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https://www.readbyqxmd.com/read/29341071/anticholinergic-medication-for-antipsychotic-induced-tardive-dyskinesia
#1
REVIEW
Hanna Bergman, Karla Soares-Weiser
BACKGROUND: Antipsychotic (neuroleptic) medication is used extensively to treat people with serious mental illnesses. However, it is associated with a wide range of adverse effects, including movement disorders. Because of this, many people treated with antipsychotic medication also receive anticholinergic drugs in order to reduce some of the associated movement side-effects. However, there is also a suggestion from animal experiments that the chronic administration of anticholinergics could cause tardive dyskinesia...
January 17, 2018: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/29337893/soybean-derived-phytoalexins-improve-cognitive-function-through-activation-of-nrf2-ho-1-signaling-pathway
#2
Ji Yeon Seo, Bo Ram Kim, Jisun Oh, Jong-Sang Kim
As soy-derived glyceollins are known to induce antioxidant enzymes in various types of cells and tissues, we hypothesized that the compounds could protect neurons from damage due to reactive oxygen species (ROS). In order to examine the neuroprotective effect of glyceollins, primary cortical neurons collected from mice and mouse hippocampal HT22 cells were challenged with glutamate. Glyceollins attenuated glutamate-induced cytotoxicity in primary cortical neuron isolated from mice carrying wild-type nuclear factor (erythroid-derived 2)-like 2 (Nrf2), but the compounds were ineffective in those isolated from Nrf2 knockout mice, suggesting the involvement of the Nrf2 signaling pathway in glyceollin-mediated neuroprotection...
January 16, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29334662/aqueous-extracts-of-two-tropical-ethnobotanicals-tetrapleura-tetraptera-and-quassia-undulata-improved-spatial-and-non-spatial-working-memories-in-scopolamine-induced-amnesic-rats-influence-of-neuronal-cholinergic-and-antioxidant-systems
#3
Veronica O Odubanjo, Emmanuel O Ibukun, Ganiyu Oboh, Stephen A Adefegha
BACKGROUND: Tetrapleura tetraptera (TT) and Quassia undulata (QU) are two predominant tropical ethnobotanicals with various medicinal values but are commonly used in folklore for the treatment of mental illness without justifiable mechanisms of action. AIM OF THE STUDY: To investigate the effects of aqueous extracts from TT fruits and QU leaves on the spatial and non-spatial working memory, antioxidant status and activities of neuronal marker enzymes of scopolamine-induced amnesic rats and thus, understand the possible mechanism of action of these plants...
January 11, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29330003/effects-of-5-ht5a-receptor-blockade-on-amnesia-or-forgetting
#4
L Aparicio-Nava, L A Márquez-García, A Meneses
Previously the effects (0.01-3.0 mg/kg) of post-training SB-699551 (a 5-HT5A receptor antagonist) were reported in the associative learning task of autoshaping, showing that SB-699551 (0.1 mg/kg) decreased lever-press conditioned responses (CR) during short-term (STM; 1.5-h) or (3.0 mg/kg) long-term memory (LTM; 24-h); relative to the vehicle animals. Moreover, as pro-cognitive efficacy of SB-699551 was reported in the ketamine-model of schizophrenia. Hence, firstly aiming improving performance (conditioned response, CR), in this work autoshaping lever-press vs...
January 9, 2018: Behavioural Brain Research
https://www.readbyqxmd.com/read/29328430/vanillin-improves-scopolamine%C3%A2-induced-memory-impairment-through-restoration-of-id1-expression-in-the-mouse-hippocampus
#5
Jae-Chul Lee, In Hye Kim, Jeong Hwi Cho, Tae-Kyeong Lee, Joon Ha Park, Ji Hyeon Ahn, Bich Na Shin, Bing Chun Yan, Jong-Dai Kim, Yong Hwan Jeon, Young Joo Lee, Moo-Ho Won, Il Jun Kang
4-Hydroxy-3-methoxybenzaldehyde (vanillin), contained in a number of species of plant, has been reported to display beneficial effects against brain injuries. In the present study, the impact of vanillin on scopolamine‑induced alterations in cognition and the expression of DNA binding protein inhibitor ID‑1 (ID1), one of the inhibitors of DNA binding/differentiation proteins that regulate gene transcription, in the mouse hippocampus. Mice were treated with 1 mg/kg scopolamine with or without 40 mg/kg vanillin once daily for 4 weeks...
January 9, 2018: Molecular Medicine Reports
https://www.readbyqxmd.com/read/29323700/heat-shock-protein-hsp-regulation-by-muscarinic-acetylcholine-receptor-machr-activation-in-the-rat-hippocampus
#6
Frinchi Monica, Scaduto Pietro, Cappello Francesco, Belluardo Natale, Mudò Giuseppa
The cholinergic system plays a crucial role in modulating in the central nervous system physiological responses such as neurogenesis, neuronal differentiation, synaptic plasticity and neuroprotection. In a recent study, we showed that Oxotremorine-M, a non-selective muscarinic acetylcholine receptor agonist, is able to transactivate the fibroblast growth factor receptor and to produce a significant increase in the hippocampal primary neurite outgrowth. In the present study we aimed to explore in the rat hippocampus the possible effect of acute or chronic treatment with Oxotremorine-M on some heat shock proteins (Hsp60, Hsp70, Hsp90) and on activation of related transcription factor heat shock factor 1 (HSF1)...
January 11, 2018: Journal of Cellular Physiology
https://www.readbyqxmd.com/read/29313138/do-psychoactive-drugs-have-a-therapeutic-role-in-compulsivity-studies-on-schedule-induced-polydipsia
#7
Elena Martín-González, Ángeles Prados-Pardo, Santiago Mora, Pilar Flores, Margarita Moreno
RATIONALE: Clinical studies have shown that some psychoactive recreational drugs have therapeutic applications in anxiety, depression, and schizophrenia. However, to date, there are few studies on the therapeutic potential efficacy of recreational drugs in compulsive neuropsychiatric disorders. OBJECTIVES: We explored the therapeutic potential of different psychoactive and psychedelic drugs in a preclinical model of compulsive behavior. METHODS: Outbred male Wistar rats were selected as either high (HD) or low (LD) drinkers according to their behavior in schedule-induced polydipsia (SIP)...
January 8, 2018: Psychopharmacology
https://www.readbyqxmd.com/read/29291439/novel-non-sulfonamide-5-ht6-receptor-partial-inverse-agonist-in-a-group-of-imidazo-4-5-b-pyridines-with-cognition-enhancing-properties
#8
David Vanda, Miroslav Soural, Vittorio Canale, Séverine Chaumont-Dubel, Grzegorz Satała, Tomasz Kos, Petr Funk, Veronika Fülöpová, Barbora Lemrová, Paulina Koczurkiewicz, Elżbieta Pękala, Andrzej J Bojarski, Piotr Popik, Philippe Marin, Paweł Zajdel
A small library of novel 3H-imidazo[4,5-b]pyridine and 1H-imidazo[4,5-c]pyridine derivatives was designed and synthesized as non-sulfonamide 5-HT6 receptor ligands. In vitro evaluation allowed to identify compound 17 (2-ethyl-3-(3-fluorobenzyl)-7-(piperazin-1-yl)-3H-imidazo[4,5-b]pyridine) as potent 5-HT6 receptor partial inverse agonist in Gs signaling (Ki = 6 nM, IC50 = 17.6 nM). Compound 17 displayed high metabolic stability, favorable cytochrome P450 isoenzyme (2D6, 3A4) profile, did not affect PgP-protein binding, without evoking mutagenic effects...
December 16, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29287786/leptin-treatment-prevents-long-term-abnormalities-in-cognition-seizure-threshold-hippocampal-mossy-fiber-sprouting-and-znt3-cb-d28k-expression-in-a-rat-developmental-twist-seizure-model
#9
Hong Ni, Su-Hong Chen, Li-Li Li, Mei-Fang Jin
The mechanism of linking neonatal seizures with long-term brain damage is unclear, and there is no effective drug to block this long-term pathological process. Recently, the fat-derived hormone leptin has been appreciated for its neuroprotective function in neurodegenerative processes, although less is known about the effects of leptin on neonatal seizure-induced brain damage. Here, we developed a "twist" seizure model by coupling pilocarpine-induced neonatal status epilepticus (SE) with later exposure to penicillin to test whether leptin treatment immediately after neonatal SE would exert neuroprotective effects on cognition, seizure threshold and hippocampal mossy fiber sprouting, as well if leptin had any influence on the expression of zinc transporter 3 (ZnT3) and calcium homeostasis-related CB-D28k in the hippocampus...
December 26, 2017: Epilepsy Research
https://www.readbyqxmd.com/read/29278947/synthesis-and-bioevaluation-of-new-tacrine-cinnamic-acid-hybrids-as-cholinesterase-inhibitors-against-alzheimer-s-disease
#10
Yao Chen, Jie Zhu, Jun Mo, Hongyu Yang, Xueyang Jiang, Hongzhi Lin, Kai Gu, Yuqiong Pei, Liang Wu, Renxiang Tan, Jing Hou, Jingyi Chen, Yang Lv, Yaoyao Bian, Haopeng Sun
Small molecule cholinesterases inhibitor (ChEI) provides an effective therapeutic strategy to treat Alzheimer's disease (AD). Currently, the discovery of new ChEI with multi-target effect is still of great importance. Herein, we report the synthesis, structure-activity relationship study and biological evaluation of a series of tacrine-cinnamic acid hybrids as new ChEIs. All target compounds are evaluated for their in vitro cholinesterase inhibitory activities. The representatives which show potent activity on cholinesterase, are evaluated for the amyloid β-protein self-aggregation inhibition and in vivo assays...
December 2018: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/29274366/vesicular-glutamate-transporter-1-vglut1-mediated-glutamate-release-and-membrane-glua1-activation-is-involved-in-the-rapid-antidepressant-like-effects-of-scopolamine-in-mice
#11
Hanjie Yu, Mengmeng Li, Dongsheng Zhou, Dan Lv, Qi Liao, Zhongze Lou, Mengxin Shen, Zhen Wang, Ming Li, Xiao Xiao, Yanhua Zhang, Chuang Wang
Emerging data have identified certain drugs such as scopolamine as rapidly acting antidepressants for major depressive disorder (MDD) that increase glutamate release and induce neurotrophic factors through α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPAR) activation in rodent models. However, little research has addressed the direct mechanisms of scopolamine on AMPAR activation or vesicular glutamate transporter 1 (VGLUT1)-mediated glutamate release in the prefrontal cortex (PFC) of mice...
December 20, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29261656/nicotinic-alpha-7-receptor-agonists-evp-6124-and-bms-933043-attenuate-scopolamine-induced-deficits-in-visuo-spatial-paired-associates-learning
#12
Michael R Weed, Joseph Polino, Laura Signor, Mark Bookbinder, Deborah Keavy, Yulia Benitex, Daniel G Morgan, Dalton King, John E Macor, Robert Zaczek, Richard Olson, Linda J Bristow
Agonists at the nicotinic acetylcholine alpha 7 receptor (nAChR α7) subtype have the potential to treat cognitive deficits in patients with Alzheimer's disease (AD) or schizophrenia. Visuo-spatial paired associates learning (vsPAL) is a task that has been shown to reliably predict conversion from mild cognitive impairment to AD in humans and can also be performed by nonhuman primates. Reversal of scopolamine-induced impairment of vsPAL performance may represent a translational approach for the development of nAChR α7 agonists...
2017: PloS One
https://www.readbyqxmd.com/read/29260547/cognitive-improving-effects-by-highbush-blueberry-vaccinium-crymbosum-l-vinegar-on-scopolamine-induced-amnesia-mice-model
#13
Seong Min Hong, Kyong Hee Soe, Taek Hwan Lee, In Sook Kim, Young Min Lee, Beong Ou Lim
The present study aimed to evaluate the preventive effects of highbush blueberry (Vaccinium corymbosum L.) vinegar (BV) on cognitive functions in a scopolamine (Sco)-induced amnesia model in mice. In this study, Sco (1 mg/kg, intraperitoneal injection) was used to induce amnesia. ICR mice were orally administered donepezil (5 mg/kg), blueberry extract (120 mg/kg), and BV (120 mg/kg) for 7 days. After inducing cognitive impairment by Sco, a behavioral assessment using behavior tests (i.e., Y-maze and passive avoidance tests) was performed...
December 20, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/29260493/effects-of-scopolamine-and-melatonin-cotreatment-on-cognition-neuronal-damage-and-neurogenesis-in-the-mouse-dentate-gyrus
#14
Bai Hui Chen, Ji Hyeon Ahn, Joon Ha Park, Soo Young Choi, Yun Lyul Lee, Il Jun Kang, In Koo Hwang, Tae-Kyeong Lee, Bich-Na Shin, Jae-Chul Lee, Seongkweon Hong, Yong Hwan Jeon, Myoung Cheol Shin, Jun Hwi Cho, Moo-Ho Won, Young Joo Lee
It has been demonstrated that melatonin plays important roles in memory improvement and promotes neurogenesis in experimental animals. We examined effects of melatonin on cognitive deficits, neuronal damage, cell proliferation, neuroblast differentiation and neuronal maturation in the mouse dentate gyrus after cotreatment of scopolamine (anticholinergic agent) and melatonin. Scopolamine (1 mg/kg) and melatonin (10 mg/kg) were intraperitoneally injected for 2 and/or 4 weeks to 8-week-old mice. Scopolamine treatment induced significant cognitive deficits 2 and 4 weeks after scopolamine treatment, however, cotreatment of scopolamine and melatonin significantly improved spatial learning and short-term memory impairments...
December 19, 2017: Neurochemical Research
https://www.readbyqxmd.com/read/29234406/amelioration-of-scopolamine-induced-learning-and-memory-impairment-by-%C3%AE-pinene-in-c57bl-6-mice
#15
Gil-Yong Lee, Chan Lee, Gyu Hwan Park, Jung-Hee Jang
Increasing evidence suggests that neurodegenerative disorders such as Alzheimer's disease (AD) are mediated via disruption of cholinergic neurons and enhanced oxidative stress. Therefore, attention has been focused on searching for antioxidant phytochemicals for the prevention and/or treatment of AD through their ability to fortify cholinergic function and antioxidant defense capacity. In this study, we have investigated the neuroprotective effect of α-pinene (APN) against learning and memory impairment induced by scopolamine (SCO, 1 mg/kg, i...
2017: Evidence-based Complementary and Alternative Medicine: ECAM
https://www.readbyqxmd.com/read/29227101/the-magic-of-crystal-structure-based-inhibitor-optimization-development-of-a-butyrylcholinesterase-inhibitor-with-picomolar-affinity-and-in-vivo-activity
#16
Urban Košak, Boris Brus, Damijan Knez, Simon Žakelj, Jurij Trontelj, Anja Pišlar, Roman Šink, Marko Jukič, Marko Živin, Adrian Podkowa, Florian Nachon, Xavier Brazzolotto, Jure Stojan, Janko Kos, Nicolas Coquelle, Kinga Sałat, Jacques-Philippe Colletier, Stanislav Gobec
The enzymatic activity of butyrylcholinesterase (BChE) in the brain increases with the progression of Alzheimer's disease, thus classifying BChE as a promising drug target in advanced Alzheimer's disease. We used structure-based drug discovery approaches to develop potent, selective, and reversible human BChE inhibitors. The most potent, compound 3, had a picomolar inhibition constant versus BChE due to strong cation-π interactions, as revealed by the solved crystal structure of its complex with human BChE...
December 22, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29225190/scopolamine-induced-passive-avoidance-memory-retrieval-deficit-is-accompanied-with-hippocampal-mmp2-mmp-9-and-mapks-alteration
#17
Maryam Moosavi, Roksana SoukhakLari, Leila Moezi, Fatema Pirsalami
Alzheimer's disease (AD) is a neurodegenerative disorder characterized by progressive loss of memory and cognitive deficit. The observed amnesia in the early stages of AD is suggested to be a retrieval problem, rather than encoding and consolidation deficit. According to the cholinergic hypothesis of AD, scopolamine is used to induce an animal model of amnesia. Howbeit the effect of scopolamine on memory retrieval is contradictory. This study aimed to assess the effect of scopolamine on passive avoidance memory retrieval...
December 7, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29220865/silver-nano-particles-ameliorate-learning-and-spatial-memory-of-male-wistar-rats-by-prevention-of-amyloid-fibril-induced-neurotoxicity
#18
H Ramshini, A-S Moghaddasi, L-S Aldaghi, N Mollania, A Ebrahim-Habibi
Alzheimer's disease (AD) is a chronic degenerative disease characterized by the presence of amyloid plaques and neurofibrillary tangles (NFTs), which results into memory and learning impairments. In the present study, we showed that the aggregates formed by a protein that has no link with Alzheimer's disease, namely the hen egg white lysozyme (HEWL), were cytotoxic and decreased spatial learning and memory in rats. The effect of Ag-nano particles (Ag-NPs) was investigated on disruption of amyloid aggregation and preservation of cognitive behavior of rats...
December 8, 2017: Archives Italiennes de Biologie
https://www.readbyqxmd.com/read/29211764/identification-expression-and-functional-characterization-of-m4l-a-muscarinic-acetylcholine-m4-receptor-splice-variant
#19
Douglas A Schober, Carrie H Croy, Cara L Ruble, Ran Tao, Christian C Felder
Rodent genomic alignment sequences support a 2-exon model for muscarinic M4 receptor. Using this model a novel N-terminal extension was discovered in the human muscarinic acetylcholine M4 receptor. An open reading frame was discovered in the human, mouse and rat with a common ATG (methionine start codon) that extended the N-terminus of the muscarinic acetylcholine M4 receptor subtype by 155 amino acids resulting in a longer variant. Transcriptional evidence for this splice variant was confirmed by RNA-Seq and RT-PCR experiments performed from human donor brain prefrontal cortices...
2017: PloS One
https://www.readbyqxmd.com/read/29209218/nootropic-and-neuroprotective-effects-of-dichrocephala-integrifolia-on-scopolamine-mouse-model-of-alzheimer-s-disease
#20
Nadège E Kouémou, Germain S Taiwe, Fleur C O Moto, Simon Pale, Gwladys T Ngoupaye, Jacqueline S K Njapdounke, Gisèle C N Nkantchoua, David B Pahaye, Elisabeth Ngo Bum
Alzheimer's disease the most common form of dementia in the elderly is a neurodegenerative disease that affects 44 millions of people worldwide. The first treatments against Alzheimer's disease are acetylcholinesterase inhibitors; however, these medications are associated with many side effects. Dichrocephala integrifolia is a traditional herb widely used by indigenous population of Cameroon to treat and prevent Alzheimer's disease and for memory improvement. In this study, we evaluated the effect of the decoction prepared from leaves of D...
2017: Frontiers in Pharmacology
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