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https://www.readbyqxmd.com/read/29032008/3-iodothyroacetic-acid-ta1-a-by-product-of-thyroid-hormone-metabolism-reduces-the-hypnotic-effect-of-ethanol-without-interacting-at-gaba-a-receptors
#1
Annunziatina Laurino, Elisa Landucci, Francesco Resta, Gaetano De Siena, Rosanna Matucci, Alessio Masi, Laura Raimondi
3-iodothyroacetic acid (TA1) is among the by-products of thyroid hormone metabolism suspected to mediate the non-genomic effects of the hormone (T3). We aim to investigate whether TA1 systemically administered to mice stimulated mice wakefulness, an effect already described for T3 and for another T3 metabolite (i.e. 3-iodothryonamine; T1AM), and whether TA1 interacted at GABA-A receptors (GABA-AR). Mice were pre-treated with either saline (vehicle) or TA1 (1.32, 4 and 11 μg/kg) and, after 10 min, they received ethanol (3...
October 11, 2017: Neurochemistry International
https://www.readbyqxmd.com/read/28986332/anticonvulsant-effects-of-senna-spectabilis-on-seizures-induced-by-chemicals-and-maximal-electroshock
#2
Nkantchoua Nkamguie Gisele Claudine, Njapdounke Kameni Jacqueline Stephanie, Fifen Jean Jules, Taiwe Sotoing Germain, Ojong Lucie Josiane, Kandeda Kavaye Antoine, Ngo Bum Elisabeth
Senna spectabilis (Fabaceae) is one of the medicinal plants used in Cameroon by traditional healers to treat epilepsy, constipation, insomnia, anxiety. The present study aimed to investigate the anticonvulsant effects of Senna spectabilis decoction induced by maximal electroshock (MES), pentylenetetrazole (PTZ), pilocarpine (PC) and its possible action mechanisms in animal models using flumazenil (FLU), methyl-ß-carboline-3-carboxylate (BC) and bicuculline (BIC). Senna spectabilis decoction (106.5 and 213...
October 3, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28969445/anxiolytic-like-effect-of-bifidobacterium-adolescentis-im38-in-mice-with-or-without-immobilisation-stress
#3
H M Jang, S-E Jang, M J Han, D-H Kim
To better understand the role of gut microbiota in the anxiety, we isolated bifidobacteria and lactobacilli from the human faecal microbiota, investigated their inhibitory effects on the expression of interleukin (IL)-6 and tumour necrosis factor (TNF)-α in lipopolysaccharide-stimulated macrophages, and examined the anxiolytic-like effect of Bifidobacterium adolescentis IM38 in mice treated with or without immobilisation stress using the elevated plus maze (EPM) task. Oral administration of IM38 at a dose of 1×10(9) cfu/mouse showed a significant anxiolytic-like effect both in mice exposed to immobilisation stress and in control mice using the EPM test (P<0...
October 3, 2017: Beneficial Microbes
https://www.readbyqxmd.com/read/28956418/protective-effects-of-smyrnium-cordifolium-boiss-essential-oil-on-pentylenetetrazol-induced-seizures-in-mice-involvement-of-benzodiazepine-and-opioid-antagonists
#4
N Abbasi, S Mohammadpour, E Karimi, A Aidy, P Karimi, M Azizi, K Asadollahi
Smyrnium cordifolium as a wild plant is used in traditional medicine in Iran for the treatment of anxiety and insomnia. The anticonvulsant effect of this plant has not been studied to date, therefore this study aimed to evaluate the anticonvulsant effects of its essential oil and curzerene on seizure. Essential oil of the Smyrnium cordifolium plant was prepared by the hydro-distillation method. Gas chromatography and gas chromatography-mass spectroscopy analysis of the essential oil revealed its main components...
July 2017: Journal of Biological Regulators and Homeostatic Agents
https://www.readbyqxmd.com/read/28936791/nmda-receptors-and-no-cgmp-signaling-pathway-mediate-the-diazepam-induced-sensitization-to-withdrawal-signs-in-mice
#5
Sylwia Talarek, Joanna Listos, Jolanta Orzelska-Gorka, Anna Serefko, Jolanta Kotlińska
The goal of the present study was to examine the effects of N-methyl-aspartate (NMDA) receptor antagonists-memantine and ketamine and the drugs modifying the NO:cGMP pathway-NG-nitro-L-arginine methyl ester (L-NAME) and 7-nitroindazole (7-NI), the endogenous precursor of NO-L-arginine, and the guanylyl cyclase inhibitor-methylene blue (MB) on the development of sensitization to withdrawal signs precipitated after chronic, interrupted treatment with diazepam, a benzodiazepine receptor agonist, in mice. To develop the sensitization, the mice were divided into groups: continuously and sporadically (with two diazepam-free periods) treated with diazepam (15 mg/kg, sc)...
September 21, 2017: Neurotoxicity Research
https://www.readbyqxmd.com/read/28929924/the-search-for-a-subtype-selective-pet-imaging-agent-for-the-gabaa-receptor-complex-evaluation-of-the-radiotracer-11-c-ado-in-nonhuman-primates
#6
Shu-Fei Lin, Frederic Bois, Daniel Holden, Nabeel Nabulsi, Richard Pracitto, Hong Gao, Michael Kapinos, Jo-Ku Teng, Anupama Shirali, Jim Ropchan, Richard E Carson, Charles S Elmore, Neil Vasdev, Yiyun Huang
The myriad physiological functions of γ-amino butyric acid (GABA) are mediated by the GABA-benzodiazepine receptor complex comprising of the GABAA, GABAB, and GABAC groups. The various GABAA subunits with region-specific distributions in the brain subserve different functional and physiological roles. For example, the sedative and anticonvulsive effects of classical benzodiazepines are attributed to the α1 subunit, and the α2 and α3 subunits mediate the anxiolytic effect. To optimize pharmacotherapies with improved efficacy and devoid of undesirable side effects for the treatment of anxiety disorders, subtype-selective imaging radiotracers are required to assess target engagement at GABA sites and determine the dose-receptor occupancy relationships...
January 2017: Molecular Imaging
https://www.readbyqxmd.com/read/28911622/sedative-and-hypnotic-effects-of-supercritical-carbon-dioxide-fluid-extraction-from-schisandra-chinensis-in-mice
#7
Hongyan Zhu, Lina Zhang, Guoli Wang, Zhongmei He, Yan Zhao, Yonghua Xu, Yugang Gao, Lianxue Zhang
Schisandra chinensis is a traditional Chinese medicine that has been used for treating insomnia and neurasthenia for centuries. Lignans, which are considered to be the bioactive components, are apt to be extracted by supercritical carbon dioxide. This study was conducted to investigate the sedative and hypnotic activities of the supercritical carbon dioxide fluid extraction of S. chinensis (SFES) in mice and the possible mechanisms. SFES exhibited an obvious sedative effect on shortening the locomotor activity in mice in a dose-dependent (10-200 mg/kg) manner...
October 2016: Journal of Food and Drug Analysis
https://www.readbyqxmd.com/read/28884085/anti-anxiety-and-hypnotic-effects-of-ethanolic-and-aqueous-extracts-of-lippia-citriodora-leaves-and-verbascoside-in-mice
#8
Bibi Marjan Razavi, Naser Zargarani, Hossein Hosseinzadeh
OBJECTIVES: The extract of Lippia citriodora and its main component, verbascoside, are known for their hypnotic effects in traditional medicine. In this study, the anxiolytic and hypnotic effects of L. citriodora leave extracts and verbascoside were evaluated in mice. MATERIALS AND METHODS: Animals were divided into 11 groups of six mice each. Group I received normal saline, Group II received Diazepam (2 mg/kg) as positive control, Groups III, IV and V received L...
July 2017: Avicenna Journal of Phytomedicine
https://www.readbyqxmd.com/read/28882371/comparison-of-subcutaneous-dexmedetomidine-midazolam-versus-alfaxalone-midazolam-sedation-in-leopard-geckos-eublepharis-macularius
#9
Grayson A Doss, Dustin M Fink, Kurt K Sladky, Christoph Mans
OBJECTIVE: To compare dexmedetomidine-midazolam with alfaxalone-midazolam for sedation in leopard geckos (Eublepharis macularius). STUDY DESIGN: Prospective, randomized, blinded, complete crossover study. ANIMALS: Nine healthy adult leopard geckos. METHODS: Geckos were administered a combination of dexmedetomidine (0.1 mg kg(-1)) and midazolam (1.0 mg kg(-1); treatment D-M) or alfaxalone (15 mg kg(-1)) and midazolam (1...
April 24, 2017: Veterinary Anaesthesia and Analgesia
https://www.readbyqxmd.com/read/28828702/-intoxication-with-psychotropic-drugs
#10
R Bellmann, M Joannidis
Psychotropic drugs are medications that are indicated for treatment of psychiatric disorders. Attempted suicide is the major reason for intoxication but inadvertent overdosing may also occur. Other psychotropic agents are taken because of their stimulating and hallucinogenic effects and many have a high addictive potential. Poisoning is usually due to accidental overdosing. For treatment of benzodiazepine and opioid intoxication, flumazenil and naloxone, respectively, are used as specific antagonists. For intoxication by tricyclic antidepressants, sodium bicarbonate is the treatment of choice...
August 21, 2017: Medizinische Klinik, Intensivmedizin und Notfallmedizin
https://www.readbyqxmd.com/read/28807671/selective-inhibition-of-extra-synaptic-%C3%AE-5-gabaa-receptors-by-s44819-a-new-therapeutic-agent
#11
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 12, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28798689/high-resolution-uhplc-ms-metabolomics-and-sedative-anxiolytic-effects-of-latua-pubiflora-a-mystic-plant-used-by-mapuche-amerindians
#12
Eliana L Sánchez-Montoya, Marco A Reyes, Joel Pardo, Juana Nuñez-Alarcón, José G Ortiz, Juan C Jorge, Jorge Bórquez, Andrei Mocan, Mario J Simirgiotis
Latua pubiflora (Griseb) Phil. Is a native shrub of the Solanaceae family that grows freely in southern Chile and is employed among Mapuche aboriginals to induce sedative effects and hallucinations in religious or medicine rituals since prehispanic times. In this work, the pentobarbital-induced sleeping test and the elevated plus maze test were employed to test the behavioral effects of extracts of this plant in mice. The psychopharmacological evaluation of L. pubiflora extracts in mice determined that both alkaloid-enriched as well as the non-alkaloid extracts produced an increase of sleeping time and alteration of motor activity in mice at 150 mg/Kg...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28796283/flumazenil-versus-placebo-or-no-intervention-for-people-with-cirrhosis-and-hepatic-encephalopathy
#13
REVIEW
Ee Teng Goh, Mette L Andersen, Marsha Y Morgan, Lise Lotte Gluud
BACKGROUND: Hepatic encephalopathy is a common complication of cirrhosis which results in poor brain functioning. The spectrum of changes associated with hepatic encephalopathy ranges from the clinically 'indiscernible' or minimal hepatic encephalopathy to the clinically 'obvious' or overt hepatic encephalopathy. Flumazenil is a synthetic benzodiazepine antagonist with high affinity for the central benzodiazepine recognition site. Flumazenil may benefit people with hepatic encephalopathy through an indirect negative allosteric modulatory effect on gamma-aminobutyric acid receptor function...
August 10, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28795023/leptocarpus-disjunctus-prolongs-sleeping-time-and-increases-nonrapid-eye-movement-sleep-with-additional-anxiolytic-capacity
#14
Watchara Damjuti, Thanes Fuangfoo, Chanida Palanuvej, Tingli Li, Nijsiri Ruangrungsi
Leptocarpus disjunctus Mast. (Restionaceae) is an edible plant which has indigenous warnings regarding its side effects which can manifest as dizziness. This study investigated hypnotic and anxiolytic properties using several animal models. Anxiolytic activities were evaluated using locomotor determination by elevated plus-maze test, open-field test, and rotarod performance test. Hypnotic activities were performed using pentobarbital sodium-induced sleeping time test. Sleep architecture and quality were obtained from sleep-wake analysis and nonrapid eye movement (NREM) delta activity using electroencephalography...
July 2017: Journal of Advanced Pharmaceutical Technology & Research
https://www.readbyqxmd.com/read/28777735/evidence-for-the-involvement-of-the-gaba-ergic-pathway-in-the-anticonvulsant-activity-of-the-roots-bark-aqueous-extract-of-anthocleista-djalonensis-a-chev-loganiaceae
#15
Germain Sotoing Taiwe, Arielle Larissa Ndieudieu Kouamou, Armelle Rosalie Mbang Ambassa, Joseph Renaud Menanga, Thierry Bang Tchoya, Paul Desire Djomeni Dzeufiet
BACKGROUND: The root bark of Anthocleista djalonensis A. Chev. (Loganiaceae) is widely used in traditional medicine in Northern Cameroon to treat epilepsy and related conditions, such as migraine, insomnia, dementia, anxiety, and mood disorders. METHODS: To investigate the anticonvulsant effects and the possible mechanisms of this plant, an aqueous extract of Anthocleista djalonensis (AEAD) was evaluated by using animal models of bicuculline-, picrotoxin-, pilocarpine-, and pentylenetetrazole-induced convulsions...
August 4, 2017: Journal of Basic and Clinical Physiology and Pharmacology
https://www.readbyqxmd.com/read/28748168/potentiating-effects-of-perovskia-abrotanoides-karel-on-pentobarbital-induced-sleep
#16
Fatemeh Forouzanfar, Azar Hosseini, Mohammad Sadegh Amiri, Hassan Rakhshandeh
OBJECTIVE: Sleeplessness is the most common sleep disorder. In this study the hypnotic effect of the hydro-alcoholic extract (HAE) of Perovskia abrotanoides Karel. and its water fraction (WF), ethyl acetate fraction (EAF) and n-butanol fraction (NBF) were studied in mice. MATERIALS AND METHODS: The test compounds were administered intraperitoneally to mice 30 min before the administration of sodium pentobarbital (30 mg/kg.). Moreover, the influence of flumazenil on the hypnotic effect of the extracts was evaluated...
May 2017: Avicenna Journal of Phytomedicine
https://www.readbyqxmd.com/read/28745801/flumazenil-versus-placebo-or-no-intervention-for-people-with-cirrhosis-and-hepatic-encephalopathy
#17
REVIEW
Ee Teng Goh, Mette L Andersen, Marsha Y Morgan, Lise Lotte Gluud
BACKGROUND: Hepatic encephalopathy is a common complication of cirrhosis which results in poor brain functioning. The spectrum of changes associated with hepatic encephalopathy ranges from the clinically 'indiscernible' or minimal hepatic encephalopathy to the clinically 'obvious' or overt hepatic encephalopathy. Flumazenil is a synthetic benzodiazepine antagonist with high affinity for the central benzodiazepine recognition site. Flumazenil may benefit people with hepatic encephalopathy through an indirect negative allosteric modulatory effect on gamma-aminobutyric acid receptor function...
July 26, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28740086/novel-molecule-exhibiting-selective-affinity-for-gabaa-receptor-subtypes
#18
Cecilia M Borghese, Melissa Herman, Lawrence D Snell, Keri J Lawrence, Hyun-Young Lee, Donald S Backos, Lauren A Vanderlinden, R Adron Harris, Marisa Roberto, Paula L Hoffman, Boris Tabakoff
Aminoquinoline derivatives were evaluated against a panel of receptors/channels/transporters in radioligand binding experiments. One of these derivatives (DCUK-OEt) displayed micromolar affinity for brain γ-aminobutyric acid type A (GABAA) receptors. DCUK-OEt was shown to be a positive allosteric modulator (PAM) of GABA currents with α1β2γ2, α1β3γ2, α5β3γ2 and α1β3δ GABAA receptors, while having no significant PAM effect on αβ receptors or α1β1γ2, α1β2γ1, α4β3γ2 or α4β3δ receptors...
July 24, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28733205/-dehydrofukinone-modulates-membrane-potential-and-delays-seizure-onset-by-gabaa-receptor-mediated-mechanism-in-mice
#19
Quelen Iane Garlet, Luana da Costa Pires, Laura Hautrive Milanesi, Joseane Righes Marafiga, Bernardo Baldisserotto, Carlos Fernando Mello, Berta Maria Heinzmann
(+)-Dehydrofukinone (DHF), isolated from Nectandra grandiflora (Lauraceae) essential oil, induces sedation and anesthesia by modulation of GABAa receptors. However, no study has addressed whether DHF modulates other cellular events involved in the control of cellular excitability, such as seizure behavior. Therefore, the aim of the present study was to investigate the effect of DHF on cellular excitability and seizure behavior in mice. For this purpose, we used isolated nerve terminals (synaptosomes) to examine the effect of DHF on the plasma membrane potential, the involvement of GABAa receptors and the downstream activation of Ca(2+) mobilization...
October 1, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28730280/evidence-for-the-involvement-of-the-gabaergic-but-not-serotonergic-transmission-in-the-anxiolytic-like-effect-of-bisabolol-in-the-mouse-elevated-plus-maze
#20
Mohaddeseh Abouhosseini Tabari, Mohammad Amir Bagherpour Tehrani
Bisabolol (α-(-)-bisabolol) is a sesquiterpene which is a part of the essential oil of a variety of plants, but its common source is German chamomile. Several bioactivities including anti-inflammatory, anti-nociceptive, and anti-tumor effects were attributed to bisabolol. However, the neuropharmacological properties of bisabolol have not yet been reported. The present study evaluated behavioral effects of bisabolol using elevated plus maze (EPM), open field test (OFT), and rotarod test. Moreover, this study also examined whether the 5-HT1A and GABAA-benzodiazepine receptor systems are involved in the anxiolytic-like effects of bisabolol...
July 20, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
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