acetylcholine system in neuropathologies such as Alzheimer's disease, schizophrenia, and substance use disorders. The two goals of this work were to develop a simplified method for α4β2(⁎) nAChR quantification with bolus plus constant infusion (B/I) (-)-[(18)F]flubatine administration, and to assess the radioligand's sensitivity to acetylcholine fluctuations in humans...
November 1, 2016: NeuroImage
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