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Gaba a antagonist

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https://www.readbyqxmd.com/read/29775659/%C3%AE-2-receptors-in-the-lateral-parabrachial-nucleus-generates-the-pressor-response-of-the-cardiovascular-chemoreflex-effects-of-gaba-a-receptor
#1
Nafiseh Mirzaei Damabi, Gholam Reza Namvar, Fahimeh Yeganeh, Masoumeh Hatam
The lateral parabrachial nucleus (LPBN) is a pontine area involved in cardiovascular chemoreflex. This study was performed to find the effects of reversible synaptic blockade of the LPBN on the chemoreflex responses, and to find the roles of GABAA receptor and α2 -adenoreceptor (α2 -AR) in chemoreflex. It also aimed to seek possible interaction between GABA and noradrenergic systems of the LPBN in urethane-anesthetized male rats. Cardiovascular chemoreflex was activated by intravenous injection of potassium cyanide (KCN, 80 μg/kg)...
May 15, 2018: Brain Research Bulletin
https://www.readbyqxmd.com/read/29766792/gabaa-receptors-various-stoichiometrics-of-subunit-arrangement-in-%C3%AE-1%C3%AE-3-and-%C3%AE-1%C3%AE-3%C3%AE%C2%B5-receptors
#2
Ahmad Tarmizi Che Has, Mary Chebib
GABAA receptors (GABAARs) are members of the Cys-loop ligand-gated ion channel (LGIC) superfamily, which includes nicotinic acetylcholine, glycine, and serotonin (5HT3) receptors [1,2,3,4]. LGICs typically mediate fast synaptic transmission via the movement of ions through channels gated by neurotransmitters, such as acetylcholine for nicotinic receptors and GABA for GABAARs [5]. The term Cys-loop receptors originates from the presence of a conserved disulphide bond (or bridge) which holds together two cysteine amino acids of the loop that forms from the structure of polypeptides in the extracellular domain of the receptor's subunit [6]...
May 15, 2018: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/29758302/plasminogen-binding-inhibitors-demonstrate-unwanted-activities-on-gaba-a-and-glycine-receptors-in-human-ipsc-derived-neurons
#3
Lisbeth Kristensson, Anders Lundin, David Gustafsson, Jan Fryklund, Tomas Fex, Delsing Louise, Erik Ryberg
Plasminogen binding inhibitors (PBIs) reduce the risk of bleeding in hemorrhagic conditions. However, generic PBIs are also associated with an increased risk of seizures, an adverse effect linked to unwanted activities towards inhibitory neuronal receptors. Development of novel PBIs serve to remove compounds with such properties, but progress is limited by a lack of higher throughput methods with human translatability. Herein we apply human induced pluripotent stem cell (hiPSC) derived neurons in combination with dynamic mass redistribution (DMR) technology to demonstrate robust and reproducible modulation of both GABAA and glycine receptors...
May 11, 2018: Neuroscience Letters
https://www.readbyqxmd.com/read/29758086/cholinergic-excitation-complements-glutamate-in-coding-visual-information-in-retinal-ganglion-cells
#4
Santhosh Sethuramanujam, Gautam B Awatramani, Malcolm M Slaughter
Starburst amacrine cells release GABA and acetylcholine This study explores the coordinated function of starburst mediated cholinergic excitation and GABAergic inhibition to bistratified retinal ganglion cells, predominantly direction-selective ganglion cells (DSGCs) In rat retina, under our recording conditions, starbursts were found to provide the major excitatory drive to a sub-population of ganglion cells whose dendrites co-stratify with starburst dendrites (putative DSGCs) In mouse retina, recordings from genetically identified DSGCs at physiological temperatures reveal that ACh inputs dominate the response to small spot-high contrast light stimuli, with preferential addition of bipolar cell input shifting the balance towards glutamate for larger spot stimuli In addition, starbursts also appear to gate glutamatergic excitation to DSGCs by postsynaptic and possibly presynaptic inhibitory processes ABSTRACT: Starburst amacrine cells release both GABA and acetylcholine (ACh), allowing them to simultaneously mediate inhibition and excitation...
May 14, 2018: Journal of Physiology
https://www.readbyqxmd.com/read/29743978/clarified-a%C3%A3-a%C3%A3-euterpe-oleracea-juice-as-an-anticonvulsant-agent-in-vitro-mechanistic-study-of-gabaergic-targets
#5
Gabriela P F Arrifano, Mathieu P Lichtenstein, José Rogério Souza-Monteiro, Marcelo Farina, Hervé Rogez, José Carlos Tavares Carvalho, Cristina Suñol, Maria Elena Crespo-López
Seizures affect about 50 million people around the world. Approximately 30% of seizures are refractory to the current pharmacological arsenal, so, the pursuit of new therapeutic alternatives is essential. Clarified Euterpe oleracea (EO) juice showed anticonvulsant properties similar to diazepam in an in vivo model with pentylenetetrazol, a GABAA receptor blocker. This study investigated the effects of EO on the main GABAergic targets for anticonvulsant drugs, analyzing the effect on the GABA receptor's benzodiazepine and picrotoxinin binding sites and the GABA uptake...
2018: Oxidative Medicine and Cellular Longevity
https://www.readbyqxmd.com/read/29729247/ionic-plasticity-and-pain-the-loss-of-descending-serotonergic-fibers-after-spinal-cord-injury-transforms-how-gaba-affects-pain
#6
Yung-Jen Huang, James W Grau
Activation of pain (nociceptive) fibers can sensitize neural circuits within the spinal cord, inducing an increase in excitability (central sensitization) that can foster chronic pain. The development of spinally-mediated central sensitization is regulated by descending fibers and GABAergic interneurons. In adult animals, the co-transporter KCC2 maintains a low intracellular concentration of the anion Cl- . As a result, when the GABA-A receptor is engaged, Cl- flows in the neuron which has a hyperpolarizing (inhibitory) effect...
May 2, 2018: Experimental Neurology
https://www.readbyqxmd.com/read/29720938/isolation-and-characterization-of-two-new-secondary-metabolites-from-quercus-incana-and-their-antidepressant-and-anxiolytic-like-potential
#7
Rizwana Sarwar, Umar Farooq, Sadia Naz, Ajmal Khan, Syed M Bukhari, Haroon Khan, Nasiara Karim, Imran Khan, Ayaz Ahmed, Ahmed Al-Harrasi
The ethyl acetate fraction of Quercus incana yielded two new compounds [ 1 and 2 ]. The characterization and structure elucidation of these compounds were carried out through various spectroscopic techniques such as mass spectrometry along with one- and two-dimensional NMR techniques. The structural formula was deduced to be 2-(4-hydroxybutan-2-yl)-5-methoxyphenol [ 1 ] and 4-hydroxy-3-(hydroxymethyl) pentanoic acid [ 2 ]. The elevated plus maze (EPM) and light-dark box (LDB) tests (classical mouse models) were performed in order to reveal the anxiolytic potential of both compounds [ 1 and 2 ]...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29720564/evidence-that-sedative-effects-of-benzodiazepines-involve-unexpected-gaba-a-receptor-subtypes-quantitative-observation-studies-in-rhesus-monkeys
#8
Angela N Duke, Zhiqiang Meng, Donna M Platt, John R Atack, Gerard R Dawson, David S Reynolds, V V N Phani Babu Tiruveedhula, Guanguan Li, Michael Rajesh Stephen, Werner Sieghart, James M Cook, James K Rowlett
Using non-human primates, we introduced a new set of behavioral categories for observable sedative effects based on pediatric anesthesiology classifications. We examined the effects of alprazolam and diazepam (non-selective benzodiazepines), zolpidem (preferential binding to α1 subunit-containing GABAA receptors), HZ-166 (8-ethynyl-6-(2'-pyridine)-4H-2,5,10b-triaza-benzo[e]azulene-3-carboxylic acid ethyl ester; functionally selective for α2 and α3 subunit-containing GABAA receptors), MRK-696 (7-cyclobutyl-6-(2-methyl-2H-1,2,4-triazol-2-ylmethoxy)-3-(2-flurophenyl)-1,2,4-triazolo(4,3-b)pyridazine; no selectivity but partial intrinsic activity), and TPA023B (6,2'-difluro-5'-(3-(1-hydroxy-1-methylethyl)imidazo(1,2-b((1,2,4)triazin-7-yl)(1,1'-biphenyl)-2-carbonitrile; selectivity for α2, α3, α5 subunit-containing GABAA receptors) using quantitative behavioral observation techniques in rhesus monkeys...
May 2, 2018: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29704480/protective-effect-and-mechanism-of-injection-of-glutamate-into-cerebellum-fastigial-nucleus-on-chronic-visceral-hypersensitivity-in-rats
#9
Ling-Ling Zhen, Bei Miao, Ying-Ying Chen, Zhen Su, Man-Qiu Xu, Sujuan Fei, Jianfu Zhang
AIMS: We investigated the effects of chemical stimulation of cerebellum fastigial nucleus (FN) on the chronic visceral hypersensitivity (CVH) and its possible mechanism in rats. MAIN METHODS: We stimulated the FN by microinjecting glutamate into the FN, in order to explore whether the cerebellum fastigial nucleus played a role on CVH in rat. The model of CVH was established by colorectal distension (CRD) in neonatal rats. Abdominal withdrawal reflex (AWR) scores, pain threshold, and amplitude of electromyography (EMG) were used to assess the hyperalgesia...
April 25, 2018: Life Sciences
https://www.readbyqxmd.com/read/29681797/electroacupuncture-potentiates-cannabinoid-receptor-mediated-descending-inhibitory-control-in-a-mouse-model-of-knee-osteoarthritis
#10
Xiao-Cui Yuan, Bing Zhu, Xiang-Hong Jing, Li-Ze Xiong, Cai-Hua Wu, Fang Gao, Hong-Ping Li, Hong-Chun Xiang, He Zhu, Bin Zhou, Wei He, Chuan-You Lin, Hui-Lin Pan, Qiang Wang, Man Li
Knee osteoarthritis (KOA) is a highly prevalent, chronic joint disorder, which can lead to chronic pain. Although electroacupuncture (EA) is effective in relieving chronic pain in the clinic, the involved mechanisms remain unclear. Reduced diffuse noxius inhibitory controls (DNIC) function is associated with chronic pain and may be related to the action of endocannabinoids. In the present study, we determined whether EA may potentiate cannabinoid receptor-mediated descending inhibitory control and inhibit chronic pain in a mouse model of KOA...
2018: Frontiers in Molecular Neuroscience
https://www.readbyqxmd.com/read/29627342/blockade-of-%C3%AE-2-adrenergic-or-metabotropic-glutamate-receptors-induces-glutamate-release-in-the-locus-coeruleus-to-activate-descending-inhibition-in-rats-with-chronic-neuropathic-hypersensitivity
#11
Ken-Ichiro Hayashida, Masafumi Kimuram, James C Eisenach
Locus coeruleus (LC)-spinal noradrenergic projections are important to endogenous analgesic mechanisms and can be activated by local glutamate signaling in the LC. The current study examined the local glutamatergic, GABAergic, and noradrenergic influences on glutamate release in the LC and noradrenergic descending inhibition in rats 6 weeks after spinal nerve ligation (SNL). Intra-LC injection of the α2 adrenoceptor antagonist idazoxan or the group 2 metabotropic glutamate receptor (mGluR) antagonist (RS)-α-Methyl-4-tetrazolylphenylglycine (MTPG) increased withdrawal thresholds in SNL animals and this was reversed by the blockade of α-amino-3-hydroxy-5-methyl- 4-isoxazolepropionic acid (AMPA) receptors in the LC or α2-adrenoceptors in the spinal cord, but not in normal animals...
April 5, 2018: Neuroscience Letters
https://www.readbyqxmd.com/read/29590745/high-frequency-stimulation-of-the-subthalamic-nucleus-activates-motor-cortex-pyramidal-tract-neurons-by-a-process-involving-local-glutamate-gaba-and-dopamine-receptors-in-hemi-parkinsonian-rats
#12
Chi-Fen Chuang, Chen-Wei Wu, Ying Weng, Pei-San Hu, Shin-Rung Yeh, Yen-Chung Chang
Deep brain stimulation (DBS) is widely used to treat advanced Parkinson’s disease. Here, we investigated how DBS applied on the subthalamic nucleus (STN) influenced the neural activity in the motor cortex. Rats, which had the midbrain dopaminergic neurons partially depleted unilaterally, called the hemi-Parkinsonian rats, were used as a study model. c-Fos expression in the neurons was used as an indicator of neural activity. Application of high-frequency stimulation (HFS) upon the STN was used to mimic the DBS treatment...
March 29, 2018: Chinese Journal of Physiology
https://www.readbyqxmd.com/read/29571967/functional-mechanism-of-asp5736-a-selective-serotonin-5-ht-5a-receptor-antagonist-with-potential-utility-for-the-treatment-of-cognitive-dysfunction-in-schizophrenia
#13
Mayako Yamazaki, Noriyuki Yamamoto, Junko Yarimizu, Mayuko Okabe, Ai Moriyama, Masako Furutani, Monica M Marcus, Torgny H Svensson, Katsuya Harada
The 5-HT5A receptor is arguably the least understood 5-HT receptor. Despite widespread expression in human and rodent brains it lacks specific ligands. Our previous results suggest that 5-HT5A receptor antagonists may be effective against cognitive impairment in schizophrenia. In this study, using behavioral, immunohistochemical, electrophysiological and microdialysis techniques, we examined the mechanism by which ASP5736, a novel and selective 5-HT5A receptor antagonist, exerts a positive effect in animal models of cognitive impairment...
March 20, 2018: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/29565038/gabaergic-inhibitory-neurons-as-therapeutic-targets-for-cognitive-impairment-in-schizophrenia
#14
REVIEW
Meng-Yi Xu, Albert H C Wong
Schizophrenia is considered primarily as a cognitive disorder. However, functional outcomes in schizophrenia are limited by the lack of effective pharmacological and psychosocial interventions for cognitive impairment. GABA (gamma-aminobutyric acid) interneurons are the main inhibitory neurons in the central nervous system (CNS), and they play a critical role in a variety of pathophysiological processes including modulation of cortical and hippocampal neural circuitry and activity, cognitive function-related neural oscillations (eg, gamma oscillations) and information integration and processing...
March 22, 2018: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29561882/effect-of-developmental-nmdar-antagonism-with-cgp-39551-on-aspartame-induced-hypothalamic-and-adrenal-gene-expression
#15
Kate S Collison, Angela Inglis, Sherin Shibin, Soad Saleh, Bernard Andres, Rosario Ubungen, Jennifer Thiam, Princess Mata, Futwan A Al-Mohanna
RATIONALE: Aspartame (L-aspartyl phenylalanine methyl ester) is a non-nutritive sweetener (NNS) approved for use in more than 6000 dietary products and pharmaceuticals consumed by the general public including adults and children, pregnant and nursing mothers. However a recent prospective study reported a doubling of the risk of being overweight amongst 1-year old children whose mothers consumed NNS-sweetened beverages daily during pregnancy. We have previously shown that chronic aspartame (ASP) exposure commencing in utero may detrimentally affect adulthood adiposity status, glucose metabolism and aspects of behavior and spatial cognition, and that this can be modulated by developmental N-methyl-D-aspartate receptor (NMDAR) blockade with the competitive antagonist CGP 39551 (CGP)...
2018: PloS One
https://www.readbyqxmd.com/read/29561292/behavioral-effects-of-toll-like-receptor-4-antagonist-eritoran-in-an-experimental-model-of-depression-role-of-prefrontal-and-hippocampal-neurogenesis-and-%C3%AE-aminobutyric-acid-glutamate-balance
#16
Sawsan Aboul-Fotouh, Mohamed Habib, Tarek Asaad, Samar K Kassim, Mohamed H Ghanem
Depression is the disease of the modern era. The lack of response to the available antidepressants, which were developed on the basis of the monoaminergic deficit hypothesis of depression, has encouraged scientists to think about new mechanisms explaining the pathogenesis of depression. In this context, the inflammatory theory has emerged to clarify many aspects of depression that the previous theories have failed to explain. Toll-like receptor-4 (TLR-4) has a regulatory role in the brain's immune response to stress, and its activation is suggested to play a pivotal role in the pathophysiology of depression...
March 20, 2018: Behavioural Pharmacology
https://www.readbyqxmd.com/read/29559911/vortioxetine-treatment-reverses-subchronic-pcp-treatment-induced-cognitive-impairments-a-potential-role-for-serotonin-receptor-mediated-regulation-of-gaba-neurotransmission
#17
Alan L Pehrson, Christian S Pedersen, Kirstine Sloth Tølbøl, Connie Sanchez
Major depressive disorder (MDD) is associated with cognitive impairments that may contribute to poor functional outcomes. Clinical data suggests that the multimodal antidepressant vortioxetine attenuates some cognitive impairments in MDD patients, but the mechanistic basis for these improvements is unclear. One theory suggests that vortioxetine improves cognition by suppressing γ-amino butyric acid (GABA)ergic neurotransmission, thereby increasing glutamatergic activation. Vortioxetine's effects on cognition, GABA and glutamate neurotransmission have been supported in separate experiments, but no empirical work has directly connected vortioxetine's cognitive effects to those on GABA and glutamate neurotransmission...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29559893/gaba-and-gap-junctions-in-the-development-of-synchronized-activity-in-human-pluripotent-stem-cell-derived-neural-networks
#18
Meeri Eeva-Liisa Mäkinen, Laura Ylä-Outinen, Susanna Narkilahti
The electrical activity of the brain arises from single neurons communicating with each other. However, how single neurons interact during early development to give rise to neural network activity remains poorly understood. We studied the emergence of synchronous neural activity in human pluripotent stem cell (hPSC)-derived neural networks simultaneously on a single-neuron level and network level. The contribution of gamma-aminobutyric acid (GABA) and gap junctions to the development of synchronous activity in hPSC-derived neural networks was studied with GABA agonist and antagonist and by blocking gap junctional communication, respectively...
2018: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/29559416/music-therapy-inhibits-morphine-seeking-behavior-via-gaba-receptor-and-attenuates-anxiety-like-behavior-induced-by-extinction-from-chronic-morphine-use
#19
Ki Jin Kim, Sang Nam Lee, Bong Hyo Lee
RATIONALE: Morphine is a representative pain killer. However, repeated use tends to induce addiction. Music therapy has been gaining interest as a useful type of therapy for neuropsychiatric diseases. OBJECTIVES: The present study examined whether Korean traditional music (KT) could suppress morphine-seeking behavior and anxiety-like behavior induced by extinction from chronic morphine use and additionally investigated a possible neuronal mechanism. MATERIAL & METHODS: Male Sprague-Dawley rats were trained to intravenously self-administer morphine hydrochloride (1...
March 17, 2018: Neuroscience Letters
https://www.readbyqxmd.com/read/29556714/pharmacological-profile-of-vestibular-inhibitory-inputs-to-superior-oblique-motoneurons
#20
Parthena Soupiadou, Francisco Branoner, Hans Straka
Vestibulo-ocular reflexes (VOR) are mediated by three-neuronal brainstem pathways that transform semicircular canal and otolith sensory signals into motor commands for the contraction of spatially specific sets of eye muscles. The vestibular excitation and inhibition of extraocular motoneurons underlying this reflex is reciprocally organized and allows coordinated activation of particular eye muscles and concurrent relaxation of their antagonistic counterparts. Here, we demonstrate in isolated preparations of Xenopus laevis tadpoles that the discharge modulation of superior oblique motoneurons during cyclic head motion derives from an alternating excitation and inhibition...
March 19, 2018: Journal of Neurology
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