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Gabaa antagonist

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https://www.readbyqxmd.com/read/29030218/acupuncture-suppresses-intravenous-methamphetamine-self-administration-through-gaba-receptor-s-mediation
#1
Yi Jeong Choi, Nam Jun Kim, Rong Jie Zhao, Da Hye Kim, Chae Ha Yang, Hee Young Kim, Young S Gwak, Eun Young Jang, Jae Su Kim, Yun Kyu Lee, Hyun Jong Lee, Sang Nam Lee, Sung Chul Lim, Bong Hyo Lee
OBJECTIVES: Methamphetamine is one of the widely abused drugs. In spite of a number of studies, there is still little successful therapy to suppress the methamphetamine abuse. Acupuncture has shown to attenuate the reinforcing effects of psychostimulant. Based on, the present study investigated if acupuncture could suppress intravenous methamphetamine self-administration behavior. In addition, a possible neuronal mechanism was investigated. MATERIALS & METHODS: Male Sprague-Dawley rats weighing 270-300g were trained to intake food pellet...
October 10, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/29023772/negative-modulation-of-the-gabaa-%C3%AF-1-receptor-function-by-l-cysteine
#2
Andrea N Beltrán González, Florencia Vicentini, Daniel J Calvo
L-Cysteine is an endogenous Sulphur containing amino acid with multiple and varied roles in the central nervous system, including neuroprotection and the maintenance of the redox balance. However, it was also suggested as an excitotoxic agent implicated in the pathogenesis of neurological disorders such as Parkinson's and Alzheimer's disease. L-Cysteine can modulate the activity of ionic channels, including voltage-gated calcium channels and glutamatergic NMDA receptors, whereas its effects on GABAergic neurotransmission had not been studied before...
October 10, 2017: Journal of Neurochemistry
https://www.readbyqxmd.com/read/29019708/effects-of-long-term-exercise-and-low-level-inhibition-of-gabaergic-synapses-on-motor-control-and-the-expression-of-bdnf-in-the-motor-related-cortex
#3
Takahiro Inoue, Shuta Ninuma, Masataka Hayashi, Akane Okuda, Tadayoshi Asaka, Hiroshi Maejima
Objectives Brain-derived neurotrophic factor (BDNF) plays important roles in neuroplasticity in the brain. The objective of this study was to examine the effects of long-term exercise combined with low-level inhibition of GABAergic synapses on motor control and the expression of BDNF in the motor-related cortex. Methods ICR mice were divided into four groups based on the factors exercise and GABAA receptor inhibition. We administered the GABAA receptor antagonist bicuculline intraperitoneally (0.25 mg/kg)...
October 11, 2017: Neurological Research
https://www.readbyqxmd.com/read/29018828/repurposing-lesogaberan-to-promote-human-islet-cell-survival-and-%C3%AE-cell-replication
#4
Jide Tian, Hoa Dang, Angela Hu, Willem Xu, Daniel L Kaufman
The activation of β-cell's A- and B-type gamma-aminobutyric acid receptors (GABAA-Rs and GABAB-Rs) can promote their survival and replication, and the activation of α-cell GABAA-Rs promotes their conversion into β-cells. However, GABA and the most clinically applicable GABA-R ligands may be suboptimal for the long-term treatment of diabetes due to their pharmacological properties or potential side-effects on the central nervous system (CNS). Lesogaberan (AZD3355) is a peripherally restricted high-affinity GABAB-R-specific agonist, originally developed for the treatment of gastroesophageal reflux disease (GERD) that appears to be safe for human use...
2017: Journal of Diabetes Research
https://www.readbyqxmd.com/read/28989834/the-change-of-picrotoxin-induced-epileptiform-discharges-to-the-beta-oscillation-by-carbachol-in-rat-hippocampal-slices
#5
Ayumi Hashimoto, Toyohiro Sawada, Kiyohisa Natsume
The study aimed to determine whether and how the activation of the acetylcholine receptor affects epileptiform discharges in the CA3 region in a rat hippocampus. Picrotoxin (100 μM), a GABAA receptor antagonist, was applied to a hippocampal slice to induce epileptiform discharges. The effects of the cholinergic agonist, carbachol, on the discharges were examined at the several concentrations (1-30 μM). Carbachol had different impacts on epileptiform discharges at the different concentrations. Relatively low concentrations of carbachol (<10 μM) increased the frequency but decreased the amplitude of the discharges...
2017: Biophysics and Physicobiology
https://www.readbyqxmd.com/read/28987273/tranexamic-acid-impairs-hippocampal-synaptic-transmission-mediated-by-gamma-aminobutyric-acid-receptor-type-a
#6
Hedwig Irl, Stephan Kratzer, Stefan Schwerin, Eberhard Kochs, Manfred Blobner, Gerhard Schneider, Gerhard Rammes, Rainer Haseneder
High-dose application of tranexamic acid (TXA), a widely used antifibrinolytic drug, can cause seizures in patients undergoing surgery. Mechanistically, seizures are considered to arise from an imbalance between inhibitory and excitatory synaptic transmission, whose main transmitters are gamma-aminobutyric acid (GABA) and glutamate. In the present study, we investigated the effects of TXA on neuronal excitability and synaptic transmission in the hippocampus, a structure that plays a pivotal role in human epilepsy...
October 4, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28970253/characterization-of-soy-deprestatin-a-novel-orally-active-decapeptide-that-exerts-antidepressant-like-effects-via-gut-brain-communication
#7
Yukiha Mori, Saho Asakura, Akane Yamamoto, Saori Odagiri, Daisuke Yamada, Masayuki Sekiguchi, Keiji Wada, Masaru Sato, Atsushi Kurabayashi, Hideyuki Suzuki, Ryuhei Kanamoto, Kousaku Ohinata
We found that the orally administered thermolysin digest of β-conglycinin exhibits antidepressant-like effects in tail suspension and forced swim tests in mice. A comprehensive peptide analysis of the digest using liquid chromatography/mass spectrometry was performed, and LSSTQAQQSY emerged as a candidate antidepressant-like peptide. Orally administered synthetic LSSTQAQQSY exhibited antidepressant-like effects at a dose of 0.3 mg/kg; therefore, we named the decapeptide soy-deprestatin. In contrast, intraperitoneally administered soy-deprestatin was ineffective...
September 27, 2017: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/28969445/anxiolytic-like-effect-of-bifidobacterium-adolescentis-im38-in-mice-with-or-without-immobilisation-stress
#8
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/28963585/effects-of-eugenol-on-respiratory-burst-generation-in-newborn-rat-brainstem-spinal-cord-preparations
#9
Sayumi Kotani, Saki Irie, Masahiko Izumizaki, Hiroshi Onimaru
Eugenol is contained in several plants including clove and is used as an analgesic drug. In the peripheral and central nervous systems, this compound modulates neuronal activity through action on voltage-gated ionic channels and/or transient receptor potential channels. However, it is unknown whether eugenol exerts any effects on the respiratory center neurons in the medulla. We examined the effects of eugenol on respiratory rhythm generation in the brainstem-spinal cord preparation from newborn rat (P0-P3)...
September 29, 2017: Pflügers Archiv: European Journal of Physiology
https://www.readbyqxmd.com/read/28959846/-analgesic-effect-and-central-mechanisms-of-cq-prescription-on-cancer-invasion-induced-mirror-image-pain-in-model-mice
#10
Yu-Mao Jiang, Dan-Dan Sun, Zhi-Guo Wang, Tao Li, Xiao-Liang Zhao, Yue Jiao, Yang Liu, Yu-Juan Li, Jing-Feng Ouyang, Dan-Qiao Wang
This study aimed to analyze the analgesic effect and related central mechanisms of CQ prescription on cancer invasion induced mirror image pain (CIIMIP)in model mice.In the study, male BALB/c mice were randomly divided into normal group, operation control group (injected with 0.2 mL inactivated S180 sarcoma cell sap), model group (injected with 0.2 mL S180 sarcoma cell sap on the right leg near the greater trochanter of femur) and CQ prescription low dose group (intraperitoneally injected with CQ prescription 100 mg•kg⁻¹ on the basis of model mice), CQ prescription middle dose group (intraperitoneally injected with CQ prescription 150 mg•kg⁻¹ on the basis of model mice), and CQ prescription high dose group (intraperitoneally injected with CQ prescription 200 mg•kg⁻¹ on the basis of model mice)...
February 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/28955770/pentylenetetrazol-modulates-redox-system-by-inducing-addicsin-translocation-from-endoplasmic-reticulum-to-plasma-membrane-in-ng108-15-cells
#11
Mitsushi J Ikemoto, Yusuke Murasawa, Pi-Chao Wang
Addicsin (Arl6ip5) is a multifunctional physiological and pathophysiological regulator that exerts its effects by readily forming homo- and hetero-complexes with various functional factors. In particular, addicsin acts as a negative modulator of neural glutamate transporter excitatory amino acid carrier 1 (EAAC1) and participates in the regulation of intracellular glutathione (GSH) content by negatively modulating EAAC1-mediated cysteine and glutamate uptake. Addicsin is considered to play a crucial role in the onset of neurodegenerative diseases including epilepsy...
September 2017: Biochemistry and Biophysics Reports
https://www.readbyqxmd.com/read/28948862/interaction-between-central-gabaa-receptor-and-dopaminergic-system-on-food-intake-in-neonatal-chicks-role-of-d1-and-gabaa-receptors
#12
Mona Hashemzadeh, Morteza Zendehdel, Vahab Babapour, Negar Panahi
OBJECTIVE: The present study designed to examine the role of central GABAA receptors and dopaminergic system on feeding behavior in neonatal layer-type chicken. METHODS: In this study, 6 experiments designed, each with 4 treatment groups (n = 44 in each experiment). In experiment 1, four groups of FD3 chicks received a dose of either the ICV injection of (A) control solution, (B) L-DOPA (levo-dihydroxyphenylalanine as precursor of dopamine; 125 nmol), (C) Gaboxadol (GABAA receptor agonist, 0...
September 26, 2017: International Journal of Neuroscience
https://www.readbyqxmd.com/read/28939165/decrease-in-nmda-receptor-signalling-activity-in-the-anterior-cingulate-cortex-diminishes-defensive-behaviour-and-unconditioned-fear-induced-antinociception-elicited-by-gabaergic-tonic-inhibition-impairment-in-the-posterior-hypothalamus
#13
Luiz Luciano Falconi-Sobrinho, Tayllon Dos Anjos-Garcia, Ricardo de Oliveira, Norberto Cysne Coimbra
Acute γ-aminobutyric acid (GABA) disinhibition in the posterior hypothalamus (PH) elicits defensive reactions that are considered anxiety- and panic attack-like behaviour, and these defensive reactions are followed by antinociception. Evidence indicates that the PH connects with the medial prefrontal cortex, particularly the anterior cingulate cortex (ACC), which seems to regulate these unconditioned fear-induced defensive responses. However, few studies have shown the participation of cortical regions in the control of behavioural and antinociceptive responses organised by diencephalic structures...
September 19, 2017: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28923348/stimulation-of-accumbal-gabaa-receptors-inhibits-delta2-but-not-delta1-opioid-receptor-mediated-dopamine-efflux-in-the-nucleus-accumbens-of-freely-moving-rats
#14
Yuri Aono, Yuri Kiguchi, Yuriko Watanabe, John L Waddington, Tadashi Saigusa
The nucleus accumbens contains delta-opioid receptors that may reduce inhibitory neurotransmission. Reduction in GABAA receptor-mediated inhibition of accumbal dopamine release due to delta-opioid receptor activation should be suppressed by stimulating accumbal GABAA receptors. As delta-opioid receptors are divided into delta2- and delta1-opioid receptors, we analysed the effects of the GABAA receptor agonist muscimol on delta2- and delta1-opioid receptor-mediated accumbal dopamine efflux in freely moving rats using in vivo microdialysis...
September 18, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28919062/progress-and-challenges-in-anti-obesity-pharmacotherapy
#15
REVIEW
Daniel H Bessesen, Luc F Van Gaal
Obesity is a serious and growing worldwide health challenge. Healthy lifestyle choices are the foundation of obesity treatment. However, weight loss can lead to physiological adaptations that promote weight regain. As a result, lifestyle treatment alone typically produces only modest weight loss that is difficult to sustain. In other metabolic diseases, pharmacotherapy is an accepted adjunct to lifestyle. Several anti-obesity drugs have been approved in the USA, European Union, Australia, and Japan including sympathomimetics, pancreatic lipase inhibitors, GABAA receptor activators, a serotonin 2C receptor agonist, opioid antagonist, dopamine-norepinephrine reuptake inhibitor, and glucagon-like peptide-1 (GLP-1) receptor agonists...
September 14, 2017: Lancet Diabetes & Endocrinology
https://www.readbyqxmd.com/read/28916137/oxytocin-induces-penile-erection-and-yawning-when-injected-into-the-bed-nucleus-of-the-stria-terminalis-involvement-of-glutamic-acid-dopamine-and-nitric-oxide
#16
Fabrizio Sanna, Jessica Bratzu, Antonio Argiolas, Maria Rosaria Melis
Oxytocin (5-100ng), but not Arg(8)-vasopressin (100ng), injected unilaterally into the bed nucleus of the stria terminalis (BNST) induces penile erection and yawning in a dose-dependent manner in male rats. The minimal effective dose was 20ng for penile erection and 5ng for yawning. Oxytocin responses were abolished not only by the oxytocin receptor antagonist d(CH2)5Tyr(Me)(2)-Orn(8)-vasotocin (1μg), but also by (+) MK-801 (1μg), an excitatory amino acid receptor antagonist of the N-methyl-d-aspartic acid (NMDA) subtype, SCH 23390 (1μg), a D1 receptor antagonist, but not haloperidol (1μg), a D2 receptor antagonist, and SMTC (40μg), an inhibitor of neuronal nitric oxide synthase, injected into the BNST 15min before oxytocin...
September 18, 2017: Hormones and Behavior
https://www.readbyqxmd.com/read/28901722/%C3%AE-6-subunit-containing-nicotinic-receptors-mediate-low-dose-ethanol-effects-on-ventral-tegmental-area-neurons-and-ethanol-reward
#17
Scott C Steffensen, Samuel I Shin, Ashley C Nelson, Stephanie S Pistorius, Stephanie B Williams, Taylor J Woodward, Hyun Jung Park, Lindsey Friend, Ming Gao, Fenfei Gao, Devin H Taylor, M Foster Olive, Jeffrey G Edwards, Sterling N Sudweeks, Lori M Buhlman, J Michael McIntosh, Jie Wu
Dopamine (DA) neuron excitability is regulated by inhibitory GABAergic synaptic transmission and modulated by nicotinic acetylcholine receptors (nAChRs). The aim of this study was to evaluate the role of α6 subunit-containing nAChRs (α6*-nAChRs) in acute ethanol effects on ventral tegmental area (VTA) GABA and DA neurons. α6*-nAChRs were visualized on GABA terminals on VTA GABA neurons, and α6*-nAChR transcripts were expressed in most DA neurons, but only a minority of VTA GABA neurons from GAD67 GFP mice...
September 13, 2017: Addiction Biology
https://www.readbyqxmd.com/read/28894409/the-effect-of-4-hydroxybenzaldehyde-on-the-%C3%AE-aminobutyric-acid-type-a-receptor
#18
COMMENT
Jingli Zhang, Habsah Mohamad, Jia Hui Wong, Muhammad Bilal, Abdul Hadi Bin Ismail, Amelia Jane Lloyd, Abdul Aziz Mohamed Yusoff, Hasnah Osman, Kok Tong Wong, Zamzuri Idris, Jafri Malin Abdullah
The α1β2γ2 subtype of GABAA receptors is the most commonly found GABAA receptor subtype in the mammalian cortex and hippocampus. It is expressed heterologously in the Xenopus laevis oocyte as a α1β2γ2S/L subtype for application as an in vitro model for the screening of compounds that modulate receptor activities. In fact, 4-hydroxybenzaldehyde (4-HB) has been identified as one of the major components in Dendrocalamus asper bamboo shoots in our previous study, and the current study showed that at 101.7 μM, 4-HB significantly reduced the GABA-induced chloride current of GABAA receptors expressed on Xenopus oocytes, indicating a possible GABAergic antagonistic effect at high concentrations...
March 2017: Malaysian Journal of Medical Sciences: MJMS
https://www.readbyqxmd.com/read/28893667/amnestic-drugs-in-the-odor-span-task-effects-of-flunitrazepam-zolpidem-and-scopolamine
#19
Mark Galizio, Michael Mathews, Madeleine Mason, Danielle Panoz-Brown, Ashley Prichard, Paul Soto
The odor span task is an incrementing non-matching-to-sample procedure designed to provide an analysis of working memory capacity in rodents. The procedure takes place in an arena apparatus and rats are exposed to a series of odor stimuli in the form of scented lids with the selection of new stimuli reinforced. This procedure makes it possible to study drug effects as a function of the number of stimuli to remember. In the present study, the non-selective positive allosteric GABAA receptor modulator flunitrazepam impaired odor span performance at doses that did not affect a control odor discrimination...
September 8, 2017: Neurobiology of Learning and Memory
https://www.readbyqxmd.com/read/28893591/neurosteroid-dehydroepiandrosterone-improves-active-avoidance-retrieval-and-induces-antidepressant-like-behavior-in-rats
#20
Janko Samardzic, Boris Hencic, Jasna Jancic, Dragana Jadzic, Milos Djuric, Dragan I Obradovic, Dubravka Svob Strac
Various studies reported beneficial effects of dehydroepiandrosterone (DHEA) and its sulphate (DHEAS), the neurosteroids involved in various brain functions, on synaptic plasticity, neuronal survival, memory, learning and behavior. This study aimed to investigate the behavioral profile of acute DHEA treatment by using active avoidance (AA) task, primarily predictive of the effects on the retrieval-based learning, and by applying forced swim test (FST), for assessment of antidepressant-like potential. Adult male Wistar rats received intraperitoneal injections of either DHEA (2, 10, 20mg/kg) or solvent, 30min prior to testing...
September 8, 2017: Neuroscience Letters
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