Read by QxMD icon Read


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...
September 30, 2016: European Journal of Medicinal Chemistry
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
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
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...
August 10, 2016: Zeitschrift Für Naturforschung. C, A Journal of Biosciences
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
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
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
Bin-Bin Wang, Yi Xie, Fan-Chi Li, Min Ni, Kai-Zun Xu, Jiang-Hai Tian, Jing-Sheng Hu, Bin Xue, Wei-De Shen, Bing Li
The main mechanism of toxicity of organophosphate (OP) and carbamate (CB) insecticides is their irreversible binding and inhibition of acetylcholinestrase (AChE), encoded by ace1 (acetylcholinestrase gene 1), leading to eventual death of insects. Mutations in AChE may significantly reduce insects susceptibility to these pesticides. Bombyx mori is an important beneficial insect, and no OP- or CB-resistant strains have been generated. In this study, wild-type ace1 (wace1) and mutant ace1 (mace1) were introduced into BmN cells, confirmed by screening and identification...
October 2016: Archives of Insect Biochemistry and Physiology
Yunkyoung Lee, Bongkyu Lee, Sumin Jeong, Ji-Won Park, Inn-Oc Han, Chang-Joong Lee
Physostigmine, an acetylcholinesterase inhibitor, is known to affect the brain function in various aspects. This study was conducted to test whether physostigmine affects cell proliferation in the telencephalon of zebrafish. BrdU-labeled cells was prominently observed in the ventral zone of the ventral telencephalon of zebrafish. The increased number of BrdU- and proliferating cell nuclear antigen-labeled cells were shown in zebrafish treated with 200μM physostigmine, which was inhibited by pretreatment with 200μM scopolamine...
August 26, 2016: Neuroscience Letters
Kiran Bamel, Rajendra Gupta, Shirish C Gupta
We present experimental evidence to show that acetylcholine (ACh) causes decrease in shoot formation in leaf explants of tomato (Lycopersicon esculentum Miller var Pusa Ruby) when cultured on shoot regeneration medium. The optimum response was obtained at 10(-4) M ACh-enriched medium. ACh also causes decrease in percentage of cultures forming callus and reduces the callus mass. Inhibitors of enzymatic hydrolysis of ACh, neostigmine and physostigmine, also suppresses callogenesis and caulogenesis. On the other hand, the breakdown products of Ach, choline and acetate, do not alter the morphogenic response induced on the shoot regeneration medium...
June 2, 2016: Plant Signaling & Behavior
Fernando Tecles, Damián Escribano, Silvia Martínez-Miró, Fuensanta Hernández, María Dolores Contreras, José Joaquín Cerón
The purpose of this study was to measure and characterize the enzyme cholinesterase (ChE) in porcine saliva, as well as to evaluate its behavior in experimental stressful conditions. The results of ChE characterization by using different substrates and the selective inhibitors ethopropazine and physostigmine showed that the main enzyme existing in porcine saliva was butyrylcholinesterase (BChE). An automated assay using butyrylthiocholine iodide as substrate was validated providing adequate reproducibility, linearity results and limit of detection...
June 2016: Research in Veterinary Science
Fen Liu, Ning Zhao, Donghai Li, Zhenguo Zeng, Qiang Shao, Feifei Peng, Yan Wang, Kejian Qian
OBJECTIVE: To observe the effect of acetylcholine (ACh) on lipopolysaccharide (LPS) induced inflammatory model of rat alveolar macrophages, and to observe the effect of the acetylcholinesterase inhibitor physostigmine (Phy) on the anti-inflammatory effect of ACh. METHODS: The rat alveolar macrophages NR8383 were cultured in vitro, which were divided into five groups: blank control group, LPS group (stimulated with 1 mg/L LPS for 12 hours), LPS + ACh group (0.01, 0...
October 2015: Zhonghua Wei Zhong Bing Ji Jiu Yi Xue
Konstanze Plaschke, Markus A Weigand, Fabia Fricke, Jürgen Kopitz
OBJECTIVES: Surgical interventions can cause systemic postoperative inflammation, which in turn can induce neuroinflammation. A close link between immune reaction and cholinergic metabolism has been postulated. Pharmacological enhancement of cholinergic activity by administering physostigmine is known to induce protective effects. It is not known, however, whether physostigmine has an impact on postoperative inflammation and acetylcholine metabolism after a partial liver resection (PLR) surgery...
May 2016: Neurological Research
Majid Jafari-Sabet, Ali-Reza Jafari-Sabet, Ali Dizaji-Ghadim
The effects on tramadol state-dependent memory of bilateral intradorsal hippocampal (intra-CA1) injections of physostigmine, an acetylcholinesterase inhibitor, and atropine, a muscarinic acetylcholine receptor antagonist, were examined in adult male NMRI mice. A single-trial step-down passive avoidance task was used for the assessment of memory retention. Post-training intra-CA1 administration of an atypical μ-opioid receptor agonist, tramadol (0.5 and 1 μg/mouse), dose dependently impaired memory retention...
August 2016: Behavioural Pharmacology
B B Wang, F C Li, K Z Xu, M Ni, J S Hu, J H Tian, Y Y Li, W D Shen, B Li
AChE is the target of organophosphate (OP) and carbamate (CB) pesticides, and mutations in the gene can significantly reduce insects' sensitivity to these pesticides. Bombyx mori is highly sensitive to pesticides. To investigate the effects of mutations on AChE1 structure and function, we used a prokaryotic system to express B.mori wild type AChE1 (wAChE1) and mutant AChE1 (mAChE1) in this study. Active AChE1 proteins were obtained after refolding and purification, and wAChE1 and mAChE1 had similar activities...
May 2016: Pesticide Biochemistry and Physiology
Jonathan D Kenny, Jessica J Chemali, Joseph F Cotten, Christa J Van Dort, Seong-Eun Kim, Demba Ba, Norman E Taylor, Emery N Brown, Ken Solt
BACKGROUND: Although emergence from general anesthesia is clinically treated as a passive process driven by the pharmacokinetics of drug clearance, agents that hasten recovery from general anesthesia may be useful for treating delayed emergence, emergence delirium, and postoperative cognitive dysfunction. Activation of central monoaminergic neurotransmission with methylphenidate has been shown to induce reanimation (active emergence) from general anesthesia. Cholinergic neurons in the brainstem and basal forebrain are also known to promote arousal...
March 17, 2016: Anesthesia and Analgesia
Emily L Spaulding, James N Sleigh, Kathryn H Morelli, Martin J Pinter, Robert W Burgess, Kevin L Seburn
UNLABELLED: Patients with Charcot-Marie-Tooth Type 2D (CMT2D), caused by dominant mutations in Glycl tRNA synthetase (GARS), present with progressive weakness, consistently in the hands, but often in the feet also. Electromyography shows denervation, and patients often report that early symptoms include cramps brought on by cold or exertion. Based on reported clinical observations, and studies of mouse models of CMT2D, we sought to determine whether weakened synaptic transmission at the neuromuscular junction (NMJ) is an aspect of CMT2D...
March 16, 2016: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
Keri M Small, Eric Nunes, Shannon Hughley, Nii A Addy
Cholinergic and dopaminergic mechanisms within the mesolimbic dopamine system are suggested to play a role in the manifestation of depression and anxiety-related disorders. However, despite the fact that cholinergic mechanisms in the ventral tegmental area (VTA) highly regulate dopamine activity, the role of VTA cholinergic mechanisms in depression-related behaviors is relatively unknown. Here we sought to determine whether enhancing cholinergic tone in the VTA would alter depression and anxiety-related behavior in the forced swim test (FST), elevated plus maze (EPM) and sucrose preference test (SPT)...
March 11, 2016: Neuroscience Letters
Diane I Bitzinger, Michael Gruber, Simon Tümmler, Bernhard Michels, Anika Bundscherer, Susanne Hopf, Benedikt Trabold, Bernhard M Graf, York A Zausig
Previous and more recent studies show that cholinesterase inhibitors (ChE-Is) are an important possibility for therapeutic intervention in Alzheimer's Disease, sepsis and other inflammatory syndromes. ChE-Is maintain high levels of acetylcholine (ACh) determining beneficial effects on the disease process. Despite numerous efforts to identify the appropriate choice of agents and dose of ChE-Is, a common protocol regarding concentration- and species-dependent differences in inhibitory potency (IC 50) of clinical relevant ChE-Is is still not available...
October 2016: Neuropharmacology
Arjun Acharya, Devendar Anumandla, Christopher S Jeffrey
A regioselective dearomative aza-(3 + 2) cycloaddition reaction of substituted indoles with α-halohydroxamates has been developed. This transformation provides rapid access to highly functionalized pyrroloindolines that are represented in large number of bioactive compounds. The natural product, physostigmine, has been concisely synthesized utilizing this method.
December 2, 2015: Journal of the American Chemical Society
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"