4,092 results match your criteria Toxicity Anticholinergic


Efficient detoxification of nerve agents by oxime-assisted reactivation of acetylcholinesterase mutants.

Neuropharmacology 2020 Apr 22;171:108111. Epub 2020 Apr 22.

Institute for Medical Research and Occupational Health, Ksaverska cesta 2, HR-10001, Zagreb, Croatia.

The recent advancements in crystallography and kinetics studies involving reactivation mechanism of acetylcholinesterase (AChE) inhibited by nerve agents have enabled a new paradigm in the search for potent medical countermeasures in case of nerve agents exposure. Poisonings by organophosphorus compounds (OP) that lead to life-threatening toxic manifestations require immediate treatment that combines administration of anticholinergic drugs and an aldoxime as a reactivator of AChE. An alternative approach to reduce the in vivo toxicity of OP centers on the use of bioscavengers against the parent organophosphate. Read More

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http://dx.doi.org/10.1016/j.neuropharm.2020.108111DOI Listing

Contribution of cholinergic system and Nrf2/HO-1 signaling to the anti-amnesic action of 7-fluoro-1,3-diphenylisoquinoline-1-amine in mice.

Chem Biol Interact 2020 Feb 27;317:108959. Epub 2020 Jan 27.

Laboratório de Síntese, Reatividade e Avaliação Farmacológica e Toxicológica de Organocalcogênios, Centro de Ciências Naturais e Exatas, Departamento de Bioquímica e Biologia Molecular, Universidade Federal de Santa Maria, Santa Maria, CEP 97105-900, RS, Brazil. Electronic address:

The isoquinoline 7-fluoro-1,3-diphenylisoquinoline-1-amine (FDPI) has been studied due to its multitarget properties, such as modulation of GABAergic and glutamatergic systems, antioxidant, and anti-inflammatory. This study investigated the contribution of oxidative stress, nuclear factor (erythroid-derived 2)-like 2 (Nrf2)/heme oxygenase (HO-1) signaling, and the cholinergic system to the anti-amnesic action of FDPI in mice. Adult male Swiss mice received FDPI for 5 days (5-25 mg/kg, i. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.108959DOI Listing
February 2020

Highly durable crack sensor integrated with silicone rubber cantilever for measuring cardiac contractility.

Nat Commun 2020 Jan 27;11(1):535. Epub 2020 Jan 27.

MEMS and Nanotechnology Laboratory, School of Mechanical Systems Engineering, Chonnam National University, Gwangju, 61186, Republic of Korea.

To date, numerous biosensing platforms have been developed for assessing drug-induced cardiac toxicity by measuring the change in contractile force of cardiomyocytes. However, these low sensitivity, low-throughput, and time-consuming processes are severely limited in their real-time applications. Here, we propose a cantilever device integrated with a polydimethylsiloxane (PDMS)-encapsulated crack sensor to measure cardiac contractility. Read More

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http://dx.doi.org/10.1038/s41467-019-14019-yDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6985253PMC
January 2020
10.742 Impact Factor

Solanum vegetable-based diets improve impairments in memory, redox imbalance, and altered critical enzyme activities in Drosophila melanogaster model of neurodegeneration.

J Food Biochem 2020 Jan 16:e13150. Epub 2020 Jan 16.

Faculty of Pharmacy, Department of Pharmacognosy, Anadolu University, Eskişehir, Turkey.

The effects of two Solanum vegetables, S. macrocarpon L. (African eggplant), and S. Read More

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http://dx.doi.org/10.1111/jfbc.13150DOI Listing
January 2020

Evaluation of high-affinity phenyltetrahydroisoquinoline aldoximes, linked through anti-triazoles, as reactivators of phosphylated cholinesterases.

Toxicol Lett 2020 Mar 19;321:83-89. Epub 2019 Dec 19.

Institute for Medical Research and Occupational Health, HR-10000 Zagreb, Croatia. Electronic address:

Acetylcholinesterase (AChE) is a pivotal enzyme in neurotransmission. Its inhibition leads to cholinergic crises and could ultimately result in death. A related enzyme, butyrylcholinesterase (BChE), may act in the CNS as a co-regulator in terminating nerve impulses and is a natural plasma scavenger upon exposure to organophosphate (OP) nerve agents that irreversibly inhibit both enzymes. Read More

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http://dx.doi.org/10.1016/j.toxlet.2019.12.016DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7053431PMC

The effects and mechanisms of the action of galangin on spatial memory in rats.

Bratisl Lek Listy 2019 ;120(12):881-886

Background: Galangin, a flavonoid compound with acetylcholinesterase inhibitory activity, may improve cognitive functions by enhancing cholinergic transmission.

Objectives: We aimed to investigate the effects of galangin on spatial memory impairment in rats.

Methods: The effects of galangin (50 and 100 mg/kg) and reference anti-dementia drug donepezil (1mg/kg) administrations were examined on memory impairment induced by the muscarinic cholinergic receptor antagonist scopolamine or the nicotinic cholinergic receptor antagonist mecamylamine in the Morris water maze (MWM) test. Read More

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http://dx.doi.org/10.4149/BLL_2019_148DOI Listing
December 2019

Design, synthesis and biological Evaluation of Dual acetyl cholinesterase and beta-secretase inhibitors in treatment for alzheimer's Disease.

Pak J Pharm Sci 2019 Sep;32(5):2091-2098

Department of Pharmaceutical Engineering, College of Chemistry and Chemical Engineering, Central South University, Changsha, PR China.

With the recent research advances in molecular biology and technology multiple credible hypotheses about the progress of Alzheimer's disease (AD) have been proposed, among which the amyloid and cholinergic hypotheses are commonly used to develop reliable therapeutic agents. The multitarget-directed ligand (MTDL) approach was taken in this work to develop muilti-functional agents, which can mainly serve as dual beta-secretase (BACE 1) and Acetylcholinesterase (AChE) inhibitors. Series of new compounds were designed, synthesized and evaluated in this work, from which we identified 2-((4-(1,3-dioxoisoindolin-2-yl)benzyl)amino)-2-oxoethyl-2-(4-methoxyphenyl)acetate (1h) as a new dual cholinesterase and beta-secretase inhibitor without toxicity. Read More

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September 2019

Clinical effects from household insecticide: pyrethroid or organophosphate toxicity?

BMJ Case Rep 2019 Nov 21;12(11). Epub 2019 Nov 21.

David Geffen School of Medicine, Los Angeles, California, USA.

A 54-year-old man with a history of schizophrenia presented to the emergency room for weakness with associated lacrimosis, drooling, nausea, emesis, diarrhoea, diplopia and burning sensation on his skin that began 6 hours after spraying five cans of Raid on his carpet. He was noted to have miotic pupils and hyperactive bowel sounds. Given the clinical presentation, the patient was diagnosed with organophosphate (OP) toxicity. Read More

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http://dx.doi.org/10.1136/bcr-2019-230966DOI Listing
November 2019

The psychopharmacology of primary and metastatic brain tumors and paraneoplastic syndromes.

Handb Clin Neurol 2019 ;165:269-283

Department of Psychiatry, St. John's Episcopal Hospital, New York, NY, United States.

Brain tumors and paraneoplastic syndromes can cause various neuropsychiatric symptoms. Rarely, psychiatric symptoms may be the initial presentation of the underlying neurologic lesion. Brain imaging studies are crucial in the diagnosis of brain tumors. Read More

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http://dx.doi.org/10.1016/B978-0-444-64012-3.00016-2DOI Listing

Unknowing ingestion of Brugmansia suaveolens leaves presenting with signs of anticholinergic toxicity: a case report.

J Med Case Rep 2019 Oct 30;13(1):322. Epub 2019 Oct 30.

Sri Jayawardenepura General Hospital, Sri Jayawardenepura Kotte, Sri Lanka.

Background: Brugmansia suaveolens is the commonest species under the Solanacea ("Angels Trumpet" in English; "Attana" in Sinhalese) plant family in Sri Lanka. It contains alkaloids like scopolamine, atropine and hyoscyamine which can cause an anticholinergic toxindrome. There have been a few reported cases of accidental ingestion of Brugmansia seeds among children, seeds being the most toxic part, but no such reported cases of Brugmansia leaves poisoning among adults. Read More

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http://dx.doi.org/10.1186/s13256-019-2250-1DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6819485PMC
October 2019

Local and generalized sensitization of thermally evoked defensive behavior in caterpillars.

J Comp Neurol 2020 Apr 31;528(5):805-815. Epub 2019 Oct 31.

Department of Biology, Tufts University, Medford, Massachusetts.

In addition to camouflage and chemical toxicity, many caterpillars defend themselves against predators with sudden sharp movements. For smaller species, these movements propel the body away from the threat, but in larger caterpillars, such as the tobacco hornworm, Manduca sexta, the movement is a defensive strike targeted to a noxious stimulus on the abdomen. Previously, strikes have been studied using mechanical stimulation like poking or pinching the insect, but such stimuli are hard to control. Read More

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http://dx.doi.org/10.1002/cne.24797DOI Listing

Encapsulation of Neurotoxins, Blockers of Nicotinic Acetylcholine Receptors, in Nanomaterials Based on Sulfated Polysaccharides.

Dokl Biochem Biophys 2019 Jul 26;487(1):251-255. Epub 2019 Sep 26.

Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, 117997, Moscow, Russia.

Three-finger snake neurotoxins are selective antagonists of some nicotinic acetylcholine receptor subtypes and are widely used to study these receptors. The peptide neurotoxin azemiopsin, recently isolated from the venom of Azemipos feae, is a selective blocker of muscle-type nicotinic acetylcholine receptor. In order to reduce their toxicity and increase resistance under physiological conditions, we have encapsulated these toxins into nanomaterials. Read More

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http://dx.doi.org/10.1134/S1607672919040021DOI Listing
July 2019
1 Read

Deduction of Novel Genes Potentially Involved in the Effects of Very Low Dose Atropine (0.003%) Treatment on Corneal Epithelial Cells Using Next-Generation Sequencing and Bioinformatics Approaches.

Medicina (Kaunas) 2019 Sep 13;55(9). Epub 2019 Sep 13.

Graduate Institute of Clinical Medicine, College of Medicine, Kaohsiung Medical University, Kaohsiung 807, Taiwan.

Atropine is a nonselective muscarinic antagonist which has been used to prevent worsening of myopia in children. Different concentrations of atropine were used for myopia, ranging from 0.01% to 1. Read More

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http://dx.doi.org/10.3390/medicina55090589DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6780702PMC
September 2019

Clothianidin, a neonicotinoid insecticide, activates α4β2, α7 and muscarinic receptors to induce in vivo dopamine release from rat striatum.

Toxicology 2019 10 31;426:152285. Epub 2019 Aug 31.

Department of Functional Biology and Health Science, University of Vigo, Spain.

Clothianidin (CLO) is a neonicotinoid insecticide that produces toxic effects in experimental animals and humans. These effects are associated primarily to its action as a nicotinic agonist, acting on insect and vertebrate nicotinic acetylcholine receptors (nAChRs), but little is known about the mechanisms of action on the mammalian nervous system. In the rat striatum, CLO induces increases in the dopamine overflow in a concentration-dependent manner. Read More

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http://dx.doi.org/10.1016/j.tox.2019.152285DOI Listing
October 2019
1 Read

Penehyclidine hydrochloride defends against LPS-induced ALI in rats by mitigating endoplasmic reticulum stress and promoting the Hes1/Notch1 pathway.

Gene 2019 Dec 30;721:144095. Epub 2019 Aug 30.

Department of Critical Care Medicine, The Affiliated Hospital of Putian University, Putian 351100, China. Electronic address:

Penehyclidine hydrochloride (PHC) is a novel anticholinergic drug applied broadly in surgeries as a preanesthetic medication. A substantial amount of research indicates that PHC has lung defensive properties. Considering that endoplasmic reticulum (ER) stress exerts a crucial function in cell apoptosis associated with the lipopolysaccharides (LPS)-induced acute lung injury (ALI) model, we aimed to determine whether regulation of ER stress in the LPS-induced ALI model was associated with the lung defensive role of PHC. Read More

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http://dx.doi.org/10.1016/j.gene.2019.144095DOI Listing
December 2019
1 Read

Is Combining an Anticholinergic with a Cholinesterase Inhibitor a Good Strategy for High-Level CNS Cholinesterase Inhibition?

Authors:
Donald E Moss

J Alzheimers Dis 2019 ;71(4):1099-1103

Department of Psychology, University of Texas at El Paso, El Paso, TX, USA.

The currently approved cholinesterase inhibitors (donepezil, rivastigmine, and galantamine) produce gastrointestinal toxicity which limits dosing to that which produces only about 25% to 35% CNS cholinesterase inhibition in Alzheimer's disease patients undergoing treatment, below the minimum therapeutic target of about 40% to 50% CNS inhibition considered necessary to treat cognitive impairment. A recent strategy for producing high-level CNS acetylcholinesterase (AChE) inhibition (50% or higher) is to co-administer a muscarinic anticholinergic with the AChE inhibitor to block the dose-limiting cholinergic overstimulation of the gastrointestinal system, allow more robust AChE inhibition in the CNS, and improve efficacy in the treatment of Alzheimer's disease. Unfortunately, most common muscarinic anticholinergics, including solifenacin, readily penetrate the CNS and are directly associated with long-term exacerbation of the underlying neuropathology of Alzheimer's disease and increased brain atrophy. Read More

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http://dx.doi.org/10.3233/JAD-190626DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6839449PMC
January 2019

Antinociceptive Activity of Petroleum Ether Fraction of Leaves Methanolic Extract: Roles of Nonopioid Pain Modulatory Systems and Potassium Channels.

Biomed Res Int 2019 5;2019:6593125. Epub 2019 Aug 5.

Integrative Pharmacogenomics Institute (iPROMISE), Level 7, FF3, Faculty of Pharmacy, Universiti Teknologi MARA, Puncak Alam Campus, 42300 Bandar Puncak Alam, Selangor, Malaysia.

Methanolic extract of Lindau leaves (MECN) has been reported to exert antinociceptive activity. The present study aimed to elucidate the possible antinociceptive mechanisms of a lipid-soluble fraction of MECN, which was obtained after sequential extraction in petroleum ether. The petroleum ether fraction of (PECN), administered orally to mice, was (i) subjected to capsaicin-, glutamate-, phorbol 12-myristate 13-acetate-, bradykinin-induced nociception model; (ii) prechallenged (intraperitoneal (i. Read More

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http://dx.doi.org/10.1155/2019/6593125DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6699298PMC
January 2020

Rational polytherapy in the treatment of cholinergic seizures.

Neurobiol Dis 2020 01 24;133:104537. Epub 2019 Aug 24.

Department of Neurology, David Geffen School of Medicine at UCLA, Los Angeles, CA, USA; Epilepsy Research Laboratory (151), Veterans Affairs Greater Los Angeles Healthcare System, Los Angeles, CA, USA; Brain Research Institute, David Geffen School of Medicine at UCLA, Los Angeles, CA., USA. Electronic address:

The initiation and maintenance phases of cholinergic status epilepticus (SE) are associated with maladaptive trafficking of synaptic GABA and glutamate receptors. The resulting pharmacoresistance reflects a decrease in synaptic GABA receptors and increase in NMDA and AMPA receptors, which tilt the balance between inhibition and excitation in favor of the latter. If these changes are important to the pathophysiology of SE, both should be treated, and blocking their consequences should have therapeutic potential. Read More

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http://dx.doi.org/10.1016/j.nbd.2019.104537DOI Listing
January 2020
7 Reads

Elucidation of the possible mechanism of analgesic action of methanol stem bark extract of Uapaca togoensis pax in mice.

J Ethnopharmacol 2019 Dec 12;245:112156. Epub 2019 Aug 12.

Department of Pharmacology and Therapeutics, Faculty of Medicine, Kogi State University, Anyigba, Nigeria.

Ethnopharmacological Relevance: Uapaca togoensis is a medicinal plant used traditionally in Africa for the treatment of rheumatism, epilepsy, cough, pneumonia, vomitting and fever. Previously, the analgesic activity of its methanol stem bark extract has been scientifically demonstrated. However, the mechanism responsible for this activity remains to be investigated. Read More

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http://dx.doi.org/10.1016/j.jep.2019.112156DOI Listing
December 2019

Ocular surface histopathological insult following sarin and VX exposure and potential treatments in the rat model.

Toxicol Lett 2019 Oct 10;314:153-163. Epub 2019 Aug 10.

Dept. Of Pharmacology, Israel Institute for Biological Research, Ness Ziona, 74100, Israel.

Eye exposure to organophosphate (OP) chemical warfare irreversible acetylcholinesterase inhibitors, results in long-term miosis and impaired visual function. In contrast to the well-documented miotic and ciliary muscle spasm observed following chemical warfare, OP ocular exposure, little is known regarding the ocular surface histopathological insult. The aim of the present study was to determine the degree of the ocular surface insult following sarin or VX ocular exposure and to evaluate potential anti-cholinergic treatments in counteracting this insult. Read More

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http://dx.doi.org/10.1016/j.toxlet.2019.08.002DOI Listing
October 2019
3 Reads

Sagas of the Solanaceae: Speculative ethnobotanical perspectives on the Norse berserkers.

Authors:
Karsten Fatur

J Ethnopharmacol 2019 Nov 9;244:112151. Epub 2019 Aug 9.

University of Ljubljana, Faculty of Pharmacy, 32 Tržaška Cesta, 1000, Ljubljana, Slovenia. Electronic address:

Ethnopharmacological Relevance: The Norse berserkers were wild warriors of Scandinavia known to enter a trance-like state that allowed them to fight with increased strength and a rage that granted them immunity to many forms of harm in battle. Though many theories have been advanced as to the cause of this state, the most widely believed is that the intoxicating mushroom Amanita muscaria was used.

Aim Of The Study: The following article underlines the issues with this theory and provides an alternate intoxicant that fits with the reports of berserker behaviour much better: Hyoscyamus niger. Read More

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http://dx.doi.org/10.1016/j.jep.2019.112151DOI Listing
November 2019
1 Read

Atropine toxicity caused by erroneous intranasal administration in a pediatric patient: case report.

Ann Saudi Med 2019 Jul-Aug;39(4):279-282. Epub 2019 Aug 5.

From the Department of Surgery, Division of Otorhinolaryngology-Head and Neck Surgery, King Abdulaziz Medical City, Riyadh, Saudi Arabia.

A 28-month-old boy mistakenly received intranasal atropine sulfate instead of Otrivin (xylometazoline hydrochloride) for the treatment of adenoid hypertrophy. Later on, he came to the emergency department with anticholinergic manifestations after the administration of multiple drops. The child presented with a tonic-clonic seizure lasting for a few minutes, followed by a brief loss of consciousness, vomiting, agitation, and irritability, all of which were stabilized by a dose of intravenous lorazepam. Read More

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http://dx.doi.org/10.5144/0256-4947.2019.279DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6838643PMC
January 2020
2 Reads

Pinnatoxins' Deleterious Effects on Cholinergic Networks: From Experimental Models to Human Health.

Mar Drugs 2019 Jul 20;17(7). Epub 2019 Jul 20.

Mitochondrial and Cardiovascular Pathophysiology (MITOVASC), Cardiovascular Mechanotransduction, UMR CNRS 6015, INSERM U1083, Angers University, 49045 Angers, France.

Pinnatoxins (PnTXs) are emerging neurotoxins that were discovered about 30 years ago. They are solely produced by the marine dinoflagellate , and may be transferred into the food chain, as they have been found in various marine invertebrates, including bivalves. No human intoxication has been reported to date although acute toxicity was induced by PnTxs in rodents. Read More

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http://dx.doi.org/10.3390/md17070425DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6669724PMC
July 2019
10 Reads

Linking cholinesterase inhibition with behavioural changes in the sea snail Gibbula umbilicalis: Effects of the organophosphate pesticide chlorpyrifos.

Comp Biochem Physiol C Toxicol Pharmacol 2019 Nov 12;225:108570. Epub 2019 Jul 12.

MARE - Marine and Environmental Sciences Centre, ESTM, Instituto Politécnico de Leiria, 2520-641 Peniche, Portugal.

Inhibition of acetylcholinesterase (AChE) activity has been widely used to assess the exposure and effects of anticholinergic environmental contaminants in several species. The aim of this study was to investigate if sublethal concentrations of the organophosphorous pesticide chlorpyrifos (CPF), a well-known AChE inhibitor, would also affect cholinesterases (ChE) in Gibbula umbilicalis and if this inhibition would result in an alteration of its behaviour, in an attempt to link the effects observed at the cellular level with effects at higher levels of ecological relevance. The biochemical properties of ChEs in this species were first characterized through the assessment of different enzymatic forms present in the sea snail, using different substrates and selective inhibitors. Read More

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http://dx.doi.org/10.1016/j.cbpc.2019.108570DOI Listing
November 2019

Ameliorative effect of deoxyvasicine on scopolamine-induced cognitive dysfunction by restoration of cholinergic function in mice.

Phytomedicine 2019 Oct 2;63:153007. Epub 2019 Jul 2.

Institute of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine; The MOE Key Laboratory for Standardization of Chinese Medicines and The SATCM Key Laboratory for New Resources and Quality Evaluation of Chinese Medicine, 1200 Cailun Rood, Shanghai 201203, China; Shanghai R&D Centre for Standardization of Chinese Medicines, 1200 Cailun Rood, Shanghai 201203, China. Electronic address:

Background: Aerial parts of Peganum harmala Linn is used as a traditional medical herb for treatment of amnesia in Uighur medicine in China. Deoxyvasicine (DVAS) is one of the chief active ingredients in P. harmala, it possesses strong acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities in vitro, but the therapeutic effect and mechanisms on amnesia in vivo are unclear. Read More

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http://dx.doi.org/10.1016/j.phymed.2019.153007DOI Listing
October 2019
9 Reads

Reduced systemic exposure and brain uptake of donepezil in rats with scopolamine-induced cognitive impairment.

Xenobiotica 2020 Apr 1;50(4):389-400. Epub 2019 Aug 1.

School of Pharmacy, Faculty of Medicine, The Chinese University of Hong Kong, Shatin, Hong Kong SAR.

1. Donepezil (DPZ) is an acetylcholinesterase (AchE) inhibitor used in the mild to moderately severe Alzheimer's disease. Among its major metabolites, 6--desmethyl DPZ (6-DDPZ), 5--desmethyl DPZ (5-DDPZ) and DPZ -oxide, the anti-AchE activities of 5-DDPZ and DPZ -oxide have never been clearly identified before. Read More

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http://dx.doi.org/10.1080/00498254.2019.1643514DOI Listing
April 2020
1 Read

Effect of Fast-Disintegrating Tablets' Characteristics on the Sublingual Permeability of Atropine Sulfate for the Potential Treatment of Organophosphates Toxicity.

AAPS PharmSciTech 2019 Jun 21;20(6):229. Epub 2019 Jun 21.

College of Pharmacy, Nova Southeastern University, 3200 South University Drive, Fort Lauderdale, Florida, 33328, USA.

Atropine sulfate (AS) fast-disintegrating sublingual tablets (FDSTs) were tested for AS sublingual permeation's feasibility as a potential alternative dosage form to treat organophosphates (OP) toxicity. More than 12,000 OP pesticide toxicity cases were reported in the USA from 2011 to 2014. AS is the recommended antidote for OP toxicity; however, it is only available as an ATROPEN® auto-injector, an IM injection, for self-administration, which is associated with several drawbacks and limitations. Read More

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http://dx.doi.org/10.1208/s12249-019-1420-1DOI Listing
June 2019
21 Reads

Investigation of comet assays under conditions mimicking ocular instillation administration in a three-dimensional reconstructed human corneal epithelial model.

Cutan Ocul Toxicol 2019 Dec 8;38(4):375-383. Epub 2019 Jul 8.

Research and Development Division, Senju Pharmaceutical Co., Ltd , Kobe , Hyogo , Japan.

A comet assay is one of the genotoxicity methods for evaluating the potential of chemicals to induce DNA strand breaks. To investigate the usefulness of comet assays for evaluating the genotoxic potential of ophthalmic solutions, a three-dimensional (3D) reconstructed human corneal epithelial model (3D corneal model) was exposed to conditions mimicking topical ocular instillation administration. The 3D corneal model was exposed to acridine orange, ethidium bromide, hydrogen peroxide, 1,1'-dimethyl-4,4'-bipyridinium dichloride (paraquat), 4-nitroquinoline 1-oxide (4-NQO), acrylamide and methyl methanesulfonate (MMS). Read More

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http://dx.doi.org/10.1080/15569527.2019.1634580DOI Listing
December 2019
10 Reads

Mode of action of sulfoxaflor on α-bungarotoxin-insensitive nAChR1 and nAChR2 subtypes: Inhibitory effect of imidacloprid.

Neurotoxicology 2019 09 15;74:132-138. Epub 2019 Jun 15.

LBLGC USC INRA 1328, Université d'Orléans, 1 rue de Chartres, 45067 Orléans, France. Electronic address:

Cockroach neurosecretory cells, dorsal unpaired median (DUM) neurons, express two distinct α-bungarotoxin-insensitive nicotinic acetylcholine receptor subtypes, nAChR1 and nAChR2 which are differently sensitive to the neonicotinoid insecticides and intracellular calcium pathways. The aim of this study is to determine whether sulfoxaflor acts as an agonist of nAChR1 and nAChR2 subtypes. We demonstrated that 1 mM sulfoxaflor induced high current amplitudes, compared to acetylcholine, suggesting that it was a full agonist of DUM neuron nAChR subtypes. Read More

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http://dx.doi.org/10.1016/j.neuro.2019.06.003DOI Listing
September 2019

Dichloroacetate-induced peripheral neuropathy.

Int Rev Neurobiol 2019 11;145:211-238. Epub 2019 Jun 11.

Department of Pathology, University of California San Diego, La Jolla, CA, United States.

Dichloroacetate (DCA) has been the focus of research by both environmental toxicologists and biomedical scientists for over 50 years. As a product of water chlorination and a metabolite of certain industrial chemicals, DCA is ubiquitous in our biosphere at low μg/kg body weight daily exposure levels without obvious adverse effects in humans. As an investigational drug for numerous congenital and acquired diseases, DCA is administered orally or parenterally, usually at doses of 10-50mg/kg per day. Read More

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http://dx.doi.org/10.1016/bs.irn.2019.05.003DOI Listing
January 2020
5 Reads

Pyrene-based prospective biomaterial: In vitro bioimaging, protein binding studies and detection of bilirubin and Fe.

Spectrochim Acta A Mol Biomol Spectrosc 2019 Oct 22;221:117150. Epub 2019 May 22.

Department of Chemistry, Vel Tech Rangarajan Dr Sagunthala R & D Institute of Science and Technology, Avadi, Chennai 600 062, Tamil Nadu, India. Electronic address:

Herein, we have meticulously derived the nanosized fluorescent aggregates from pyrene Schiff base (PS) in DMSO:water (10:90) ratio. The aggregation property of PS molecule was characterized by SEM and TEM measurements, revealed the aggregated particles are in spherical shape with ~3 nm in size. Moreover, aggregates exhibit a high fluorescence quantum yield (48%) which was effectively used for the in vitro bioimaging of two different cancer cells such as A549 and MCF-7 cells in which it exhibiting excellent biocompatibility. Read More

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http://dx.doi.org/10.1016/j.saa.2019.117150DOI Listing
October 2019
8 Reads

Neuroprotective Effects of Red Ginseng Saponins in Scopolamine-Treated Rats and Activity Screening Based on Pharmacokinetics.

Molecules 2019 Jun 6;24(11). Epub 2019 Jun 6.

Institute of Special Wild Economic Animals and Plants, Chinese Academy of Agriculture Sciences, Changchun 130112, China.

Ginseng has been used to alleviate age-related dementia and memory deterioration for thousands of years. This study investigated the protective effect of red ginseng saponins against scopolamine-induced cerebral injury. Meanwhile, pharmacokinetics of ginsenosides in normal and scopolamine-treated rats were compared. Read More

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http://dx.doi.org/10.3390/molecules24112136DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6600263PMC
June 2019
16 Reads

Development of the "hidden" multifunctional agents for Alzheimer's disease.

Eur J Med Chem 2019 Sep 27;177:247-258. Epub 2019 May 27.

Key Laboratory of Neuropsychiatric Drug Research of Zhejiang Province, Institute of Materia Medica, Zhejiang Academy of Medical Sciences, Hangzhou, 310013, PR China. Electronic address:

Alzheimer's disease (AD) is a chronic, fatal and complex neurodegenerative disorder, which is characterized by cholinergic system dysregulation, metal dyshomeostasis, amyloid-β (Aβ) aggregation, etc. Therefore in most cases, single-target or single-functional agents are insufficient to achieve the desirable effect against AD. Multi-Target-Directed Ligand (MTDL), which is rationally designed to simultaneously hit multiple targets to improve the pharmacological profiles, has been developed as a promising approach for drug discovery against AD. Read More

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http://dx.doi.org/10.1016/j.ejmech.2019.05.051DOI Listing
September 2019
25 Reads
3.447 Impact Factor

Prophylactic NS-21 maintains the skin moisture but does not reduce the severity of radiation dermatitis in patients with head and neck cancer: a randomized control trial.

Radiat Oncol 2019 May 30;14(1):90. Epub 2019 May 30.

Division of Radiation Oncology, Department of Radiology, Far Eastern Memorial Hospital, 21 Sec 2, Nanya S Road, Banciao District, New Taipei City, 220, Taiwan.

Background: To evaluate the practicality of NS-21 cream with regard to its skin-related toxicity in patients with head and neck cancer (HNC) who are undergoing concurrent chemoradiation therapy (CCRT) or radiotherapy (RT).

Methods: Between July 2015 and November 2017, 30 HNC patients who underwent RT or CCRT were randomly allocated to receive either NS-21 or control treatment on their irradiated skin three times per day, starting at the initiation of RT or CCRT and ending 2 weeks after the completion of RT or until the appearance of grade 3 acute radiation dermatitis (ARD). Dermatitis was recorded weekly according to the Common Terminology Criteria for Adverse Events (CTCAE) version 4. Read More

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http://dx.doi.org/10.1186/s13014-019-1302-4DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6543645PMC
May 2019
1 Read

Evaluation of the Memory Enhancing Activity of Dichloromethane Fraction of the Methanolic Extract of Pycnanthus angolensis Stem Bark on Experimental Models of Memory Impairment.

Drug Res (Stuttg) 2019 Oct 29;69(10):551-558. Epub 2019 May 29.

Neuropharmacology Unit, Department of Pharmacology and Therapeutics, Faculty of Basic Medical Sciences, College of Medicine, University of Ibadan, Ibadan, Nigeria.

(Welw) Warb., Myristicaceae, is used extensively in ethnomedicine. Numerous health benefits have been ascribed to the use of different parts of including its role in cognitive function and inflammatory conditions. Read More

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http://dx.doi.org/10.1055/a-0875-3631DOI Listing
October 2019
1 Read

Retrograde activation of CB1R by muscarinic receptors protects against central organophosphorus toxicity.

Neuropharmacology 2019 09 24;155:113-120. Epub 2019 May 24.

Department of Neuroscience, United States Army Medical Research Institute of Chemical Defense, 2900 Ricketts Point Road, Gunpowder, MD, 21010, USA. Electronic address:

The acute toxicity of organophosphorus-based compounds is primarily a result of acetylcholinesterase inhibition in the central and peripheral nervous systems. The resulting cholinergic crisis manifests as seizure, paralysis, respiratory failure and neurotoxicity. Though overstimulation of muscarinic receptors is the mechanistic basis of central organophosphorus (OP) toxicities, short-term changes in synapse physiology that precede OP-induced seizures have not been investigated in detail. Read More

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http://dx.doi.org/10.1016/j.neuropharm.2019.05.028DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6588469PMC
September 2019
11 Reads
5.106 Impact Factor

Time dependent dual effect of anti-inflammatory treatments on sarin-induced brain inflammation: Suggested role of prostaglandins.

Neurotoxicology 2019 09 13;74:19-27. Epub 2019 May 13.

Israel Institute for Biological Research, Israel.

A common consequence of exposure to organophosphate nerve agents is the centrally mediated seizure activity that appears even after conventional treatment with atropine and oximes. We have previously demonstrated a major inflammatory response with subsequent brain damage which was correlated with the duration of the sarin-induced seizures (Chapman et al., 2006). Read More

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https://linkinghub.elsevier.com/retrieve/pii/S0161813X193004
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http://dx.doi.org/10.1016/j.neuro.2019.05.006DOI Listing
September 2019
11 Reads

Multinational comparison of new antidepressant use in older adults: a cohort study.

BMJ Open 2019 05 14;9(5):e027663. Epub 2019 May 14.

Department of Medicine, University of Manchester, Manchester, UK.

Objectives: We used an international pharmacosurveillance network to estimate the rate and characteristics of antidepressant use in older adults in countries with more conservative (UK) and liberal depression guidelines (Canada, USA).

Setting: Electronic health records and population-based administrative data from six jurisdictions in four countries (UK, Taiwan, USA and Canada).

Participants: A historical cohort of older adults (≥65 years) who had a new episode of antidepressant use between 2009 and 2014. Read More

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http://dx.doi.org/10.1136/bmjopen-2018-027663DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6530307PMC
May 2019
10 Reads

Organophosphorus Compounds Poisoning in a Neonate: A Case Report.

Mymensingh Med J 2019 Apr;28(2):470-473

Professor Jagadish C Das, Professor, Department of Neonatology, Chittagong Medical College (CMC), Chittagong, Bangladesh; E-mail:

Organophosphorus compounds (OPC) are widely used insecticides. Such poisoning is very rare in neonate. A 23 days old infant was admitted with severe respiratory distress, excessive secretion from nose and mouth, bluish discoloration of extremities and poor feeding for 4 hours. Read More

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April 2019
12 Reads

Cognitive-enhancing and ameliorative effects of acanthoside B in a scopolamine-induced amnesic mouse model through regulation of oxidative/inflammatory/cholinergic systems and activation of the TrkB/CREB/BDNF pathway.

Food Chem Toxicol 2019 Jul 8;129:444-457. Epub 2019 May 8.

Department of Applied Life Sciences, Graduate School of Konkuk University, Research Institute of Inflammatory Diseases, Chungju, 27478, Republic of Korea; Department of Integrated Bio Science and Biotechnology, College of Biomedical and Health Science, Nanotechnology Research Center, Konkuk University, Chungju, 27478, Republic of Korea. Electronic address:

Recently, our research team reported the anti-amnesic potential of desalted-hydroethanolic extracts of Salicornia europaea L. (SE-EE). In this study, we performed bioactivity-guided isolation and identification of Acanthoside B (Aca. Read More

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http://dx.doi.org/10.1016/j.fct.2019.04.062DOI Listing
July 2019
3 Reads
2.895 Impact Factor

Effect of hydroalcoholic Echium amoenum extract on scopolamine-induced learning and memory impairment in rats.

Pharm Biol 2018 Dec;56(1):672-677

b Department of Biology , Izeh Branch, Islamic Azad University , Izeh , Iran.

Context: Scopolamine, a muscarinic receptor antagonist, causes memory loss that resembles Alzheimer's disease (AD). Echium amoenum L. (Boraginaceae) is a famous medicinal plant of Iran that is traditionally used as a sedative and mood enhancer. Read More

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http://dx.doi.org/10.1080/13880209.2018.1543330DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6292346PMC
December 2018
2 Reads

Adverse events associated with diphenhydramine in children, 2008-2015.

Clin Toxicol (Phila) 2020 Feb 7;58(2):99-106. Epub 2019 May 7.

Rocky Mountain Poison and Drug Center, Denver Health and Hospital Authority, Denver, CO, USA.

Diphenhydramine (DPH) exposures in children may be the result of accidental unsupervised ingestions, caregiver error, and intentional misuse of DPH-containing cough and cold medications (CCM). We sought to understand the nature of pediatric ingestions of DPH, particularly the toxicity and outcome of a single product, single ingredient DPH (DPH-only) exposures, in order to derive ingredient-specific information about the clinical effects and course of such cases. As part of a U. Read More

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http://dx.doi.org/10.1080/15563650.2019.1609683DOI Listing
February 2020
11 Reads

Neuroprotective effect of -acetylcysteine against cisplatin-induced toxicity in rat brain by modulation of oxidative stress and inflammation.

Drug Des Devel Ther 2019 11;13:1155-1162. Epub 2019 Apr 11.

Department of Zoology, Faculty of Science, University of Alexandria, Alexandria, Egypt,

Background: Neurotoxicity is a major obstacle to the effectiveness of cisplatin (CDDP) in cancer chemotherapy. Oxidative stress and inflammation are considered to be the major mechanisms involved in CDDP-induced neurotoxicity. The rationale of our study was to investigate the efficacy of -acetylcysteine (NAC) at two different doses in the management of CDDP-induced toxicity in rat brain by monitoring its antioxidant and anti-inflammatory effects. Read More

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http://dx.doi.org/10.2147/DDDT.S191240DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6469471PMC
September 2019
1 Read

Inhibition of Oxidative Neurotoxicity and Scopolamine-Induced Memory Impairment by -Mangostin: and Evidence.

Oxid Med Cell Longev 2019 24;2019:3640753. Epub 2019 Mar 24.

College of Pharmacy, Dongguk University-Seoul, Goyang, Gyeonggi-do 10326, Republic of Korea.

Among a series of xanthones identified from mangosteen, the fruit of L. (Guttifereae), - and -mangostins are known to be major constituents exhibiting diverse biological activities. However, the effects of -mangostin on oxidative neurotoxicity and impaired memory are yet to be elucidated. Read More

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http://dx.doi.org/10.1155/2019/3640753DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6451816PMC
August 2019
2 Reads

Exendin-4 attenuates brain mitochondrial toxicity through PI3K/Akt-dependent pathway in amyloid beta (1-42)-induced cognitive deficit rats.

Neurochem Int 2019 09 17;128:39-49. Epub 2019 Apr 17.

Division of Pharmacology, Institute of Pharmaceutical Research, GLA University, Mathura, 281 406, India.

Alzheimer's disease (AD) is a progressive neurodegenerative disorder characterized by memory loss, disorientation and gradual deterioration of intellectual ability. In the pharmacotherapy of AD, the mitochondrial protective activity of Exendin-4 in experimental studies is yet to be established though its effectiveness is demonstrated in these patients. Therefore, the mitochondria protective activity of Exendin-4 (5 μg/kg, i. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S01970186193002
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http://dx.doi.org/10.1016/j.neuint.2019.04.006DOI Listing
September 2019
17 Reads

Scopolamine Toxicity in an Elderly Patient.

Mil Med 2019 12;184(11-12):937-938

Department of Anesthesia, Brooke Army Medical Center, 3551 Rodger Brooke Dr, Ft Sam Houston, TX 78234.

We present a case of a 66-year-old female who was to undergo a scheduled operation and placed on our institution's ERAS (Enhanced Recovery After Surgery) protocol. The intraoperative course was unremarkable. The patient developed delayed emergence in the Post-Anesthesia Care Unit. Read More

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http://dx.doi.org/10.1093/milmed/usz086DOI Listing
December 2019
23 Reads

Toxicological analysis of cocaine adulterants in blood samples.

Forensic Sci Int 2019 Jun 12;299:95-102. Epub 2019 Mar 12.

National Institute of Legal Medicine and Forensic Sciences, Portugal.

Cocaine was the second most widely used drug in Europe in 2016, with 3.5 million consumers aged 15-64 years old. Adulterants are pharmacologically active substances developed for medical purposes, however, there is little knowledge about their influence in the human body when there is concomitant use with cocaine. Read More

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http://dx.doi.org/10.1016/j.forsciint.2019.03.005DOI Listing
June 2019
18 Reads

Counteracting tabun inhibition by reactivation by pyridinium aldoximes that interact with active center gorge mutants of acetylcholinesterase.

Toxicol Appl Pharmacol 2019 06 9;372:40-46. Epub 2019 Apr 9.

Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California at San Diego, La Jolla, USA. Electronic address:

Tabun represents the phosphoramidate class of organophosphates that are covalent inhibitors of acetylcholinesterase (AChE), an essential enzyme in neurotransmission. Currently used therapy in counteracting excessive cholinergic stimulation consists of a muscarinic antagonist (atropine) and an oxime reactivator of inhibited AChE, but the classical oximes are particularly ineffective in counteracting tabun exposure. In a recent publication (Kovarik et al. Read More

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http://dx.doi.org/10.1016/j.taap.2019.04.007DOI Listing
June 2019
18 Reads