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https://www.readbyqxmd.com/read/27904421/cannabis-induced-moto-cognitive-dysfunction-in-wistar-rats-ameliorative-efficacy-of-nigella-sativa
#1
Aminu Imam, Moyosore Saliu Ajao, Abdulbasit Amin, Wahab Imam Abdulmajeed, Abdulmumin Ibrahim, Olayemi Joseph Olajide, Musa Iyiola Ajibola, Abdulmusawir Alli-Oluwafuyi, Wasiu Gbolahan Balogun
BACKGROUND: Cannabis is a widely used illicit drug with various threats of personality syndrome, and Nigella sativa has been widely implicated as having therapeutic efficacy in many neurological diseases. The present study investigates the ameliorative efficacy of Nigella sativa oil (NSO) on cannabis-induced moto-cognitive defects. METHODS: Scopolamine (1 mg/kg i.p.) was given to induce dementia as a standard base line for cannabis (20 mg/kg)-induced cognitive impairment, followed by an oral administration of NSO (1 ml/kg) for 14 consecutive days...
September 2016: Malaysian Journal of Medical Sciences: MJMS
https://www.readbyqxmd.com/read/27888375/hbk-14-and-hbk-15-with-antidepressant-like-and-or-memory-enhancing-properties-increase-serotonin-levels-in-the-hippocampus-after-chronic-treatment-in-mice
#2
Karolina Pytka, Katarzyna Gawlik, Dorota Pawlica-Gosiewska, Jadwiga Witalis, Anna Waszkielewicz
5-HT1A and 5-HT7 receptor ligands might have antidepressant-like properties and improve cognitive function. We previously reported significant antidepressant- and anxiolytic-like effects of two dual 5-HT1A and 5-HT7 receptor antagonists in various behavioral tests in rodents. As a continuation of our previous experiments, in this study we aimed to investigate whether chronic administration of 1-[(2,6-dimethylphenoxy)ethoxyethyl]-4-(2-methoxyphenyl)piperazine hydrochloride (HBK-14) and 1-[(2-chloro-6-methylphenoxy)ethoxyethyl]-4-(2-methoxyphenyl)piperazine hydrochloride (HBK-15) caused antidepressant-like effects and elevated serotonin levels in the murine hippocampus...
November 25, 2016: Metabolic Brain Disease
https://www.readbyqxmd.com/read/27885411/scopolamine-disrupts-place-navigation-in-rats-and-humans-a-translational-validation-of-the-hidden-goal-task-in-the-morris-water-maze-and-a-real-maze-for-humans
#3
Jan Laczó, Hana Markova, Veronika Lobellova, Ivana Gazova, Martina Parizkova, Jiri Cerman, Tereza Nekovarova, Karel Vales, Sylva Klovrzova, John Harrison, Manfred Windisch, Kamil Vlcek, Jan Svoboda, Jakub Hort, Ales Stuchlik
RATIONALE: Development of new drugs for treatment of Alzheimer's disease (AD) requires valid paradigms for testing their efficacy and sensitive tests validated in translational research. OBJECTIVES: We present validation of a place-navigation task, a Hidden Goal Task (HGT) based on the Morris water maze (MWM), in comparable animal and human protocols. METHODS: We used scopolamine to model cognitive dysfunction similar to that seen in AD and donepezil, a symptomatic medication for AD, to assess its potential reversible effect on this scopolamine-induced cognitive dysfunction...
November 24, 2016: Psychopharmacology
https://www.readbyqxmd.com/read/27865771/cholinergic-activation-affects-the-acute-and-chronic-antinociceptive-effects-of-morphine
#4
Kinga Gawel, Ewa Gibula-Bruzda, Marcin Dziedzic, Malgorzata Jenda-Wojtanowska, Marta Marszalek-Grabska, Jerzy Silberring, Jolanta H Kotlinska
Current studies indicate that the cholinergic and opioid systems interact to modulate pain. In the present work, we investigated the influence of the cholinesterase inhibitors, donepezil (0.5; 1 or 3mg/kg, i.p.) and rivastigmine (0.03; 0.5 or 1mg/kg, i.p.), on the acute antinociceptive effects of morphine (5mg/kg, i.p.) in the hot plate test in mice. Herein, both inhibitors were found to enhance and prolong the analgesic effects of morphine without affecting latencies themselves. In an extension of this work, we determined which cholinergic receptors subtype mediates the enhancement of analgesic effects of morphine, following inhibition of cholinesterases...
November 16, 2016: Physiology & Behavior
https://www.readbyqxmd.com/read/27863370/novel-tacrine-1-2-3-triazole-hybrids-in%C3%A2-vitro-in%C3%A2-vivo-biological-evaluation-and-docking-study-of-cholinesterase-inhibitors
#5
Zahra Najafi, Mohammad Mahdavi, Mina Saeedi, Elahe Karimpour-Razkenari, Raymond Asatouri, Fahimeh Vafadarnejad, Farshad Homayouni Moghadam, Mahnaz Khanavi, Mohammad Sharifzadeh, Tahmineh Akbarzadeh
A new series of tacrine-1,2,3-triazole hybrids were designed, synthesized, and evaluated as potent dual cholinesterase inhibitors. Most of synthesized compounds showed good in vitro inhibitory activities toward both acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Among them, 7-chloro-N-((1-(4-methoxybenzyl)-1H-1,2,3-triazol-4-yl)methyl)-1,2,3,4-tetrahydroacridin-9-amine (5l) was found to be the most potent anti-AChE derivative (IC50 = 0.521 μM) and N-((1-(4-methoxybenzyl)-1H-1,2,3-triazol-4-yl)methyl)-1,2,3,4-tetrahydroacridin-9-amine (5j) demonstrated the best anti-BChE activity (IC50 = 0...
January 5, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27846048/scopolamine-ointment-for-clozapine-associated-sialorrhea-a-case-report
#6
Takashi Goto, Miyoko Kato, Yukiko Matsumura, Naoto Omata, Masato Higashima, Yuji Wada, Mari Yoshida, Kyohei Watanabe, Tetsuya Takahashi
No abstract text is available yet for this article.
November 14, 2016: Journal of Clinical Psychopharmacology
https://www.readbyqxmd.com/read/27829340/preclinical-evaluation-of-avn-322-novel-and-highly-selective-5-ht6-receptor-antagonist-for-the-treatment-of-alzheimer-s-disease
#7
Alexandre V Ivachtchenko, Yan A Ivanenkov, Mark S Veselov
Alla Chem LLC, Hallandale Beach, USA; bAvineuro Pharmaceuticals, Inc., Hallandale Beach, USA; cMoscow Institute of Physics and Technology (State University), Dolgoprudny city, Russian Federation. Abstract: In recent years, 5-hydroxytryptamine subtype 6 receptor (5-HT6 receptor, 5-HT6R) has rapidly emerged as a promising therapeutic target for the treatment of neuropathological disorders, including Alzheimer's disease (AD). Evidence indicates that 5-HT6 receptors are deeply implicated in the processes of learning and memory, while 5-HT6R antagonists were shown to improve cognition in animal models of cognitive impairment...
November 7, 2016: Current Alzheimer Research
https://www.readbyqxmd.com/read/27829270/biflorin-ameliorates-memory-impairments-induced-by-cholinergic-blockade-in-mice
#8
Se Jin Jeon, Boseong Kim, Byeol Ryu, Eunji Kim, Sunhee Lee, Dae Sik Jang, Jong Hoon Ryu
To examine the effect of biflorin, a component of Syzygium aromaticum, on memory deficit, we introduced a scopolamine-induced cognitive deficit mouse model. A single administration of biflorin increased latency time in the passive avoidance task, ameliorated alternation behavior in the Y-maze, and increased exploration time in the Morris water maze task, indicating the improvement of cognitive behaviors against cholinergic dysfunction. The biflorin-induced reverse of latency in the scopolamine-treated group was attenuated by MK-801, an NMDA receptor antagonist...
November 8, 2016: Biomolecules & Therapeutics
https://www.readbyqxmd.com/read/27826121/differential-effects-of-3-4-methylenedioxymethamphetamine-methamphetamine-meta-chlorophenylpiperazine-and-scopolamine-on-behavioral-repetition-versus-variation-in-rats
#9
Rebecca A Olsen, Anne C Macaskill, David N Harper
Acute administration of drugs of abuse, such as MDMA and methamphetamine, disrupts performance on many operant tasks, for example, those used to study memory. This might occur in part because drugs make behavior, in general, more repetitive or more variable, or because they produce a more global disruption to performance. The current study explored this across two experiments by employing Neuringer's 'reinforced variability' procedure. Varied behavior was reinforced at some times during the session and repetitive behavior at other times; lights signalled the behavior required...
November 5, 2016: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/27822508/clozapine-n-oxide-administration-produces-behavioral-effects-in-long-evans-rats-implications-for-designing-dreadd-experiments
#10
Duncan A A MacLaren, Richard W Browne, Jessica K Shaw, Sandhya Krishnan Radhakrishnan, Prachi Khare, Rodrigo A España, Stewart D Clark
Clozapine N-oxide (CNO) is a ligand for a powerful chemogenetic system that can selectively inhibit or activate neurons; the so-called Designer Receptors Exclusively Activated by Designer Drugs (DREADD) system. This system consists of synthetic G-protein-coupled receptors, which are not believed to be activated by any endogenous ligand, but are activated by the otherwise inert CNO. However, it has previously been shown that the administration of CNO in humans and rats leads to detectable levels of the bioactive compounds clozapine and N-desmethylclozapine (N-Des)...
September 2016: ENeuro
https://www.readbyqxmd.com/read/27822272/combined-administration-of-melissa-officinalis-and-boswellia-serrata-extracts-in-an-animal-model-of-memory
#11
Mohaddese Mahboubi, Mohsen Taghizadeh, Sayyed Alireza Talaei, Sayyed Mehdi Takht Firozeh, Ali Akbar Rashidi, Omid Reza Tamtaji
BACKGROUND: Boswellia serrata and Melissa officinalis is traditionally used for its memory enhancing effects. OBJECTIVES: In this study, we evaluated the protective effects of combined form of these extracts on memory improvement of scopolamine treated rats by the Morris water maze method. MATERIALS AND METHODS: Two groups (group 1 and 2) of animals were pretreated with combined extracts of B. serrata and M. officinalis (200, 400 mg/Kg body weight) for four weeks and then, 30 minutes before starting the experiment scopolamine was injected (0...
September 2016: Iranian Journal of Psychiatry and Behavioral Sciences
https://www.readbyqxmd.com/read/27815136/phenylquinoxalinone-cftr-activator-as-potential-prosecretory-therapy-for-constipation
#12
Onur Cil, Puay-Wah Phuan, Jung-Ho Son, Jie S Zhu, Colton K Ku, Niloufar Akhavan Tabib, Andrew P Teuthorn, Loretta Ferrera, Nicholas C Zachos, Ruxian Lin, Luis J V Galietta, Mark Donowitz, Mark J Kurth, A S Verkman
Constipation is a common condition for which current treatments can have limited efficacy. By high-throughput screening, we recently identified a phenylquinoxalinone activator of the cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel that stimulated intestinal fluid secretion and normalized stool output in a mouse model of opioid-induced constipation (Cil et al Cell Mol Gastroenterol Hepatol 2:317-327, 2016). Here, we report phenylquinoxalinone structure-activity analysis, mechanism of action, animal efficacy data in acute and chronic models of constipation, and functional data in ex vivo primary cultured human enterocytes...
October 15, 2016: Translational Research: the Journal of Laboratory and Clinical Medicine
https://www.readbyqxmd.com/read/27813263/modulation-of-cue-triggered-reward-seeking-by-cholinergic-signaling-in-the-dorsomedial-striatum
#13
Sean B Ostlund, Angela T Liu, Kate M Wassum, Nigel T Maidment
The dorsomedial striatum (DMS) has been strongly implicated in flexible, outcome-based decision making, including the outcome-specific Pavlovian-to-instrumental transfer effect (PIT), which measures the tendency for a reward-predictive cue to preferentially motivate actions that have been associated with the predicted reward over actions associated with different rewards. Although the neurochemical underpinnings of this effect are not well understood, there is growing evidence that striatal acetylcholine signaling may play an important role...
November 4, 2016: European Journal of Neuroscience
https://www.readbyqxmd.com/read/27810788/anthriscus-nemorosa-essential-oil-inhalation-prevents-memory-impairment-anxiety-and-depression-in-scopolamine-treated-rats
#14
Eyup Bagci, Emel Aydin, Eugen Ungureanu, Lucian Hritcu
Anthriscus nemorosa (Bieb.) Sprengel is used for medicinal purposes in traditional medicine around the world, including Turkey. Ethnobotanical studies suggest that Anthriscus essential oil could improve memory in Alzheimer's disease. The current study was hypothesized to investigate the beneficial effects of inhaled Anthriscus nemorosa essential oil on memory, anxiety and depression in scopolamine-treated rats. Anthriscus nemorosa essential oil was administered by inhalation in the doses of 1% and 3% for 21 continuous days and scopolamine (0...
October 29, 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/27808424/cholinergic-modulation-of-the-parafacial-respiratory-group
#15
Rozlyn C T Boutin, Zaki Alsahafi, Silvia Pagliardini
Active inspiration and expiration are opposing respiratory phases generated by two separate oscillators in the brainstem; inspiration driven by a neuronal network located in the preBötzinger Complex (preBötC) and expiration driven by a neuronal network located in the paraFacial Respiratory Group (pFRG). While continuous activity of the preBötC is necessary for maintaining ventilation, the pFRG behaves as a conditional expiratory oscillator, being silent in resting conditions and becoming rhythmically active in presence of increased respiratory drive (e...
November 3, 2016: Journal of Physiology
https://www.readbyqxmd.com/read/27777121/efficacy-of-a-new-topical-cationic-emulsion-of-cyclosporine-a-on-dry%C3%A2-eye-clinical-signs-in-an-experimental-mouse-model-of-dry-eye
#16
Philippe Daull, Laurence Feraille, Stefano Barabino, Nicolas Cimbolini, Sophie Antonelli, Virgine Mauro, Jean-Sébastien Garrigue
Dry eye disease (DED) is a complex, multifactorial pathology characterized by corneal epithelium lesions and inflammation. The aim of the present study was to evaluate the efficacy of a cationic emulsion of cyclosporine A (CsA) in a mouse model that mimics severe dry eye. Eight to 12-week-old female C57BL/6N mice with tail patches of scopolamine were housed in controlled environment chambers to induce dry eye. At day three, following dry eye confirmation by corneal fluorescein staining (CFS, score 0-15) and phenol red thread (PRT) lacrimation test, the mice (n = 10/gp) were either treated 3 times a day in both eyes with drug-free cationic emulsion, a 0...
October 21, 2016: Experimental Eye Research
https://www.readbyqxmd.com/read/27771379/novel-highly-potent-and-in%C3%A2-vivo-active-inhibitor-of-gaba-transporter-subtype-1-with-anticonvulsant-anxiolytic-antidepressant-and-antinociceptive-properties
#17
Kinga Sałat, Adrian Podkowa, Natalia Malikowska, Felix Kern, Jörg Pabel, Ewelina Wojcieszak, Katarzyna Kulig, Klaus T Wanner, Beata Strach, Elżbieta Wyska
BACKGROUND AND PURPOSE: Since GABAergic dysfunction underlies a variety of neurological and psychiatric disorders, numerous strategies leading to the augmentation of GABAergic neurotransmission have been introduced. One of them is the inhibition of GABA reuptake from the synaptic cleft mediated by four plasma membrane GABA transporters (GAT1-4). GAT1 which is exclusively expressed in the brain is an interesting target for centrally acting drugs. In this research, pharmacological properties of a novel, highly potent and selective inhibitor of GAT1, the guvacine derivative named DDPM-2571, were assessed in vivo...
February 2017: Neuropharmacology
https://www.readbyqxmd.com/read/27760517/neuroprotective-effects-of-htr1a-antagonist-way-100635-on-scopolamine-induced-delirium-in-rats-and-underlying-molecular-mechanisms
#18
Yimin Qiu, Dongmei Chen, Xiaojing Huang, Lina Huang, Liang Tang, Jihong Jiang, Lianhua Chen, Shitong Li
BACKGROUND: Limited surveys have assessed the performance of 5-hydroxytreptamine receptor 1A and its antagonist WAY-100635 in pharmacological manipulations targeting delirium therapies. The purpose of this paper was to assess the central pharmacological activity of WAY-100635 in a rat model of scopolamine-induced delirium and its underlying mechanism. RESULTS: A delirium rat model was established by intraperitoneal injection of scopolamine and behavioral changes evaluated through open field and elevated plus maze experiments...
October 19, 2016: BMC Neuroscience
https://www.readbyqxmd.com/read/27758699/design-synthesis-and-molecular-docking-studies-of-new-potential-piperazine-derivatives-as-cognition-enhancers
#19
Chhanda C Danta, Poonam Piplani
BACKGROUND: In 2016, the statistical reports stated that Alzheimer is not just memory loss but it kills and has become the 6th leading cause of death. The number of dementia patients is increasing rapidly and expected to rise to 131.5 million by 2050. Still there is not a drug candidate that can cure the cognitive deficits completely. OBJECTIVE: Series of novel piperazine derivatives have been designed, synthesized and evaluated for cognition enhancing activity...
October 14, 2016: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27753138/buscopan-labeled-with-carbon-14-and-deuterium
#20
Bachir Latli, Michael Stiasni, Matt Hrapchak, Zhibin Li, Nelu Grinberg, Heewon Lee, Carl A Busacca, Chris H Senanayake
Hyosine butyl bromide, the active ingredient in Buscopan, is an anticholinergic and antimuscarinic drug used to treat pain and discomfort caused by abdominal cramps. A straightforward synthesis of carbon-14- and deuterium-labeled Buscopan was developed using scopolamine, n-butyl-1-(14) C bromide, and n-butyl-(2) H9 bromide, respectively. In a second carbon-14 synthesis, the radioactive carbon was incorporated in the tropic acid moiety to follow its metabolism. Herein, we describe the detailed preparations of carbon-14- and deuterium-labeled Buscopan...
November 2016: Journal of Labelled Compounds & Radiopharmaceuticals
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