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Gabaa antagonist

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https://www.readbyqxmd.com/read/28099880/modifications-of-inhibitory-transmission-onto-pyramidal-neurons-by-postnatal-exposure-to-mk-801-effects-of-enriched-environment
#1
Amir Shojaei, Afsaneh Kamali Anaraki, Javad Mirnajafi-Zadeh, Nafiseh Atapour
Early enriched environment (EE) prevents several deficits associated with postnatal MK-801 [N-Methyl-D-Aspartate (NMDA) receptor antagonist] treatment such as cognitive and locomotor deficits. We sought physiological correlates to such changes by looking at inhibitory synaptic inputs onto pyramidal cells in a prefrontal cortex slice preparation. Pharmacologically isolated γ-amino-butyric acid A (GABAA) receptor-mediated currents were measured using whole-cell patch clamp recordings. Wistar rats were raised in standard or EE from birth up to the time of experiments and were injected with saline or MK-801 (1mg/kg) on postnatal days (P) 6-10...
January 15, 2017: International Journal of Developmental Neuroscience
https://www.readbyqxmd.com/read/28071892/transient-adenosine-release-is-modulated-by-nmda-and-gabab-receptors
#2
Michael D Nguyen, Ying Wang, Mallikarjunarao Ganesana, B Jill Venton
Adenosine is a neuroprotective agent that modulates neurotransmission and is modulated by other neurotransmitters. Spontaneous, transient adenosine is a recently discovered mode of signaling where adenosine is released and cleared from the extracellular space quickly, in less than three seconds. Spontaneous adenosine release is regulated by adenosine A1 and A2a receptors, but regulation by other neurotransmitter receptors has not been studied. Here, we examined the effect of glutamate and GABA receptors on the concentration and frequency of spontaneous, transient adenosine release by measuring adenosine with fast-scan cyclic voltammetry in the rat caudate-putamen...
January 10, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28066142/participation-of-central-gabaa-receptors-in-the-trigeminal-processing-of-mechanical-allodynia-in-rats
#3
Min Ji Kim, Young Hong Park, Kui Ye Yang, Jin Sook Ju, Yong Chul Bae, Seong Kyu Han, Dong Kuk Ahn
Here we investigated the central processing mechanisms of mechanical allodynia and found a direct excitatory link with low-threshold input to nociceptive neurons. Experiments were performed on male Sprague-Dawley rats weighing 230-280 g. Subcutaneous injection of interleukin 1 beta (IL-1β) (1 ng/10 µL) was used to produce mechanical allodynia and thermal hyperalgesia. Intracisternal administration of bicuculline, a gamma aminobutyric acid A (GABAA) receptor antagonist, produced mechanical allodynia in the orofacial area under normal conditions...
January 2017: Korean Journal of Physiology & Pharmacology
https://www.readbyqxmd.com/read/28065795/rational-identification-of-a-novel-soy-derived-anxiolytic-like-undecapeptide-acting-via-gut-brain-axis-after-oral-administration
#4
Ami Ota, Akane Yamamoto, Saeko Kimura, Yukiha Mori, Takafumi Mizushige, Yoshiki Nagashima, Masaru Sato, Hideyuki Suzuki, Saori Odagiri, Daisuke Yamada, Masayuki Sekiguchi, Keiji Wada, Ryuhei Kanamoto, Kousaku Ohinata
Here we found that the chymotryptic digest of soy β-conglycinin, a major storage protein, exhibited anxiolytic-like effects in mice. We then searched for anxiolytic-like peptides in the digest. Based on a comprehensive peptide analysis of the chymotryptic digest by high performance liquid chromatograph connected to an LTQ Orbitrap mass spectrometer and the structure-activity relationship of known peptides, we explored anxiolytic-like peptides present in the digest. FLSSTEAQQSY, which corresponds to 323-333 of the β-conglycinin α subunit [βCGα(323-333)] emerged as a candidate...
January 5, 2017: Neurochemistry International
https://www.readbyqxmd.com/read/28032294/examination-of-the-role-of-nmda-and-gabaa-receptors-in-the-effects-of-hyperbaric-oxygen-on-striatal-dopamine-levels-in-rats
#5
C Lavoute, M Weiss, J J Risso, J C Rostain
Hyperbaric oxygen induced in rats a decrease in striatal dopamine levels. Such decrease could be a result of changes in glutamatergic and GABAergic controls of the dopaminergic neurons into the Substantia Nigra Pars Compacta. The aim of this study was to determine the role of gluatamatergic and Gama-Amino-Butyric-Acid neurotransmissions in this alteration. Dopamine-sensitive electrodes were implanted into the striatum under general anesthesia. After one week rest, awaked rats were exposed to oxygen-nitrogen mixture at a partial pressure of oxygen of 3 absolute atmospheres...
December 28, 2016: Neurochemical Research
https://www.readbyqxmd.com/read/28012732/gabaergic-control-of-neostriatal-dopamine-d2-receptor-binding-and-behaviors-in-the-rat
#6
Susanne Nikolaus, Markus Beu, Maria Angelica de Souza Silva, Joseph P Huston, Christina Antke, Hans-Wilhelm Müller, Hubertus Hautzel
PURPOSE: The present study assessed the influence of the GABAA receptor agonist muscimol and the GABAA receptor antagonist bicuculline on neostriatal dopamine D2 receptor binding in relation to motor and exploratory behaviors in the rat. METHODS: D2 receptor binding was measured in baseline and after challenge with either 1mg/kg muscimol or 1mg/kg bicuculline. In additional rats, D2 receptor binding was measured after injection of saline. After treatment with muscimol, bicuculline and saline, motor and exploratory behaviors were assessed for 30min in an open field prior to administration of [(123)I]S-3-iodo-N-(1-ethyl-2-pyrrolidinyl)methyl-2-hydroxy-6-methoxybenzamide ([(123)I]IBZM)...
December 21, 2016: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/28009294/synaptic-specializations-support-frequency-independent-purkinje-cell-output-from-the-cerebellar-cortex
#7
Josef Turecek, Skyler L Jackman, Wade G Regehr
The output of the cerebellar cortex is conveyed to the deep cerebellar nuclei (DCN) by Purkinje cells (PCs). Here, we characterize the properties of the PC-DCN synapse in juvenile and adult mice and find that prolonged high-frequency stimulation leads to steady-state responses that become increasingly frequency independent within the physiological firing range of PCs in older animals, resulting in a linear relationship between charge transfer and activation frequency. We used a low-affinity antagonist to show that GABAA-receptor saturation occurs at this synapse but does not underlie frequency-invariant transmission...
December 20, 2016: Cell Reports
https://www.readbyqxmd.com/read/27987210/anti-anhedonic-effect-of-selective-serotonin-reuptake-inhibitors-with-affinity-for-%C3%AF-1-receptors-in-picrotoxin-treated-mice
#8
S Hasebe, Y Ago, Y Watabe, S Oka, N Hiramatsu, T Tanaka, C Umehara, H Hashimoto, K Takuma, T Matsuda
BACKGROUND AND PURPOSE: We have previously shown that prefrontal dopamine release by the combined activation of 5-HT1A and σ1 receptors is enhanced by the GABAA receptor antagonist picrotoxin in mice. Here, we examined whether this neurochemical event is accompanied by behavioural changes. EXPERIMENTAL APPROACH: Male mice were treated with picrotoxin to decrease GABAA receptor function. Their anhedonic behaviour was measured using the female encounter test. The expression of c-Fos was determined immunohistochemically...
December 17, 2016: British Journal of Pharmacology
https://www.readbyqxmd.com/read/27986929/genetic-and-pharmacologic-manipulation-of-tlr4-has-minimal-impact-on-ethanol-consumption-in-rodents
#9
R Adron Harris, Michal Bajo, Richard L Bell, Yuri A Blednov, Florence P Varodayan, Jay Truitt, Giordano de Guglielmo, Amy W Lasek, Marian L Logrip, Leandro F Vendruscolo, Amanda J Roberts, Edward Roberts, Olivier George, Jody Mayfield, Timothy R Billiar, David J Hackam, R Dayne Mayfield, George F Koob, Marisa Roberto, Gregg E Homanics
: Toll-like receptor 4 (TLR4) is a critical component of innate immune signaling and has been implicated in alcohol responses in preclinical and clinical models. Members of the Integrative Neuroscience Initiative on Alcoholism (INIA-Neuroimmune) consortium tested the hypothesis that TLR4 mediates excessive ethanol drinking using i) Tlr4 knockout (KO) rats, ii) selective knockdown of Tlr4 mRNA in mouse nucleus accumbens (NAc), and iii) injection of the TLR4 antagonist (+)-naloxone in mice...
December 16, 2016: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/27984263/ketamine-increases-the-function-of-%C3%AE-aminobutyric-acid-type-a-receptors-in-hippocampal-and-cortical-neurons
#10
Dian-Shi Wang, Antonello Penna, Beverley A Orser
BACKGROUND: The "dissociative " general anesthetic ketamine is a well-known N-methyl-D-aspartate receptor antagonist. However, whether ketamine, at clinically relevant concentrations, increases the activity of inhibitory γ-aminobutyric acid (GABA) receptor type A (GABAA) receptors in different brain regions remains controversial. Here, the authors studied the effects of ketamine on synaptic and extrasynaptic GABAA receptors in hippocampal neurons. Ketamine modulation of extrasynaptic GABAA receptors in cortical neurons was also examined...
December 14, 2016: Anesthesiology
https://www.readbyqxmd.com/read/27940054/betaine-attenuates-memory-impairment-after-water-immersion-restraint-stress-and-is-regulated-by-the-gabaergic-neuronal-system-in-the-hippocampus
#11
Kazuo Kunisawa, Kiwamu Kido, Natsuki Nakashima, Takuya Matsukura, Toshitaka Nabeshima, Masayuki Hiramatsu
GABA mediated neuronal system regulates hippocampus-dependent memory and stress responses by controlling plasticity and neuronal excitability. Here, we demonstrate that betaine ameliorates water-immersion restraint stress (WIRS)-induced memory impairments. This improvement was inhibited by a betaine/GABA transporter-1 (GABA transporter-2: GAT2) inhibitor, NNC 05-2090. In this study, we investigated whether memory amelioration by betaine was mediated by the GABAergic neuronal system. Adult male mice were co-administered betaine and GABA receptor antagonists after WIRS...
December 7, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27924875/gabab-receptor-mediates-opposing-adaptations-of-gaba-release-from-two-types-of-prefrontal-interneurons-after-observational-fear
#12
Lei Liu, Wataru Ito, Alexei Morozov
The observational fear (OF) paradigm in rodents, in which the subject is exposed to a distressed conspecific, elicits contextual fear learning and enhances future passive avoidance learning, which may model certain behavioral traits resulting from traumatic experiences in humans. Because these behaviors affected by the OF, require dorso-medial prefrontal cortex (dmPFC), we searched for synaptic adaptations in dmPFC resulting from OF in mice by recording synaptic responses in dmPFC layer V pyramidal neurons elicited by repeated 5 Hz electrical stimulation of dmPFC layer I, or by optogenetic stimulation of specific interneurons ex vivo one day after OF...
December 7, 2016: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/27923665/nicotine-enhances-gabaergic-inhibition-of-oxytocin-mrna-expressing-neuron-in-the-hypothalamic-paraventricular-nucleus-in-vitro-in-rats
#13
Ke-Min Zhang, Guo-Yan Zhao, Bin-Bin Zhang, Qi Xu, Chun-Ping Chu, Hua Jin, De-Lai Qiu
We recently found that extracellular administration of nicotine indirectly excited hypothalamic paraventricular nucleus (PVN) corticotropin-releasing hormone (CRH) mRNA-expressing neurons. In this study, we studied the effect of nicotine on PVN oxytocin (OT) mRNA-expressing neuron in vitro in rats, by whole-cell patch-clamp recording technique, immunohistochemistry methods and single-cell reverse-transcription multiplex polymerase chain reaction (SC-RT-mPCR) methods Our results showed that 79.3% (73/92) of the 92 PVN putative magnocellular neurons co-expressed GAPDH mRNA and OT mRNA...
December 5, 2016: Neuroscience Letters
https://www.readbyqxmd.com/read/27884341/propofol-inhibits-t-helper-cell-type-2-differentiation-by-inducing-apoptosis-via-activating-gamma-aminobutyric-acid-receptor
#14
Jingxia Meng, Xin Xin, Zhen Liu, Hao Li, Bo Huang, Yuguang Huang, Jing Zhao
BACKGROUND: Propofol has been shown to attenuate airway hyperresponsiveness in asthma patients. Our previous study showed that it may alleviate lung inflammation in a mouse model of asthma. Given the critical role of T-helper cell type-2 (Th2) differentiation in asthma pathology and the immunomodulatory role of the gamma-aminobutyric acid type A (GABAA) receptor, we hypothesized that propofol could alleviate asthma inflammation by inhibiting Th2 cell differentiation via the GABA receptor...
December 2016: Journal of Surgical Research
https://www.readbyqxmd.com/read/27865151/effects-of-the-benzodiazepine-gabaa-%C3%AE-1-preferring-antagonist-3-isopropoxy-%C3%AE-carboline-hydrochloride-3-isopbc-on-alcohol-seeking-and-self-administration-in-baboons
#15
August F Holtyn, V V N Phani Babu Tiruveedhula, Michael Rajesh Stephen, James M Cook, Elise M Weerts
BACKGROUND: The major inhibitory neurotransmitter, gamma-aminobutyric acid (GABA), modulates many of the behavioral effects of alcohol, including sedation, tolerance, and withdrawal. The α1 subunit of the benzodiazepine GABAA receptor is the most widely expressed alpha subunit in the brain, and has been implicated in the reinforcing- and abuse-related effects of alcohol. The aim of the present study was to examine whether treatment with a benzodiazepine GABAA α1-preferring ligand, 3-isopropoxy-β-carboline hydrochloride (3-ISOPBC), selectively decreases alcohol seeking and consumption...
January 1, 2017: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/27860547/the-discovery-of-suvorexant-the-first-orexin-receptor-drug-for-insomnia
#16
Paul J Coleman, Anthony L Gotter, W Joseph Herring, Christopher J Winrow, John J Renger
Historically, pharmacological therapies have used mechanisms such as γ-aminobutyric acid A (GABAA) receptor potentiation to drive sleep through broad suppression of central nervous system activity. With the discovery of orexin signaling loss as the etiology underlying narcolepsy, a disorder associated with hypersomnolence, orexin antagonism emerged as an alternative approach to attenuate orexin-induced wakefulness more selectively. Dual orexin receptor antagonists (DORAs) block the activity of orexin 1 and 2 receptors to both reduce the threshold to transition into sleep and attenuate orexin-mediated arousal...
January 6, 2017: Annual Review of Pharmacology and Toxicology
https://www.readbyqxmd.com/read/27818352/exercise-combined-with-low-level-gabaa-receptor-inhibition-up-regulates-the-expression-of-neurotrophins-in-the-motor-cortex
#17
Kazuma Takahashi, Hiroshi Maejima, Gaku Ikuta, Hiroki Mani, Tadayoshi Asaka
Neurotrophins play a crucial role in neuroplasticity, neurogenesis, and neuroprotection in the central nervous system. Aerobic exercise is known to increase the expression of BDNF in the cerebral cortex. Several animal studies have evaluated the tonic inhibition of GABAergic synapses to enhance hippocampal plasticity as well as learning and memory, whereas the effects of GABAergic inhibition on plasticity in the cerebral cortex related to motor learning are not well characterized. The objective of the present study was to examine the interactive effect of low-level GABAA receptor inhibition and exercise on the expression of neurotrophins including BDNF in the murine motor cortex...
January 1, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/27780724/bicuculline-a-gabaa-receptor-antagonist-blocked-hpa-axis-activation-induced-by-ghrelin-under-an-acute-stress
#18
M S Gastón, M P Cid, N A Salvatierra
Ghrelin is a peptide of 28 amino acids with a homology between species, which acts on the central nervous system to regulate different actions, including the control of growth hormone secretion and metabolic regulation. It has been suggested that central ghrelin is a mediator of behavior linked to stress responses and induces anxiety in rodents and birds. Previously, we observed that the anxiogenic-like behavior induced by ghrelin injected into the intermediate medial mesopallium (IMM) of the forebrain was blocked by bicuculline (a GABAA receptor competitive antagonist) but not by diazepam (a GABAA receptor allosteric agonist) in neonatal meat-type chicks (Cobb)...
October 22, 2016: Behavioural Brain Research
https://www.readbyqxmd.com/read/27778437/increase-of-kcc2-in-hippocampal-synaptic-plasticity-disturbances-after-perinatal-ethanol-exposure
#19
Benoît Silvestre de Ferron, Catherine Vilpoux, Myriam Kervern, Alexandre Robert, Johan Antol, Mickael Naassila, Olivier Pierrefiche
Low to moderate perinatal ethanol exposure (PEE) may have disastrous consequences for the central nervous system resulting notably in permanent cognitive deficits. Learning and memory are mediated in the hippocampus by long-term potentiation (LTP) and long term depression (LTD), two forms of synaptic plasticity. PEE decreases LTP but also abnormally facilitates LTD (Kervern et al. ) through a presently unknown mechanism. We studied in rat hippocampus slice, the involvement of the chloride co-transporters NKCC1 and KCC2, in the role of GABAA inhibitions in facilitated LTD after moderate PEE...
October 25, 2016: Addiction Biology
https://www.readbyqxmd.com/read/27764759/6-methoxyflavanone-attenuates-mechanical-allodynia-and-vulvodynia-in-the-streptozotocin-induced-diabetic-neuropathic-pain
#20
Shehla Akbar, Fazal Subhan, Nasiara Karim, Muhammad Shahid, Nisar Ahmad, Gowhar Ali, Wajahat Mahmood, Khwaja Fawad
BACKGROUND: Diabetic neuropathy is the most prevalent, persistent and debilitating complication of diabetes mellitus often coupled with vulvodynia that may present as an isolated symptom or as a part of constellation of other neuropathic abnormalities. OBJECTIVE: Flavonoids have selective affinity for GABA receptors and 6-methoxyflavanone (6-MeOF) is a positive allosteric modulator of GABA responses at human recombinant GABAA receptors. GABAergic and opioidergic system inhibition have been shown to facilitate neuropathic pain...
December 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
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