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Physostigmine

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https://www.readbyqxmd.com/read/28756934/postoperative-anticholinergic-poisoning-concealed-complications-of-a-commonly-used-medication
#1
Xiao Chi Zhang, Natalija Farrell, Thomas Haronian, Jason Hack
BACKGROUND: Scopolamine is a potent anticholinergic compound used commonly for the prevention of postoperative nausea and vomiting. Scopolamine can cause atypical anticholinergic syndromes due to its prominent central antimuscarinic effects. CASE REPORT: A 47-year-old female presented to the emergency department (ED) 20 h after hospital discharge for a right-knee meniscectomy, with altered mental status (AMS) and dystonic extremity movements that began 12 h after her procedure...
July 27, 2017: Journal of Emergency Medicine
https://www.readbyqxmd.com/read/28718647/fecl3-catalyzed-allylation-reactions-onto-3-hydroxy-2-oxindoles-formal-total-syntheses-of-bis-cyclotryptamine-alkaloids-%C3%A2-chimonanthine-and-%C3%A2-folicanthine
#2
Lakshmana K Kinthada, Sai Raghavendra Medisetty, Amarchand Parida, K Naresh Babu, Alakesh Bisai
An FeCl3-catalyzed efficient strategy for the allylation reactions of 3-hydroxy-2-oxindoles with allyltrimethylsilane has been developed. The reaction affords a variety of 2-oxindoles having quaternary center at the pseudobenzylic position in an operationally simple and inexpensive procedure. Control experiments using enantioenriched 3-hydroxy-2-oxindole show that the reaction proceeds through in situ generated 2H-indol-2-one (8). The methodology presents an efficient and concise access to the pyrroloindoline alkaloids (±)-deoxyeseroline (1a), (±)-esermethole (1b), (±)-physostigmine (1c), (±)-phenserine (1d), and (±)-physovenine (1e)...
August 7, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28703024/safety-and-effectiveness-of-physostigmine-a-10-year-retrospective-review
#3
Ann M Arens, Krishna Shah, Suad Al-Abri, Kent R Olson, Tom Kearney
BACKGROUND: Physostigmine has long been recognized as an antidote to reverse anticholinergic delirium. However, its effectiveness, safety profile, and dosing have been disputed. OBJECTIVES: To describe effectiveness, adverse events, and dosing associated with the use of physostigmine to reverse anticholinergic delirium. METHODS: A retrospective cohort study of hospitalized patients reported to a regional poison center system between 2003 and 2012 who received physostigmine to reverse an anticholinergic toxidrome...
July 13, 2017: Clinical Toxicology
https://www.readbyqxmd.com/read/28630263/determination-of-the-residues-in-the-extracellular-domain-of-the-nicotinic-%C3%AE-subunit-required-for-the-actions-of-physostigmine-on-neuronal-nicotinic-receptors
#4
Xiaochun Jin, Allison L Germann, Daniel J Shin, Gustav Akk, Joe Henry Steinbach
Physostigmine can potentiate and inhibit neuronal nicotinic receptors, in addition to inhibiting the activity of acetylcholinesterase. We found that receptors containing three copies of the α2 subunit are inhibited by low concentrations of physostigmine in contrast to receptors containing three copies of the α4 subunit that are potentiated. We exploited this observation to determine the regions required for the actions of physostigmine. Chimeric constructs of the α2 and α4 subunits located two regions in the extracellular amino-terminal domain of the subunit: the E loop (a loop of the transmitter-binding domain) and a region closer to the amino-terminus that collectively could completely determine the different effects of physostigmine...
September 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/28615883/clinicobiochemical-changes-in-ivermectin-toxicity-in-doberman-pinscher-pups
#5
Sahadeb Dey, Nitin P Kurade, Kishore Lal Khurana, Ananya Dan
This study is based on naturally intoxicated Doberman pinscher pups. Six Doberman pinscher pups were overdosed 50 times of recommended ivermectin dose by the pet owner and presented to Referral Veterinary Polyclinic section of this institute in a state of coma. The pups were unable to hold their head up and had no pupillary reflex. The pups were examined clinically and samples of blood were taken for haemato-biochemical studies, before and after treatment. During intoxication there was marked haemoconcentration, increase in values of serum creatinine phosphokinase, gamma glutamyl transpeptidase but decrease in serum glucose levels...
June 2017: Journal of Parasitic Diseases: Official Organ of the Indian Society for Parasitology
https://www.readbyqxmd.com/read/28571775/critical-role-of-ca1-muscarinic-receptors-on-memory-acquisition-deficit-induced-by-total-tsd-and-rem-sleep-deprivation-rsd
#6
Bibi-Zahra Javad-Moosavi, Gholamhassan Vaezi, Mohammad Nasehi, Seyed-Ali Haeri-Rouhani, Mohammad-Reza Zarrindast
AIM: Despite different theories regarding sleep physiological function, an overall census indicates that sleep is useful for neural plasticity which eventually strengthens cognition and brain performance. Different studies show that sleep deprivation (SD) leads to impaired learning and hippocampus dependent memory. According to some studies, cholinergic system plays an important role in sleep (particularly REM sleep), learning, memory, and its retrieval. So this study has been designed to investigate the effect of CA1 Cholinergic Muscarinic Receptors on memory acquisition deficit induced by total sleep deprivation (TSD) and REM sleep deprivation (RSD)...
May 30, 2017: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/28500787/corticosterone-primes-the-neuroinflammatory-response-to-gulf-war-illness-relevant-organophosphates-independently-of-acetylcholinesterase-inhibition
#7
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
#8
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...
June 25, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28445778/the-impact-of-bilateral-vagotomy-on-the-physostigmine-induced-airway-constriction-in-ferrets
#9
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...
August 2017: Respiratory Physiology & Neurobiology
https://www.readbyqxmd.com/read/28373858/enhanced-cholinergic-activity-improves-cerebral-blood-flow-during-orthostatic-stress
#10
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
#11
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-ach-receptors-contribute-to-modulation-of-depression-like-behaviour-in-c57bl-6j-mice
#12
Yann S Mineur, Tenna N Mose, Sam Blakeman, Marina R Picciotto
BACKGROUND AND PURPOSE: Clinical studies have identified links between cholinergic signalling and depression in human subjects. Increased cholinergic signalling in hippocampus also increases behaviours related to anxiety and depression in mice, which can be reversed by ACh receptor antagonists. EXPERIMENTAL APPROACH: As the α7 subunit of the nicotinic ACh receptor (nAChR) is highly expressed in hippocampus, we determined whether blocking α7 nAChRs could reverse the effects of increased ACh signalling in anxiety- and depression-related behaviours 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
#13
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
#14
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...
March 1, 2017: 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
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
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