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GABAB Receptor

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https://www.readbyqxmd.com/read/29143124/the-effect-of-inhibition-on-stimulus-specific-adaptation-in-the-inferior-colliculus
#1
Yaneri A Ayala, Manuel S Malmierca
The inferior colliculus is a center of convergence for inhibitory and excitatory synaptic inputs that may be activated simultaneously by sound stimulation. Stimulus repetition may generate response habituation by changing the efficacy of neuron's synaptic inputs. Specialized IC neurons reduce their response to repetitive tones, but restore their firing when a different and infrequent tone occurs, a phenomenon known as stimulus specific adaptation. Here, using the microiontophoresis technique, we determined the role of GABAA-, GABAB-, and glycinergic receptors in stimulus-specific adaptation (SSA)...
November 15, 2017: Brain Structure & Function
https://www.readbyqxmd.com/read/29137473/effect-of-short-and-long-term-administration-of-baclofen-on-spatial-learning-and-memory-in-rats
#2
M Holajova, M Franek
Baclofen is the only clinically available metabotropic GABAB receptor agonist. In our experiment, we tested the hypothesis that long-term baclofen administration can impair learning and memory in rats. The experiment consisted of three parts. In the first part of the study the drug was administered simultaneously with the beginning of the behavioral tests. In the second and third part of the experiment baclofen was administered daily for 14 days and for one month before the tests. In each part of the experiment, adult rats were randomly divided into four treatment groups...
November 10, 2017: Physiological Research
https://www.readbyqxmd.com/read/29131436/gabab-receptors-in-neocortical-and-hippocampal-pyramidal-neurons-are-coupled-to-different-potassium-channels
#3
Jean-Didier Breton, Greg J Stuart
Classically, GABAB receptors are thought to regulate neuronal excitability via G-protein coupled inwardly rectifying potassium (GIRK) channels. Recent data, however, indicates that GABAB receptors can also activate two-pore domain potassium channels. Here, we investigate which potassium channels are coupled to GABAB receptors in rat neocortical layer 5 and hippocampal CA1 pyramidal neurons. Bath application of the non-specific GIRK channel blocker barium (200 μM) abolished outward currents evoked by GABAB receptors in CA1 pyramidal, but only partially blocked GABAB responses in layer 5 neurons...
November 13, 2017: European Journal of Neuroscience
https://www.readbyqxmd.com/read/29115173/role-of-gabab-receptors-and-p38mapk-nf-%C3%AE%C2%BAb-pathway-in-paclitaxel-induced-apoptosis-of-hippocampal-neurons
#4
Zhao Li, Peng Liu, Hailin Zhang, Shuang Zhao, Zi Jin, Rui Li, Yuexian Guo, Xiuli Wang
CONTEXT: The effects of the anticancer drug paclitaxel on learning and memory are rarely studied. OBJECTIVE: This study investigated changes in GABAB receptor expression during paclitaxel-induced apoptosis of hippocampal neurons and the role of the p38MAPK/NF-κB pathway in this process. MATERIALS AND METHODS: Hippocampal neurons isolated from neonatal Sprague-Dawley rats were divided into six groups: Control (C), SB (10 µL of 10-µmol/L SB203580), SN (53 µg/mL SN50), N (1 µmol/L paclitaxel), SB + N (10 µmol/L SB203580 + 1 µmol/L paclitaxel) and SN + N (53 µg/mL SN50 + 1 µmol/L paclitaxel)...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/29114105/neuregulin-3-signaling-mediates-nicotine-dependent-synaptic-plasticity-in-the-orbitofrontal-cortex-and-cognition
#5
Luyi Zhou, Miranda L Fisher, Robert D Cole, Thomas J Gould, Vinay Parikh, Pavel I Ortinski, Jill R Turner
Neuregulin 3 (NRG3) and ErbB4 have been linked to nicotine addiction; however, the neuronal mechanisms and behavioral consequences of NRG3-ErbB4 sensitivity to nicotine remain elusive. Recent literature suggests that relapse to smoking is due to a lack of impulsive control, which is thought to be due to altered functioning within the orbitofrontal cortex (OFC). Therefore, we examined circuitry changes within this structure following nicotine application. We report that nicotine controls synaptic plasticity in the OFC through NRG3/ErbB4-dependent regulation of GABAergic inhibition...
November 7, 2017: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/29111036/gabab-receptor-ligand-directed-trimethyl-chitosan-tripolyphosphate-nanoparticles-and-their-pmdi-formulation-for-survivin-sirna-pulmonary-delivery
#6
Suhui Ni, Yun Liu, Yue Tang, Jing Chen, Shuhan Li, Ji Pu, Lidong Han
The effect of gene silencing by survivin siRNA (siSurvivin) on the proliferation and apoptosis of lung tumor has been attracted more interest. GABAB receptor ligand-directed nanoparticles consisting of baclofen functionalized trimethyl chitosan (Bac-TMC) as polymeric carriers, tripolyphosphate (TPP) as ionic crosslinker, and siSurvivin as therapeutic genes, were designed to enhance the survivin gene silencing. GABAB receptor agonist baclofen (Bac) was initially introduced into TMC as a novel ligand. This Bac-TMC/TPP nanoparticles increased the uptake of survivin siRNA through the interaction with GABAB receptor, further resulted in efficient cell apoptosis and gene silencing...
January 1, 2018: Carbohydrate Polymers
https://www.readbyqxmd.com/read/29106983/gabab-receptor-subtypes-differentially-regulate-thalamic-spindle-oscillations
#7
REVIEW
Daniel Ulrich, Txomin Lalanne, Martin Gassmann, Bernhard Bettler
Following the discovery of GABAB receptors by Norman Bowery and colleagues, cloning and biochemical efforts revealed that GABAB receptors assemble multi-subunit complexes composed of principal and auxiliary subunits. The principal receptor subunits GABAB1a, GABAB1b and GABAB2 form two heterodimeric GABAB(1a,2) and GABAB(1b,2) receptors that can associate with tetramers of auxiliary KCTD (K(+) channel tetramerization domain) subunits. Experiments with subunit knock-out mice revealed that GABAB(1b,2) receptors activate slow inhibitory postsynaptic currents (sIPSCs) while GABAB(1a,2) receptors function as heteroreceptors and inhibit glutamate release...
October 26, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29101366/identification-of-an-analgesic-lipopeptide-produced-by-the-probiotic-escherichia-coli-strain-nissle-1917
#8
Teresa Pérez-Berezo, Julien Pujo, Patricia Martin, Pauline Le Faouder, Jean-Marie Galano, Alexandre Guy, Claude Knauf, Jean Claude Tabet, Sophie Tronnet, Frederick Barreau, Maud Heuillet, Gilles Dietrich, Justine Bertrand-Michel, Thierry Durand, Eric Oswald, Nicolas Cenac
Administration of the probiotic Escherichia coli strain Nissle 1917 (EcN) decreases visceral pain associated with irritable bowel syndrome. Mutation of clbA, a gene involved in the biosynthesis of secondary metabolites, including colibactin, was previously shown to abrogate EcN probiotic activity. Here, we show that EcN, but not an isogenic clbA mutant, produces an analgesic lipopeptide. We characterize lipoamino acids and lipopeptides produced by EcN but not by the mutant by online liquid chromatography mass spectrometry...
November 3, 2017: Nature Communications
https://www.readbyqxmd.com/read/29071990/-effect-of-electroacupuncture-intervention-on-expression-of-synaptic-plasticity-related-molecules-in-amygdala-in-chronic-pain-negative-affection-rats
#9
Cheng-Lin Duanmu, Xiu-Mei Feng, Ya-Xia Yan, Jun-Ying Wang, Yong-Hui Gao, Li-Na Qiao, Shu-Ping Chen, Jian-Liang Zhang, Jun-Ling Liu
OBJECTIVE: To observe the effect of electroacupuncture (EA) on expression of synaptic plasticity-related glutamate N-methyl-D-aspartate (NMDA) receptor subunit NR 1, gamma-aminobutyric acid (GABA) receptor subunits (Aβ 2, B 1), etc. in the amygdala in chronic neuropathic pain negative affection (CNPPNA) rats, so as to reveal its mechanism underlying pain relief. METHODS: Male Wistar rats were randomized into normal control, CNPPNA model, EA, and anesthesia+EA (AEA)groups (n=14 in each group, 8 for quantitative RT-PCR and 6 for immunofluorescence staining)...
February 25, 2017: Zhen Ci Yan Jiu, Acupuncture Research
https://www.readbyqxmd.com/read/29051549/chronic-antidepressant-potentiates-spontaneous-activity-of-dorsal-raphe-serotonergic-neurons-by-decreasing-gabab-receptor-mediated-inhibition-of-l-type-calcium-channels
#10
Nozomi Asaoka, Naoya Nishitani, Haruko Kinoshita, Hiroyuki Kawai, Norihiro Shibui, Kazuki Nagayasu, Hisashi Shirakawa, Takayuki Nakagawa, Shuji Kaneko
Spontaneous activity of serotonergic neurons of the dorsal raphe nucleus (DRN) regulates mood and motivational state. Potentiation of serotonergic function is one of the therapeutic strategies for treatment of various psychiatric disorders, such as major depression, panic disorder and obsessive-compulsive disorder. However, the control mechanisms of the serotonergic firing activity are still unknown. In this study, we examined the control mechanisms for serotonergic spontaneous activity and effects of chronic antidepressant administration on these mechanisms by using modified ex vivo electrophysiological recording methods...
October 19, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29050951/microinjection-of-baclofen-and-cgp7930-into-the-ventral-tegmental-area-suppresses-alcohol-self-administration-in-alcohol-preferring-rats
#11
REVIEW
Paola Maccioni, Irene Lorrai, Andrea Contini, Kimberly Leite-Morris, Giancarlo Colombo
Systemic administration of the orthosteric agonist, baclofen, and several positive allosteric modulators (PAMs) of the GABAB receptor has repeatedly been reported to decrease operant oral alcohol self-administration in rats. The aim of the present study was to evaluate the contribution of the mesolimbic dopamine system to the reducing effect of baclofen and GABAB PAMs on the reinforcing properties of alcohol. To this end, baclofen or the GABAB PAM CGP7930 were microinjected into the ventral tegmental area (VTA) of selectively bred, Sardinian alcohol-preferring (sP) rats trained to self-administer alcohol...
October 16, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29050820/gabab-receptor-modulation-to-b-or-not-to-be-b-a-pro-cognitive-medicine
#12
REVIEW
Jordi Serrats, Mark Oliver Cunningham, Ceri Hywel Davies
Metabotropic GABAB receptors clearly modify cognitive performance in preclinical animal models, yet translation to treating human disease has been elusive. Compared to their ionotropic GABAA receptor counterpart GABAB receptors not only regulate postsynaptic excitability but also regulate diverse synaptic inputs by presynaptically inhibiting neurotransmitter release. As such, the choice of agonist, antagonist, -ve or +ve modulator as well as CNS exposure level, timing of delivery and longevity of action strongly influence the probability of unlocking the procognitive potential of GABAB receptors in human disease...
October 16, 2017: Current Opinion in Pharmacology
https://www.readbyqxmd.com/read/29038006/role-of-ca1-gabaa-and-gabab-receptors-on-learning-deficit-induced-by-d-ap5-in-passive-avoidance-step-through-task
#13
Mohaddeseh Ebrahimi-Ghiri, Masoumeh Rostampour, Mehdi Jamshidi-Mehr, Mohammad Nasehi, Mohammad-Reza Zarrindast
To investigate the interaction between hippocampal γ-aminobutyric acid GABAA receptor (GABAAR) or GABAB receptor (GABABR) and N-methyl-D-aspartate receptor (NMDAR) in the acquisition of passive avoidance memory in rats, we used GABAA or GABAB agents, D-AP5 (as a NMDAR antagonist), and a combination of the mentioned drugs in a step-through task. All agents were microinjected into the intra-CA1 regions at a volume of 1 µl/rat, prior to training. GABAAR agonist muscimol (0.2 µg/rat), selective GABABR agonist baclofen (0...
October 13, 2017: Brain Research
https://www.readbyqxmd.com/read/29032104/participation-of-gabab-receptors-in-cortical-postictal-excitability-in-immature-rats
#14
Pavel Mareš
Arrest of seizures is due to an active inhibition and is followed in mature brain by period of refractoriness markedly present one min after the end of seizures. To study changes in cortical excitability after epileptic seizures we used electrical stimulation of sensorimotor cortical area in immature rats - 25-day-old ones with mature postictal refractoriness and 12-day-old where postictal potentiation of afterdischarges (ADs) is present instead of refractoriness at one minute after the end of the conditioning AD...
October 13, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29031577/structural-biology-of-gabab-receptor
#15
REVIEW
Aurel Frangaj, Qing R Fan
Metabotropic GABAB receptor is a G protein-coupled receptor (GPCR) that mediates slow and prolonged inhibitory neurotransmission in the brain. It functions as a constitutive heterodimer composed of the GABAB1 and GABAB2 subunits. Each subunit contains three domains; the extracellular Venus flytrap module, seven-helix transmembrane region and cytoplasmic tail. In recent years, the three-dimensional structures of GABAB receptor extracellular and intracellular domains have been elucidated. These structures reveal the molecular basis of ligand recognition, receptor heterodimerization and receptor activation...
October 12, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29030218/acupuncture-suppresses-intravenous-methamphetamine-self-administration-through-gaba-receptor-s-mediation
#16
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/29018828/repurposing-lesogaberan-to-promote-human-islet-cell-survival-and-%C3%AE-cell-replication
#17
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/28984295/r-baclofen-reverses-cognitive-deficits-and-improves-social-interactions-in-two-lines-of-16p11-2-deletion-mice
#18
Laura J Stoppel, Tatiana M Kazdoba, Melanie D Schaffler, Anthony R Preza, Arnold Heynen, Jacqueline N Crawley, Mark F Bear
Human chromosome 16p11.2 microdeletion is among the most common gene copy number variations (CNVs) known to confer risk for intellectual disability (ID) and autism spectrum disorder (ASD), and affects an estimated 3 in 10 000 people. Caused by a single copy deletion of ~27 genes, 16p11.2 microdeletion syndrome is characterized by ID, impaired language, communication and socialization skills, and ASD. Studies in animal models where a single copy of the syntenic 16p11.2 region has been deleted have revealed morphological, behavioral, and electrophysiological abnormalities...
October 6, 2017: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28983255/the-regulatory-effects-of-lateral-hypothalamus-area-gabab-receptor-on-gastric-ischemia-reperfusion-injury-in-rats
#19
Lin Gao, Huiru Zhao, Tao Zhu, Yeliu Liu, Li Hu, Zhenguo Liu, Hai Huang, Fuxue Chen, Zhenxu Deng, Dechang Chu, Dongshu Du
HIGHLIGHTS The aim of the research was to determine the functional effects and molecular mechanisms of GABAB receptor on ischemia reperfusion-induced gastric injury in rats.The lateral hypothalamus area GABAB receptor attenuated the ischemia reperfusion-induced gastric injury by up-regulating the production of GABA, GABABR, and down-regulating P-GABABR in the brain.This work would provide a new therapeutic strategy for acute gastric injury. Gastric ischemia-reperfusion (GI-R) injury progression is largely associated with excessive activation of the greater splanchnic nerve (GSN)...
2017: Frontiers in Physiology
https://www.readbyqxmd.com/read/28981616/spreading-depression-promotes-astrocytic-calcium-oscillations-and-enhances-gliotransmission-to-hippocampal-neurons
#20
Dong Chuan Wu, Rita Yu-Tzu Chen, Ting-Chun Cheng, Yao-Chang Chiang, Mei-Lin Shen, Li-Ling Hsu, Ning Zhou
Spreading depression (SD) is a pathophysiological phenomenon characterized by propagating waves of profound neuronal and glial depolarization in central nervous system gray matter. Although SD is primarily mediated by neurons with a subsequent astrocytic response, it remains unclear how astrocytic activity is modulated after SD and how altered astrocyte signaling contribute to neuronal excitability. Here, we report that after the concurrent Ca2+ wave, SD enhanced astrocytic activity by promoting a secondary period of Ca2+ oscillations...
August 1, 2017: Cerebral Cortex
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