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Scopolamine

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https://www.readbyqxmd.com/read/28807671/selective-inhibition-of-extra-synaptic-%C3%AE-5-gabaa-receptors-by-s44819-a-new-therapeutic-agent
#1
Lori-An Etherington, Balázs Mihalik, Adrienn Pálvölgyi, István Ling, Katalin Pallagi, Szabolcs Kertész, Péter Varga, Ben G Gunn, Adam R Brown, Matthew R Livesey, Olivia Monteiro, Delia Belelli, József Barkóczy, Michael Spedding, István Gacsályi, Ferenc A Antoni, Jeremy J Lambert
In the mammalian central nervous system (CNS) GABAA receptors (GABAARs) mediate neuronal inhibition and are important therapeutic targets. GABAARs are composed of 5 subunits, drawn from 19 proteins, underpinning expression of 20-30 GABAAR subtypes. In the CNS these isoforms are heterogeneously expressed and exhibit distinct physiological and pharmacological properties. We report the discovery of S44819, a novel tricyclic oxazolo-2,3-benzodiazepine-derivative, that selectively inhibits α5-subunit-containing GABAARs (α5-GABAARs)...
August 11, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28807620/muscarinic-acetylcholine-receptor-but-not-nicotinic-acetylcholine-receptor-plays-a-role-in-morphine-induced-behavioral-sensitization-in-rats
#2
Jinling Sun, Lin Tian, Ruisi Cui, Heng Ruan, Xinwang Li
Background and Aim The cholinergic system can affect drug reward. The present study aimed to examine the roles of muscarinic acetylcholine receptor (mAChR) and nicotinic acetylcholine receptor (nAChR) in morphine-induced behavioral sensitization. METHODS: To analyze the roles of mAChR and nAChR in behavioral sensitization induced by morphine (5mg/kg), seven experiments were designed. Experiments 1 and 2 examined the effects of 3, 1, and 0.3 mg/kg scopolamine and 0.2, 0.1, and 0.05mg/kg scopolamine, respectively, on the locomotor activity when administered alone...
August 11, 2017: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/28806057/rational-design-and-multi-biological-profiling-of-novel-donepezil-trolox-hybrids-against-alzheimer-s-disease-with-cholinergic-antioxidant-neuroprotective-and-cognition-enhancing-properties
#3
Pei Cai, Si-Qiang Fang, Xue-Lian Yang, Jia-Jia Wu, Qiao-Hong Liu, Hao Hong, Xiao-Bing Wang, Lingyi Kong
A novel series of donepezil-trolox hybrids were designed, synthesized and evaluated as multifunctional ligands against Alzheimer's disease (AD). Biological assays showed that these derivatives possessed moderate to good inhibitory activities against acetylcholinesterase (AChE) and monoamine oxidase B (MAO-B) as well as remarkable antioxidant effects. The optimal compound 6d exhibited balanced functions with good inhibition against hAChE (IC50 = 0.54 μM) and hMAO-B (IC50 = 4.3 μM), significant antioxidant activity (41...
August 14, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28805429/the-effect-of-scopolamine-on-matching-behavior-and-the-estimation-of-relative-reward-magnitude
#4
Matthew I Leon, Vanessa Rodriguez-Barrera, Aldo Amaya
We investigated the behavioral effects of scopolamine on rats that bar pressed for trains of electrically stimulating pulses under concurrent variable interval schedules of reward. For the first half of the session (30 min) a 1:4 ratio in the programmed number of stimulation trains delivered at each option was in effect. At the start of the second half of the session, an unsignaled reversal in the relative train number (4:1) occurred. We tracked the relative magnitude of reward estimated for each contiguous pair of reinforced visits to competing options...
August 14, 2017: Behavioral Neuroscience
https://www.readbyqxmd.com/read/28803078/safety-and-effectiveness-of-palliative-drug-treatment-in-the-last-days-of-life-a-systematic-literature-review
#5
REVIEW
Kristian Jansen, Dagny Faksvåg Haugen, Lisa Pont, Sabine Ruths
CONTEXT: Dying patients commonly experience potentially distressing symptoms. Palliative care guidelines recommend opioids, anticholinergics, antipsychotics and benzodiazepines for symptom relief. OBJECTIVES: To systematically review the effectiveness and safety of palliative drug treatment in the last days of life of adult patients, focusing on the management of pain, dyspnea, anxiety, restlessness, and death rattle. METHODS: A systematic search of the literature published before December 2016 in PubMed/MEDLINE, Embase, CINAHL, PsycINFO, Cochrane, ClinicalTrials...
August 9, 2017: Journal of Pain and Symptom Management
https://www.readbyqxmd.com/read/28792471/comparative-studies-on-behavioral-cognitive-and-biomolecular-profiling-of-icr-c57bl-6-and-its-sub-strains-suitable-for-scopolamine-induced-amnesic-models
#6
Govindarajan Karthivashan, Shin-Young Park, Joon-Soo Kim, Duk-Yeon Cho, Palanivel Ganesan, Dong-Kug Choi
Cognitive impairment and behavioral disparities are the distinctive baseline features to investigate in most animal models of neurodegenerative disease. However, neuronal complications are multifactorial and demand a suitable animal model to investigate their underlying basal mechanisms. By contrast, the numerous existing neurodegenerative studies have utilized various animal strains, leading to factual disparity. Choosing an optimal mouse strain for preliminary assessment of neuronal complications is therefore imperative...
August 9, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28781727/cross-state-dependent-learning-interaction-between-scopolamine-and-morphine-in-mice-the-role-of-dorsal-hippocampus
#7
Morteza Maleki, Majid Hassanpour-Ezatti, Majid Navaeian
INTRODUCTION: The current study aimed at investigating the existence of the cross state-dependent learning between morphine and scopolamine (SCO) in mice by passive avoidance method, pointing to the role of CA1 area. METHODS: The effects of pre-training SCO (0.75, 1.5, and 3 μg, Intra-CA1), or morphine (1, 3, and 6 mg/kg, intraperitoneal (i.p.) was evaluated on the retrieval of passive avoidance learning using step-down task in mice (n=10). Then, the effect of pretest administration of morphine (1...
May 2017: Basic and Clinical Neuroscience
https://www.readbyqxmd.com/read/28764962/chiral-pool-synthesis-of-1-2-4-trisubstituted-1-4-diazepanes-as-novel-%C3%AF-1-receptor-ligands
#8
Lena Fanter, Christoph Müller, Dirk Schepmann, Franz Bracher, Bernhard Wünsch
Starting from enantiomerically pure amino acids, 1,4-diazepanes with various substituents in 1, 2, and 4-position were synthesized following the late stage diversification strategy. The key step in the formation of the seven-membered ring was the intramolecular EDC coupling of amino acids 15, 26, and 39. The configuration in 2-position does not influence the σ1 affinity and selectivity over related receptors. A cyclohexylmethyl or a butyl group are the preferred substituents in 4-position, whereas a methyl moiety in 2-position and a (substituted) benzyl moiety in 1-position result in the highest σ1 affinity...
July 17, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28763213/novel-3-1-2-3-6-tetrahydropyridin-4-yl-1h-indole-based-multifunctional-ligands-with-antipsychotic-like-mood-modulating-and-procognitive-activity
#9
Adam Bucki, Monika Marcinkowska, Joanna Śniecikowska, Krzysztof Więckowski, Maciej H Pawłowski, Monika Głuch-Lutwin, Anna Gryboś, Agata Siwek, Karolina Pytka, Magdalena Jastrzębska-Więsek, Anna Partyka, Anna Wesołowska, Paweł Mierzejewski, Marcin Kołaczkowski
The most troublesome aspects of behavioral and psychological symptoms of dementia (BPSD) are nowadays addressed by antidepressant, anxiolytic and antipsychotic drugs, often administered off-label. Considering their modest effectiveness in dementia patients, the increased risk of adverse events and cognitive decline, there is an unmet need for well-tolerated and effective therapy of BPSD. We designed and synthesized multifunctional ligands characterized in vitro as high-affinity partial agonists of D2R, antagonists of 5-HT6R and blockers of SERT...
August 1, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28756934/postoperative-anticholinergic-poisoning-concealed-complications-of-a-commonly-used-medication
#10
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/28751069/activity-dependent-brain-derived-neurotrophic-factor-release-is-required-for-the-rapid-antidepressant-actions-of-scopolamine
#11
Sriparna Ghosal, Eunyoung Bang, Wenzhu Yue, Brendan D Hare, Ashley E Lepack, Matthew J Girgenti, Ronald S Duman
BACKGROUND: Brain-derived neurotrophic factor (BDNF) plays a key role in the pathophysiology and treatment of depression. Recent clinical studies demonstrate that scopolamine, a nonselective muscarinic acetylcholine receptor antagonist, produces rapid antidepressant effects in patients with depression. Rodent studies demonstrate that scopolamine increases glutamate transmission and synaptogenesis in the medial prefrontal cortex (mPFC). Here we tested the hypothesis that activity-dependent BDNF release within the mPFC is necessary for the antidepressant actions of scopolamine...
June 23, 2017: Biological Psychiatry
https://www.readbyqxmd.com/read/28738608/a-fast-bioanalytical-method-based-on-microextraction-by-packed-sorbent-and-uplc-ms-ms-for-determining-new-psychoactive-substances-in-oral-fluid
#12
A M Ares, P Fernández, M Regenjo, A M Fernández, A M Carro, R A Lorenzo
The emergence in recent years of potentially dangerous new psychoactive substances (NPS) that are not under international control has led to the development of multi-analyte procedures for their unequivocal quantification. A fast ultra-performance liquid chromatography-tandem mass spectrometry method (UPLC-MS/MS), in combination with a sample pretreatment based on microextraction by packed sorbent (MEPS), was for the first time used in this work for the simultaneous determination of NPS in oral fluid. This matrix is an effective alternative to typical biological samples for drug control in substitution therapy programs, and also for the prevention and reduction of traffic accidents...
November 1, 2017: Talanta
https://www.readbyqxmd.com/read/28735367/short-term-and-long-term-effects-of-diazepam-on-the-memory-for-discrimination-and-generalization-of-scopolamine
#13
C Casasola-Castro, L Weissmann-Sánchez, E Calixto-González, A Aguayo-Del Castillo, D N Velázquez-Martínez
Benzodiazepines are among the most widely prescribed and misused psychopharmaceutical drugs. Although they are well-tolerated, they are also capable of producing amnestic effects similar to those observed after pharmacological or organic cholinergic dysfunction. To date, the effect of benzodiazepine diazepam on the memory for discrimination of anticholinergic drugs has not been reported. The aim of the present study was to analyze the immediate and long-term effects of diazepam on a drug discrimination task with scopolamine...
July 22, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28733814/neuroprotective-effect-of-ipriflavone-against-scopolamine-induced-memory-impairment-in-rats
#14
Hani S Hafez, Doaa A Ghareeb, Samar R Saleh, Mariam M Abady, Maha A El Demellawy, Hend Hussien, Nihad Abdel-Monem
BACKGROUND: Alzheimer's disease is an age-related neurodegenerative disorder characterized clinically by a progressive loss of memory and cognitive functions resulting in severe dementia. Ipriflavone (IPRI) is a non-hormonal, semi-synthetic isoflavone, clinically used in some countries for the treatment and prevention of postmenopausal osteoporosis. Moreover, ipriflavone is a non-peptidomimetic small molecule AChE inhibitor with an improved bioavailability after systemic administration, due to its efficient blood-brain barrier permeability in comparison with peptidomimetic inhibitors...
July 22, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28720796/eeg-machine-learning-for-accurate-detection-of-cholinergic-intervention-and-alzheimer-s-disease
#15
Sonja Simpraga, Ricardo Alvarez-Jimenez, Huibert D Mansvelder, Joop M A van Gerven, Geert Jan Groeneveld, Simon-Shlomo Poil, Klaus Linkenkaer-Hansen
Monitoring effects of disease or therapeutic intervention on brain function is increasingly important for clinical trials, albeit hampered by inter-individual variability and subtle effects. Here, we apply complementary biomarker algorithms to electroencephalography (EEG) recordings to capture the brain's multi-faceted signature of disease or pharmacological intervention and use machine learning to improve classification performance. Using data from healthy subjects receiving scopolamine we developed an index of the muscarinic acetylcholine receptor antagonist (mAChR) consisting of 14 EEG biomarkers...
July 18, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28716085/the-protective-effect-of-fermented-curcuma-longa-l-on-memory-dysfunction-in-oxidative-stress-induced-c6-gliomal-cells-proinflammatory-activated-bv2-microglial-cells-and-scopolamine-induced-amnesia-model-in-mice
#16
Cheong-Su Eun, Jong-Soon Lim, Jihye Lee, Sam-Pin Lee, Seun-Ah Yang
BACKGROUND: Curcuma longa L. is a well-known medicinal plant that has been used for its anti-cancer, neuroprotective, and hepatoprotective effects. However, the neuroprotective effect of fermented C. longa (FCL) has not been reported. Therefore, in this study, the effectiveness of FCL for the regulation of memory dysfunction was investigated in two brain cell lines (rat glioma C6 and murine microglia BV2) and scopolamine-treated mice. METHODS: C. longa powder was fermented by 5% Lactobacillus plantarum K154 containing 2% (w/v) yeast extract at 30 °C for 72 h followed by sterilization at 121 °C for 15 min...
July 17, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28713618/vanillin-and-4-hydroxybenzyl-alcohol-attenuate-cognitive-impairment-and-the-reduction-of-cell-proliferation-and-neuroblast-differentiation-in-the-dentate-gyrus-in-a-mouse-model-of-scopolamine-induced-amnesia
#17
Yang Hee Kim, Joon Ha Park
4-Hydroxy-3-methoxybenzaldehyde (vanillin) and 4-hydroxybenzyl alcohol (4-HBA) are natural phenolic compounds, which present in many plants and have diverse biological properties. In this study, we examined effects of vanillin and 4-HBA on learning and memory function, cell proliferation, and neuroblast differentiation in the hippocampal dentate gyrus in a mouse model of scopolamine-induced amnesia. Scopolamine (SCO; 1 mg/kg/day, intraperitoneally), vanillin, and 4-HBA (40 mg/kg/day, orally) were administered for 28 days...
June 2017: Anatomy & Cell Biology
https://www.readbyqxmd.com/read/28711308/the-impact-of-scopolamine-pretreatment-on-3-iodothyronamine-t1am-effects-on-memory-and-pain-in-mice
#18
Annunziatina Laurino, Ersilia Lucenteforte, Gaetano De Siena, Laura Raimondi
We previously demonstrated that 3-iodothyronamine (T1AM), a by-product of thyroid hormone metabolism, pharmacologically administered to mice acutely stimulated learning and memory acquisition and provided hyperalgesia with a mechanism which remains to be defined. We now aimed to investigate whether the T1AM effect on memory and pain was maintained in mice pre-treated with scopolamine, a non-selective muscarinic antagonist expected to induce amnesia and, possibly, hyperalgesia. Mice were pre-treated with scopolamine and, after 20min, injected intracerebroventricularly (i...
July 19, 2017: Hormones and Behavior
https://www.readbyqxmd.com/read/28710722/organosulfur-compound-protects-against-memory-decline-induced-by-scopolamine-through-modulation-of-oxidative-stress-and-na-k-atpase-activity-in-mice
#19
Fernanda D da Silva, Mikaela P Pinz, Renata L de Oliveira, Karline C Rodrigues, Francine R Ianiski, Mariana M Bassaco, Claudio C Silveira, Cristiano R Jesse, Silvane S Roman, Ethel A Wilhelm, Cristiane Luchese
The present study investigated the possible effect of BMMS in protecting against memory impairment in an Alzheimer's disease model induced by scopolamine in mice. Another objective was to evaluate the involvement of oxidative stress and Na(+)/K(+) ATPase activity in cerebral cortex and hippocampus of mice. Male Swiss mice were divided into four groups: groups I and III received canola oil (10 ml/kg, intragastrically (i.g.)), while groups II and IV received BMMS (10 mg/kg, i.g.). Thirty minutes after treatments, groups III and IV received scopolamine (1 mg/kg, intraperitoneal (i...
July 14, 2017: Metabolic Brain Disease
https://www.readbyqxmd.com/read/28707113/genetically-engineered-hairy-root-cultures-of-hyoscyamus-senecionis-and-h-muticus-ploidy-as-a-promising-parameter-in-the-metabolic-engineering-of-tropane-alkaloids
#20
Esmaeil Dehghan, Darwin W Reed, Patrick S Covello, Zeinab Hasanpour, Javier Palazon, Kirsi-Marja Oksman-Caldentey, Farajollah Shahriari Ahmadi
Tetraploidy improves overexpression of h6h and scopolamine production of H. muticus, while in H. senecionis, pmt overexpression and elicitation can be used as effective methods for increasing tropane alkaloids. The effects of metabolic engineering in a polyploid context were studied by overexpression of h6h in the tetraploid hairy root cultures of H. muticus. Flow cytometry analysis indicated genetic stability in the majority of the clones, while only a few clones showed genetic instability. Among all the diploid and tetraploid clones, the highest level of h6h transgene expression and scopolamine accumulation was interestingly observed in the tetraploid clones of H...
July 13, 2017: Plant Cell Reports
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