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Gabaa receptor

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https://www.readbyqxmd.com/read/28733205/-dehydrofukinone-modulates-membrane-potential-and-delays-seizure-onset-by-gabaa-receptor-mediated-mechanism-in-mice
#1
Quelen Iane Garlet, Luana da Costa Pires, Laura Hautrive Milanesi, Joseane Righes Marafiga, Bernardo Baldisserotto, Carlos Fernando de Mello, Berta Maria Heinzmann
(+)-Dehydrofukinone (DHF), isolated from Nectandra grandiflora (Lauraceae) essential oil, induces sedation and anesthesia by modulation of GABAa receptors. However, no study has addressed whether DHF modulates other cellular events involved in the control of cellular excitability, such as seizure behavior. Therefore, the aim of the present study was to investigate the effect of DHF on cellular excitability and seizure behavior in mice. For this purpose, we used isolated nerve terminals (synaptosomes) to examine the effect of DHF on the plasma membrane potential, the involvement of GABAa receptors and the downstream activation of Ca(2+) mobilization...
July 18, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28730280/evidence-for-the-involvement-of-the-gabaergic-but-not-serotonergic-transmission-in-the-anxiolytic-like-effect-of-bisabolol-in-the-mouse-elevated-plus-maze
#2
Mohaddeseh Abouhosseini Tabari, Mohammad Amir Bagherpour Tehrani
Bisabolol (α-(-)-bisabolol) is a sesquiterpene which is a part of the essential oil of a variety of plants, but its common source is German chamomile. Several bioactivities including anti-inflammatory, anti-nociceptive, and anti-tumor effects were attributed to bisabolol. However, the neuropharmacological properties of bisabolol have not yet been reported. The present study evaluated behavioral effects of bisabolol using elevated plus maze (EPM), open field test (OFT), and rotarod test. Moreover, this study also examined whether the 5-HT1A and GABAA-benzodiazepine receptor systems are involved in the anxiolytic-like effects of bisabolol...
July 20, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28728911/effects-of-riluzole-on-spinal-seizure-like-activity-in-the-brainstem-spinal-cord-preparation-of-newborn-rat
#3
Shih Tien Lin, Masayuki Ohbayashi, Toshinori Yamamoto, Hiroshi Onimaru, Mari Kogo
Riluzole blocks persistent Na(+) current, inhibits generation of neuronal bursts and decreases glutamate-induced excitotoxicity. In previous studies of respiratory activity, riluzole suppressed inspiratory-related burst generation activity in rat slice or en bloc preparations. We examined riluzole's effects on inspiratory burst generation and drug-induced seizure-like activity in newborn rat en bloc preparations. Medulla-spinal cord preparations from postnatal day 0-3 Wistar rats were isolated under deep isoflurane anesthesia and were superfused with artificial cerebrospinal fluid equilibrated with 95% O2 and 5% CO2, pH 7...
July 17, 2017: Neuroscience Research
https://www.readbyqxmd.com/read/28720884/molecular-tools-for-gabaa-receptors-high-affinity-ligands-for-%C3%AE-1-containing-subtypes
#4
Xenia Simeone, David C B Siebert, Konstantina Bampali, Zdravko Varagic, Marco Treven, Sabah Rehman, Jakob Pyszkowski, Raphael Holzinger, Friederike Steudle, Petra Scholze, Marko D Mihovilovic, Michael Schnürch, Margot Ernst
γ-Aminobutyric acid type A (GABAA) receptors are pentameric GABA-gated chloride channels that are, in mammalians, drawn from a repertoire of 19 different genes, namely α1-6, β1-3, γ1-3, δ, ε, θ, π and ρ1-3. The existence of this wide variety of subunits as well as their diverse assembly into different subunit compositions result in miscellaneous receptor subtypes. In combination with the large number of known and putative allosteric binding sites, this leads to a highly complex pharmacology. Recently, a novel binding site at extracellular α+/β- interfaces was described as the site of modulatory action of several pyrazoloquinolinones...
July 18, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28717969/decreasing-the-expression-of-gabaa-%C3%AE-5-subunit-containing-receptors-partially-improves-cognitive-electrophysiological-and-morphological-hippocampal-defects-in-the-ts65dn-model-of-down-syndrome
#5
Verónica Vidal, Susana García-Cerro, Paula Martínez, Andrea Corrales, Sara Lantigua, Rebeca Vidal, Noemí Rueda, Laurence Ozmen, Maria-Clemencia Hernández, Carmen Martínez-Cué
Trisomy 21 or Down syndrome (DS) is the most common cause of intellectual disability of a genetic origin. The Ts65Dn (TS) mouse, which is the most commonly used and best-characterized mouse model of DS, displays many of the cognitive, neuromorphological, and biochemical anomalies that are found in the human condition. One of the mechanisms that have been proposed to be responsible for the cognitive deficits in this mouse model is impaired GABA-mediated inhibition. Because of the well-known modulatory role of GABAA α5 subunit-containing receptors in cognitive processes, these receptors are considered to be potential targets for improving the intellectual disability in DS...
July 17, 2017: Molecular Neurobiology
https://www.readbyqxmd.com/read/28716958/%C3%AE-subunit-containing-gabaa-receptor-prevents-overgeneralization-of-fear-in-adult-mice
#6
Wen-Hua Zhang, Jin Zhou, Han-Qing Pan, Xiao-Yang Wang, Wei-Zhu Liu, Jun-Yu Zhang, Xiao-Ping Yin, Bing-Xing Pan
The role of δ subunit-containing GABAA receptor (GABAA(δ)R) in fear generalization is uncertain. Here, by using mice with or without genetic deletion of GABAA(δ)R and using protocols in which the conditioned tone stimuli were cross presented with different nonconditioned stimuli, we observed that when the two tone stimuli were largely similar, both genotypes froze similarly to either of them. However, when they differed markedly, the knockout mice froze much more than their wild-type littermates to the nonconditioned but not conditioned stimuli...
August 2017: Learning & Memory
https://www.readbyqxmd.com/read/28716952/differential-involvement-of-the-medial-prefrontal-cortex-across-variants-of-contextual-fear-conditioning
#7
Nicholas A Heroux, Patrese A Robinson-Drummer, Hollie R Sanders, Jeffrey B Rosen, Mark E Stanton
The context preexposure facilitation effect (CPFE) is a contextual fear conditioning paradigm in which learning about the context, acquiring the context-shock association, and retrieving/expressing contextual fear are temporally dissociated into three distinct phases. In contrast, learning about the context and the context-shock association happens concurrently in standard contextual fear conditioning (sCFC). By infusing the GABAA receptor agonist muscimol into medial prefrontal cortex (mPFC) in adolescent Long-Evans rats, the current set of experiments examined the functional role of the mPFC in each phase of the CPFE and sCFC...
August 2017: Learning & Memory
https://www.readbyqxmd.com/read/28716844/microglia-control-the-glycinergic-but-not-the-gabaergic-synapses-via-prostaglandin-e2-in-the-spinal-cord
#8
Yasmine Cantaut-Belarif, Myriam Antri, Rocco Pizzarelli, Sabrina Colasse, Ilaria Vaccari, Sylvia Soares, Marianne Renner, Radhouane Dallel, Antoine Triller, Alain Bessis
Microglia control excitatory synapses, but their role in inhibitory neurotransmission has been less well characterized. Herein, we show that microglia control the strength of glycinergic but not GABAergic synapses via modulation of the diffusion dynamics and synaptic trapping of glycine (GlyR) but not GABAA receptors. We further demonstrate that microglia regulate the activity-dependent plasticity of glycinergic synapses by tuning the GlyR diffusion trap. This microglia-synapse cross talk requires production of prostaglandin E2 by microglia, leading to the activation of neuronal EP2 receptors and cyclic adenosine monophosphate-dependent protein kinase...
July 17, 2017: Journal of Cell Biology
https://www.readbyqxmd.com/read/28715875/acute-orexigenic-effect-of-agmatine-involves-interaction-between-central-%C3%AE-2-adrenergic-and-gabaergic-receptors
#9
Brijesh Gulabrao Taksande, Omi Sharma, Manish Manohar Aglawe, Mayur Bhimrao Kale, Dinesh Yugraj Gawande, Milind Janraoji Umekar, Nandkishor Ramdas Kotagale
Agmatine and GABA have been abundantly expressed in brain nuclei involved in regulation of energy homeostasis and promoting stimulation of food intake in rodents. However, their mutual interaction, if any, in the elicitation of feeding behavior is largely remains unclear. The current study provides experimental evidence for the possible interaction of agmatine, adrenergic and GABAergic systems in stimulation of feeding in satiated rats. Satiated rats fitted with intracerebroventricular (i.c.v.) cannulae and were administered agmatine, alone or jointly with (a) GABAA receptor agonist, muscimol, diazepam or antagonist bicuculline and flumazenil, GABAA positive modulator, allopregnanolone or negative modulator of GABAA receptor, dehydroepiandrosterone (b) In view of the high affinity of agmatine for α2-adrenoceptors and the close association between α2-adrenoceptors and GABAergic system, the effect of their modulators on feeding elicited by agmatine/GABAergic agonists were also examined...
July 13, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28713263/the-frequency-dependent-aerobic-exercise-effects-of-hypothalamic-gabaergic-expression-and-cardiovascular-functions-in-aged-rats
#10
Yan Li, Ziqi Zhao, Jiajia Cai, Boya Gu, Yuanyuan Lv, Li Zhao
A decline in cardiovascular modulation is a feature of the normal aging process and associated with cardiovascular diseases (CVDs) such as hypertension and stroke. Exercise training is known to promote cardiovascular adaptation in young animals and positive effects on motor and cognitive capabilities, as well as on brain plasticity for all ages in mice. Here, we examine the question of whether aerobic exercise interventions may impact the GABAergic neurons of the paraventricular nucleus (PVN) in aged rats which have been observed to have a decline in cardiovascular integration function...
2017: Frontiers in Aging Neuroscience
https://www.readbyqxmd.com/read/28713246/differential-contribution-of-ca-2-dependent-mechanisms-to-hyperexcitability-in-layer-v-neurons-of-the-medial-entorhinal-cortex
#11
Eric C Lin, Crescent L Combe, Sonia Gasparini
Temporal lobe epilepsy is characterized by recurrent seizures in one or both temporal lobes of the brain; some in vitro models show that epileptiform discharges initiate in entorhinal layer V neurons and then spread into other areas of the temporal lobe. We previously found that, in the presence of GABAA receptor antagonists, stimulation of afferent fibers, terminating both at proximal and distal dendritic locations, initiated hyperexcitable bursts in layer V medial entorhinal neurons. We investigated the differential contribution of Ca(2+)-dependent mechanisms to the plateaus underlying these bursts at proximal and distal synapses...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/28708891/loss-of-neuroligin3-specifically-downregulates-retinal-gabaa%C3%AE-2-receptors-without-abolishing-direction-selectivity
#12
Mrinalini Hoon, Vidhyasankar Krishnamoorthy, Tim Gollisch, Bjoern Falkenburger, Frederique Varoqueaux
The postsynaptic adhesion proteins Neuroligins (NLs) are essential for proper synapse function, and their alterations are associated with a variety of neurodevelopmental disorders. It is increasingly clear that each NL isoform occupies specific subsets of synapses and is able to regulate the function of discrete networks. Studies of NL2 and NL4 in the retina in particular have contributed towards uncovering their role in inhibitory synapse function. In this study we show that NL3 is also predominantly expressed at inhibitory postsynapses in the retinal inner plexiform layer (IPL), where it colocalizes with both GABAA- and glycinergic receptor clusters in a 3:2 ratio...
2017: PloS One
https://www.readbyqxmd.com/read/28707143/clinical-sleep-wake-disorders-ii-focus-on-insomnia-and-circadian-rhythm-sleep-disorders
#13
Kai Spiegelhalder, Christoph Nissen, Dieter Riemann
Insomnia and circadian rhythm sleep disorders affect large proportions of the population and have pronounced effects on quality of life and daytime performance. While the neurobiology of insomnia is not yet fully understood, circadian rhythm sleep disorders are assumed to be caused by a mismatch between the individual circadian phase position and the desired sleep-wake schedule. Benzodiazepines and non-benzodiazepine positive allosteric GABAA receptor modulators improve sleep onset and maintenance in the short-term treatment of insomnia...
July 14, 2017: Handbook of Experimental Pharmacology
https://www.readbyqxmd.com/read/28706559/insights-into-the-roles-of-midazolam-in-cancer-therapy
#14
REVIEW
Jinghua Jiao, Yuheng Wang, Xiaofeng Sun, Xiaojing Jiang
With its high worldwide mortality and morbidity, cancer has gained increasing attention and novel anticancer drugs have become the focus for cancer research. Recently, studies have shown that most anesthetic agents can influence the activity of tumor cells. Midazolam is a γ-aminobutyric acid A (GABAA) receptor agonist, used widely for preoperative sedation and as an adjuvant during neuraxial blockade. Some studies have indicated the potential for midazolam as a novel therapeutic cancer drug; however, the mechanism by which midazolam affects cancer cells needs to be clarified...
2017: Evidence-based Complementary and Alternative Medicine: ECAM
https://www.readbyqxmd.com/read/28698637/distinct-properties-of-long-term-potentiation-in-the-dentate-gyrus-along-the-dorsoventral-axis-influence-of-age-and-inhibition
#15
An Schreurs, Victor Sabanov, Detlef Balschun
The hippocampus is important for spatial navigation, episodic memory and affective behaviour. Increasing evidence suggests that these multiple functions are accomplished by different segments along the dorsal-ventral (septal-temporal) axis. Long-term potentiation (LTP), the best-investigated cellular correlate of learning and memory, has distinct properties along this axis in the CA1 region, but so far, little is known about longitudinal differences in dentate gyrus (DG). Therefore, here we examined potential dorsoventral differences in DG-LTP using in vitro multi-electrode array recordings...
July 11, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28698388/delayed-cryptochrome-degradation-asymmetrically-alters-the-daily-rhythm-in-suprachiasmatic-clock-neuron-excitability
#16
Sven Wegner, Mino D C Belle, Alun T L Hughes, Casey O Diekman, Hugh D Piggins
Suprachiasmatic nuclei (SCN) neurons contain an intracellular molecular circadian clock and the Cryptochromes (CRY1/2), key transcriptional repressors of this molecular apparatus, are subject to post-translational modification through ubiquitination and targeting for proteosomal degradation by the ubiquitin E3 ligase complex. Loss-of-function point mutations in a component of this ligase complex, Fbxl3, delay CRY1/2 degradation, reduce circadian rhythm strength, and lengthen the circadian period by ∼2.5h...
July 11, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28694181/allopregnanolone-involvement-in-feeding-regulation-overeating-and-obesity
#17
E Holmberg, J Sjöstedt, E Malinina, M Johansson, S Turkmen, G Ragagnin, A Lundqvist, M Löfgren, L Jaukkuri, M Bixo, T Bäckström
Obesity is strongly associated with ill health, primarily caused by consumption of excessive calories, and promoted (inter alia) by gamma-amino-butyric-acid (GABA) stimulating food intake by activating GABAA receptors (primarily with α3 and α2 subunits) in the hypothalamic arcuate nucleus and paraventricular nucleus. Allopregnanolone is a potent positive GABAA receptor modulating steroid (GAMS). As reviewed here, elevated allopregnanolone levels are associated with increases in food intake, preferences for energy-rich food, and obesity in humans and other mammals...
July 8, 2017: Frontiers in Neuroendocrinology
https://www.readbyqxmd.com/read/28694097/behavioural-pharmacology-of-the-%C3%AE-5-gabaa-receptor-antagonist-s44819-enhancement-and-remediation-of-cognitive-performance-in-preclinical-models
#18
István Gacsályi, Krisztina Móricz, Gábor Gigler, János Wellmann, Katalin Nagy, István Ling, József Barkóczy, József Haller, Jeremy J Lambert, Gábor Szénási, Michael Spedding, Ferenc A Antoni
Previous work has shown that S44819 is a novel GABAA receptor (GABAAR) antagonist, which is selective for extrasynaptic GABAARs incorporating the α5 subunit (α5-GABAARs). The present study reports on the preclinical neuropsychopharmacological profile of S44819. Significantly, no sedative or pro-convulsive side effects of S44819 were found at doses up to 30 mg/kg i.p. Object recognition (OR) memory in intact mice was enhanced by S44819 (0.3 mg/kg p.o.) given before the acquisition trial. Mice treated with phencyclidine for two weeks and tested six days after the cessation of treatment failed to show OR memory...
July 8, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28683403/monastrol-a-3-4-dihydropyrimidin-2-1h-thione-as-structural-scaffold-for-the-development-of-modulators-for-ghb-high-affinity-binding-sites-and-%C3%AE-1%C3%AE-2%C3%AE-gabaa-receptors
#19
Maria Damgaard, Anas Al-Khawaja, Mia Nittegaard-Nielsen, Rebekka F Petersen, Petrine Wellendorph, Bente Frølund
The α4βδ subtype of the γ-aminobutyric acid (GABA) type A receptors (GABAARs) has been shown to be implicated in high-affinity binding of the neuromodulator γ-hydroxybutyric acid (GHB), but may not be the only GHB high-affinity binding sites. Monastrol has been identified as a modulator of GHB high-affinity binding and is furthermore reported as an allosteric modulator selective for the α1β2δ GABAARs. Therefore, structural determinants for selectivity at the two targets were investigated. 39 structural diverse monastrol analogues were synthesized by employing the Biginelli cyclocondensation and examined for modulation of GHB high-affinity binding using the GHB-specific ligand [(3)H]NCS-382 [(E,RS)-6,7,8,9-tetrahydro-5-hydroxy-5H-benzocyclohept-6-ylidene)acetic acid] in rat brain homogenate...
June 15, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28683270/inter-synaptic-lateral-diffusion-of-gabaa-receptors-shapes-inhibitory-synaptic-currents
#20
Emanuela de Luca, Tiziana Ravasenga, Enrica Maria Petrini, Alice Polenghi, Thierry Nieus, Stefania Guazzi, Andrea Barberis
The lateral mobility of neurotransmitter receptors has been shown to tune synaptic signals. Here we report that GABAA receptors (GABAARs) can diffuse between adjacent dendritic GABAergic synapses in long-living desensitized states, thus laterally spreading "activation memories" between inhibitory synapses. Glutamatergic activity limits this inter-synaptic diffusion by trapping GABAARs at excitatory synapses. This novel form of activity-dependent hetero-synaptic interplay is likely to modulate dendritic synaptic signaling...
July 5, 2017: Neuron
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