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Gaba a antagonist

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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
#1
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
#2
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/28890150/antagonizing-the-gabaa-receptor-during-behavioral-training-improves-spatial-memory-at-different-doses-in-control-and-chronically-stressed-rats
#3
Kenji J Nishimura, J Bryce Ortiz, Cheryl D Conrad
Chronic stress leads to a dysregulated inhibitory tone that could impact hippocampal-dependent spatial learning and memory. The present study examined whether spatial memory deficits resulting from chronic stress could be overcome by antagonizing the GABAA receptor, a prominent inhibitory receptor of GABA in the hippocampus. Young adult male Sprague-Dawley rats were chronically stressed (STR, wire mesh restraint, 6h/d/21d) or placed in a no-stress control group (CON). When chronic restraint ended, rats were tested on a 2-trial object placement (OP) task at a delay (3hr) that would result in chance performance without intervention and then on novel object recognition (NOR) and the elevated plus maze (EPM) to assess non-spatial memory and anxiety profile...
September 7, 2017: Neurobiology of Learning and Memory
https://www.readbyqxmd.com/read/28881444/gabaergic-inhibition-gates-excitatory-ltp-in-perirhinal-cortex
#4
Vibhakar C Kotak, Ana Mirallave, Todd M Mowery, Dan H Sanes
The perirhinal cortex (PRh) is a key region downstream of auditory cortex (ACx) that processes familiarity linked mnemonic signaling. In gerbils, ACx-driven EPSPs recorded in PRh neurons are largely shunted by GABAergic inhibition (Kotak et al. 2015). To determine whether inhibitory shunting prevents the induction of excitatory long-term potentiation (e-LTP), we stimulated ACx-recipient PRh in a brain slice preparation using theta burst stimulation (TBS). Under control conditions, without GABA blockers, the majority of PRh neurons exhibited long-term depression...
September 7, 2017: Hippocampus
https://www.readbyqxmd.com/read/28877214/direct-versus-indirect-actions-of-ghrelin-on-hypothalamic-npy-neurons
#5
Hiroshi Hashiguchi, Zhenyu Sheng, Vanessa Routh, Volodymyr Gerzanich, J Marc Simard, Joseph Bryan
OBJECTIVES: Assess direct versus indirect action(s) of ghrelin on hypothalamic NPY neurons. MATERIALS AND METHODS: Electrophysiology was used to measure ion channel activity in NPY-GFP neurons in slice preparations. Ca2+ imaging was used to monitor ghrelin activation of isolated NPY GFP-labeled neurons. Immunohistochemistry was used to localize Trpm4, SUR1 and Kir6.2 in the hypothalamus. RESULTS: Acylated ghrelin depolarized the membrane potential (MP) of NPY-GFP neurons in brain slices...
2017: PloS One
https://www.readbyqxmd.com/read/28870570/effects-of-naftopidil-on-inhibitory-transmission-in-substantia-gelatinosa-neurons-of-the-rat-spinal-dorsal-horn-in-vitro
#6
Daisuke Uta, Du-Jie Xie, Tsuyoshi Hattori, Ken-Ichi Kasahara, Megumu Yoshimura
OBJECTIVE: Naftopidil is used clinically for the treatment of voiding disorders in benign prostatic hyperplasia. Previous in vivo experiments in which naftopidil was applied intrathecally abolished rhythmic bladder contraction, suggesting that naftopidil might inhibit a voiding reflex through interaction with spinal dorsal horn neurons. Here we aimed to clarify the mechanism of action of naftopidil on dorsal horn neurons. METHODS: Whole-cell patch-clamp recordings were performed using substantia gelatinosa neurons of adult rat spinal cord slices...
September 15, 2017: Journal of the Neurological Sciences
https://www.readbyqxmd.com/read/28865483/suppression-of-cortical-seizures-by-optic-stimulation-of-the-reticular-thalamus-in-pv-mhchr2-yfp-bac-transgenic-mice
#7
Wei Jen Chang, Wei Pang Chang, Bai Chuang Shyu
Deep brain stimulation in thalamic regions has been proposed as a treatment for epilepsy. The electrical current excites thalamocortical activity which is controlled by γ-aminobutyric acid (GABA)ergic interneurons in the reticular thalamic nucleus (nRT). Previous studies showed that enhancing GABAergic inhibitory strength in the nRT reduces the duration and power of seizures, indicating that the thalamus plays an important role in modulating cortical seizures. The aim of the present study was to apply optogenetics to study the role of the nRT in modulating cortical seizures...
September 2, 2017: Molecular Brain
https://www.readbyqxmd.com/read/28856406/panicolytic-like-effects-caused-by-substantia-nigra-pars-reticulata-pretreatment-with-low-doses-of-endomorphin-1-and-high-doses-of-ctop-or-the-nop-receptors-antagonist-jtc-801-in-male-rattus-norvegicus
#8
Juliana Almeida da Silva, Audrey Franceschi Biagioni, Rafael Carvalho Almada, Renato Leonardo de Freitas, Norberto Cysne Coimbra
RATIONALE: Gamma-aminobutyric acid (GABA)ergic neurons of the substantia nigra pars reticulata (SNpr) are connected to the deep layers of the superior colliculus (dlSC). The dlSC, in turn, connect with the SNpr through opioid projections. Nociceptin/orphanin FQ peptide (N/OFQ) is a natural ligand of a Gi protein-coupled nociceptin receptor (ORL1; NOP) that is also found in the SNpr. Our hypothesis is that tectonigral opioid pathways and intranigral orphanin-mediated mechanisms modulate GABAergic nigrotectal connections...
August 30, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28853438/periaqueductal-gray-glutamatergic-transmission-governs-chronic-stress-induced-depression
#9
Yu-Cheng Ho, Tzer-Bin Lin, Ming-Chun Hsieh, Cheng-Yuan Lai, Dylan Chou, Yat-Pang Chau, Gin-Den Chen, Hsien-Yu Peng
The mechanisms underlying chronic stress-induced dysfunction of glutamatergic transmission that contribute to helplessness-associated depressive disorder are unknown. We investigated the relationship of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors and stress, and the neuroplastic changes of stress-induced depression-like behavior in the ventrolateral periaqueductal gray (vlPAG). We conducted whole-cell patch-clamp electrophysiological recordings in the vlPAG neurons. Depression-like behavior was assayed using tail suspension test and sucrose preference test...
August 30, 2017: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28840535/chronic-exposure-to-%C3%AE-alanine-generates-oxidative-stress-and-alters-energy-metabolism-in-cerebral-cortex-and-cerebellum-of-wistar-rats
#10
Tanise Gemelli, Rodrigo Binkowski de Andrade, Denise Bertin Rojas, Ângela Zanatta, Gabriel Henrique Schirmbeck, Cláudia Funchal, Moacir Wajner, Carlos Severo Dutra-Filho, Clovis Milton Duval Wannmacher
β-Alanine occurs naturally in the human central nervous system and performs different functions. It can act as either a neurotransmitter or a neuromodulator, depletion of taurine levels and competitive antagonist of γ-aminobutyric acid (GABA). The β-amino acid accumulation exerts an important biological function as delay in brain development, oxidative stress and disturbances in energy metabolism, characterized as an inborn error of metabolism classified as β-alaninemia. We evaluated the effects of the chronic administration of β-alanine on some parameters of oxidative stress and enzymes of energy metabolism in cerebral cortex and cerebellum of 21-day-old Wistar rats...
August 24, 2017: Molecular Neurobiology
https://www.readbyqxmd.com/read/28839004/ventilation-and-neurochemical-changes-during-%C3%A2%C2%B5-opioid-receptor-activation-or-blockade-of-excitatory-receptors-in-the-hypoglossal-motor-nucleus-of-goats
#11
Thomas M Langer, Suzanne E Neumueller, Emma Crumley, Nicholas J Burgraff, Sawan Talwar, Matthew Robert Hodges, Lawrence G Pan, Hubert V Forster
Neuromodulator interdependence posits that changes in one or more neuromodulators are compensated by changes in other modulators to maintain stability in the respiratory control network. Herein, we studied compensatory neuromodulation in the hypoglossal motor nucleus (HMN) after chronic implantation of microtubules unilaterally (n=5) or bilaterally (n=5) into the HMN. After recovery, receptor agonists or antagonists in mock cerebrospinal fluid (mCSF) were dialyzed during the awake and NREM sleep state. During day studies, dialysis of the µ-opioid inhibitory receptor agonist DAMGO (100 µM) decreased pulmonary ventilation (V̇I), breathing frequency (f), and genioglossus (GG) muscle activity, but did not alter neuromodulators measured in the effluent mCSF...
August 24, 2017: Journal of Applied Physiology
https://www.readbyqxmd.com/read/28838986/ammonia-modifies-enteric-neuromuscular-transmission-through-glial-gamma-aminobutyric-acid-signaling
#12
David E Fried, Ralph E Watson, Simon C Robson, Brian D Gulbransen
OBJECTIVE: Impaired gut motility may contribute, at least in part, to the development of systemic hyperammonemia and systemic neurological disorders in inherited metabolic disorders, or in severe liver and renal disease. It is not known whether enteric neurotransmission regulates intestinal luminal and hence systemic ammonia levels by induced changes in motility. DESIGN: Here, we propose and test the hypothesis that ammonia acts through specific enteric circuits to influence gut motility...
August 24, 2017: American Journal of Physiology. Gastrointestinal and Liver Physiology
https://www.readbyqxmd.com/read/28828402/neuregulin-and-dopamine-d4-receptors-contribute-independently-to-depotentiation-of-schaffer-collateral-ltp-by-temperoammonic-path-stimulation
#13
Yukitoshi Izumi, Charles F Zorumski
Prior studies have found that dopamine (DA), acting at D4 receptors, and neuregulin (NRG), likely acting at ErbB4 receptors, are involved in a form of depotentiation of long-term potentiation (LTP) at Schaffer collateral (SC) synapses in the hippocampus. Furthermore, DA and NRG actions are intertwined in that NRG induces DA release. We previously found that low-frequency stimulation (LFS) of temperoammonic (TA) inputs to area CA1 also depotentiates previously established SC LTP through a complex signaling pathway involving endocannabinoids, GABA, adenosine, and mitogen-activated protein kinases (MAPKs), but not glutamate...
July 2017: ENeuro
https://www.readbyqxmd.com/read/28827179/oligodendrocyte-progenitor-cells-are-paired-with-gaba-neurons-in-the-mouse-dorsal-cortex-unbiased-stereological-analysis
#14
Jenna J Boulanger, Claude Messier
Oligodendrocyte progenitor cells (OPC) are glial cells that differentiate into myelinating oligodendrocytes during early stages of post-natal life. However, OPCs persist beyond developmental myelination and represent an important population of cycling cells in the gray and white matter of the adult brain. While adult OPCs form unique territories that are maintained through self-avoidance, some cortical OPCs appear to position their cell body very close to that of a neuron, forming what are known as OPC-neuron pairs...
August 18, 2017: Neuroscience
https://www.readbyqxmd.com/read/28818421/erbb-signaling-antagonist-ameliorates-behavioral-deficit-induced-by-phencyclidine-pcp-in-mice-without-affecting-metabolic-syndrome-markers
#15
Hagar Tadmor, Idit Golani, Ravid Doron, Ilana Kremer, Alon Shamir
Schizophrenia is a severe syndrome that affects about 1% of the world population. Since the mid-1950s, antipsychotics have been used to treat schizophrenia with preference for treating positive symptoms; however, their tolerance level is low, there are numerous side effects, and only some patients respond to the treatment. Antipsychotic medications that are more effective, better tolerated, and with fewer adverse effects are urgently needed. Given the accumulating evidence of the role filled by the ErbB signaling network in the biology of the dopamine, GABA, and glutamate systems, and in the etiology of schizophrenia, we hypothesized that the ErbB network is a candidate for development of a novel agent through which various symptoms of schizophrenia and other psychiatric disorders might be treated...
August 14, 2017: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/28818303/nkcc1-chloride-importer-antagonists-attenuate-many-neurological-and-psychiatric-disorders
#16
REVIEW
Yehezkel Ben-Ari
In physiological conditions, adult neurons have low intracellular Cl(-) [(Cl(-))I] levels underlying the γ-aminobutyric acid (GABA)ergic inhibitory drive. In contrast, neurons have high (Cl(-))I levels and excitatory GABA actions in a wide range of pathological conditions including spinal cord lesions, chronic pain, brain trauma, cerebrovascular infarcts, autism, Rett and Down syndrome, various types of epilepsies, and other genetic or environmental insults. The diuretic highly specific NKCC1 chloride importer antagonist bumetanide (PubChem CID: 2461) efficiently restores low (Cl(-))I levels and attenuates many disorders in experimental conditions and in some clinical trials...
August 14, 2017: Trends in Neurosciences
https://www.readbyqxmd.com/read/28808187/g-aminobutyric-acid-promotes-methionine-choline-deficient-diet-induced-nonalcoholic-steatohepatitis
#17
Yoon Seok Roh, Ara Cho, Zixiong Zhou, Hyuneui Jeong, Jeong-Eun Park, Youn-Soo Cha, Suk-Heung Oh, Chae-Woong Lim, Bumseok Kim
Nonalcoholic steatohepatitis (NASH) is one of the most common liver diseases and a major cause of liver fibrosis worldwide. G-Aminobutyric acid (GABA) is one of the most abundant inhibitory neurotransmitters in the central nervous system. Recently, it has been reported that GABAergic signaling pathways are found in various non-neuronal tissues including the immune system and play a functional role. In the present study, we investigated whether administration of GABA has effects on NASH through its immunomodulatory effects...
October 17, 2016: Journal of Biomedical Research
https://www.readbyqxmd.com/read/28807671/selective-inhibition-of-extra-synaptic-%C3%AE-5-gabaa-receptors-by-s44819-a-new-therapeutic-agent
#18
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/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
#19
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/28777177/chronic-insomnia-disorder
#20
Alon Y Avidan, David N Neubauer
PURPOSE OF REVIEW: Neurologists, along with all health care providers, commonly encounter patients with insomnia, which is a condition that impacts patients' underlying neurologic conditions in a bidirectional manner. While chronic insomnia is one of the most common sleep disturbances, only a small proportion of individuals with this condition discuss their sleep problems with their providers. When insomnia is described, it is more often in relationship to another medical problem, as opposed to an independent condition...
August 2017: Continuum: Lifelong Learning in Neurology
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