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https://www.readbyqxmd.com/read/28726252/central-amygdala-relaxin-3-rxfp3-signalling-modulates-alcohol-seeking-in-rats
#1
Leigh C Walker, Hanna E Kastman, Elena Krstew, Andrew L Gundlach, Andrew J Lawrence
BACKGROUND AND PURPOSE: Alcohol use disorders are a leading cause of preventable deaths worldwide and stress is a major trigger of relapse. The neuropeptide relaxin-3 and its cognate receptor, relaxin family peptide receptor 3 (RXFP3), modulate stress-induced relapse to alcohol seeking in rats and while the bed nucleus of the stria terminalis has been implicated in this regard, the central nucleus of the amygdala (CeA) also receives a relaxin-3 innervation and CeA neurons densely express RXFP3 mRNA...
July 20, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28725181/impact-of-proestrus-on-gene-expression-in-the-medial-preoptic-area-of-mice
#2
Csaba Vastagh, Zsolt Liposits
The antero-ventral periventricular zone (AVPV) and medial preoptic area (MPOA) have been recognized as gonadal hormone receptive regions of the rodent brain that-via wiring to gonadotropin-releasing hormone (GnRH) neurons-contribute to orchestration of the preovulatory GnRH surge. We hypothesized that neural genes regulating the induction of GnRH surge show altered expression in proestrus. Therefore, we compared the expression of 48 genes obtained from intact proestrous and metestrous mice, respectively, by quantitative real-time PCR (qPCR) method...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/28720884/molecular-tools-for-gabaa-receptors-high-affinity-ligands-for-%C3%AE-1-containing-subtypes
#3
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
#4
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/28715875/acute-orexigenic-effect-of-agmatine-involves-interaction-between-central-%C3%AE-2-adrenergic-and-gabaergic-receptors
#5
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/28714121/acetylcholine-dependent-upregulation-of-task-1-channels-in-thalamic-interneurons-by-a-smooth-muscle-like-signalling-pathway
#6
Michael Leist, Susanne Rinné, Maia Datunashvili, Ania Aissaoui, Hans-Christian Pape, Niels Decher, Sven G Meuth, Thomas Budde
The dorsal part of the lateral geniculate nucleus (dLGN) is the main thalamic site for state-dependent transmission of visual information. Non-retinal inputs from the ascending arousal system and inhibition provided by γ-aminobutyric acid (GABA)ergic local circuit interneurons (INs) control neuronal activity within the dLGN. In particular, acetylcholine (ACh) depolarizes thalamocortical relay (TC) neurons by inhibiting two-pore domain potassium (K2P ) channels. Conversely, ACh also hyperpolarizes INs via an as-yet-unknown mechanism...
July 17, 2017: Journal of Physiology
https://www.readbyqxmd.com/read/28713569/kctd12-modulation-of-gaba-b-receptor-function
#7
Melody Li, Carol J Milligan, Haiyan Wang, Andrew Walker, Leonid Churilov, Andrew J Lawrence, Christopher A Reid, Seth C Hopkins, Steven Petrou
The molecular composition and functional diversity of native GABAB receptors (GABABR) are still poorly understood, thus hindering development of selective GABABR ligands. Potassium channel tetramerization domain-containing protein (KCTD) 12 is a GABABR auxiliary subunit and mouse KCTD12 can alter GABABR function. In this study, we sought to characterize the effects of human KCTD12 on GABABR kinetics and pharmacology, using an automated electrophysiological assay. Seizure susceptibility and ethanol consumption were also investigated in a KCTD12 knockout mouse model...
August 2017: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/28711518/antagonism-of-the-5-ht6-receptor-preclinical-rationale-for-the-treatment-of-alzheimer-s-disease
#8
REVIEW
Inge E M de Jong, Arne Mørk
Antagonism of the 5-HT6 receptor is a promising approach for the symptomatic treatment of Alzheimer's disease (AD). There is compelling preclinical evidence for the procognitive potential of 5-HT6 receptor antagonists and several compounds are in clinical development, as adjunct therapy to acetylcholinesterase inhibitors (AChEIs). This manuscript summarizes the scientific rationale for the use of 5-HT6 receptor antagonists as AD treatment, with some focus on the selective and high-affinity 5-HT6 receptor antagonist idalopirdine (Lu AE58054)...
July 12, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28701925/postsynaptic-gaba-b-receptors-contribute-to-the-termination-of-giant-depolarizing-potentials-in-ca3-neonatal-rat-hippocampus
#9
Ilgam Khalilov, Marat Minlebaev, Marat Mukhtarov, Elvira Juzekaeva, Roustem Khazipov
During development, hippocampal CA3 network generates recurrent population bursts, so-called Giant Depolarizing Potentials (GDPs). GDPs are characterized by synchronous depolarization and firing of CA3 pyramidal cells followed by afterhyperpolarization (GDP-AHP). Here, we explored the properties of GDP-AHP in CA3 pyramidal cells using gramicidin perforated patch clamp recordings from neonatal rat hippocampal slices. We found that GDP-AHP occurs independently of whether CA3 pyramidal cells fire action potentials (APs) or remain silent during GDPs...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/28699326/gamma-aminobutyric-acid-gaba-receptors-rho-gabrr-gene-polymorphisms-and-risk-for-migraine
#10
Elena García-Martín, Carmen Martínez, Mercedes Serrador, Hortensia Alonso-Navarro, Francisco Navacerrada, Gara Esguevillas, Esteban García-Albea, José A G Agúndez, Félix Javier Jiménez-Jiménez
BACKGROUND/OBJECTIVES: The possible role of gammaaminobutyric acid (GABA) in the pathogenesis of migraine has been suggested by a number of biochemical, pharmacological, neurophysiological and experimental data. We investigated the possible association between the most common single nucleotide polymorphisms (SNPs) in the GABA receptor rho1, 2, and 3 genes (GABRR1, GABRR2, and GABRR3) and the risk of developing migraine. METHODS: The frequency of GABRR1 rs12200969, GABRR1 rs1186902, GABRR2 rs282129, and GABRR3 rs832032 genotypes and allelic variants were studied in a case-control association study involving 197 patients with migraine and 278 healthy controls by means of a TaqMan-based qPCR Assay...
July 2017: Headache
https://www.readbyqxmd.com/read/28694181/allopregnanolone-involvement-in-feeding-regulation-overeating-and-obesity
#11
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/28686214/current-study-of-the-mechanism-of-action-of-the-potential-anti-epileptic-agent-q808
#12
Xiang Li, Hong-Jian Zhang, Qing Wang, Dian-Wen Zhang, Di Wu, Wei Li, Zhe-Shan Quan
Our previous study showed that the anticonvulsant Q808 might be effective against seizures induced by maximal electroshock, pentylenetetrazole (PTZ), isoniazid (ISO), thiosemicarbazide (THIO), and 3-mercaptopropionic acid (3-MP). In the present study, we explored the possible mechanism of action of Q808. Results obtained with high-performance liquid chromatography (HPLC) suggest that Q808 may affect neurotransmitter content in the brain, by specifically increasing GABA content in the rat hippocampus at doses of 40 mg/kg and 80 mg/kg, and by reducing the content of glutamate and glutamine in the rat thalamus at a dose of 80 mg/kg...
July 7, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
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
#13
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/28683263/igf1-dependent-synaptic-plasticity-of-mitral-cells-in-olfactory-memory-during-social-learning
#14
Zhihui Liu, Zijun Chen, Congping Shang, Fei Yan, Yingchao Shi, Jiajing Zhang, Baole Qu, Hailin Han, Yanying Wang, Dapeng Li, Thomas C Südhof, Peng Cao
During social transmission of food preference (STFP), mice form long-term memory of food odors presented by a social partner. How does the brain associate a social context with odor signals to promote memory encoding? Here we show that odor exposure during STFP, but not unconditioned odor exposure, induces glomerulus-specific long-term potentiation (LTP) of synaptic strength selectively at the GABAergic component of dendrodendritic synapses of granule and mitral cells in the olfactory bulb. Conditional deletion of synaptotagmin-10, the Ca(2+) sensor for IGF1 secretion from mitral cells, or deletion of IGF1 receptor in the olfactory bulb prevented the socially relevant GABAergic LTP and impaired memory formation after STFP...
July 5, 2017: Neuron
https://www.readbyqxmd.com/read/28680877/metabolic-products-of-linalool-and-modulation-of-gabaa-receptors
#15
Sinem Milanos, Shaimaa A Elsharif, Dieter Janzen, Andrea Buettner, Carmen Villmann
Terpenoids are major subcomponents in aroma substances which harbor sedative physiological potential. We have demonstrated that various monoterpenoids such as the acyclic linalool enhance GABAergic currents in an allosteric manner in vitro upon overexpression of inhibitory α1β2 GABAA receptors in various expression systems. However, in plants or humans, i.e., following intake via inhalation or ingestion, linalool undergoes metabolic modifications including oxygenation and acetylation, which may affect the modulatory efficacy of the generated linalool derivatives...
2017: Frontiers in Chemistry
https://www.readbyqxmd.com/read/28680103/chemogenetic-silencing-of-gabaergic-dorsal-horn-interneurons-induces-morphine-resistant-spontaneous-nocifensive-behaviours
#16
Keisuke Koga, Kensho Kanehisa, Yuta Kohro, Miho Shiratori-Hayashi, Hidetoshi Tozaki-Saitoh, Kazuhide Inoue, Hidemasa Furue, Makoto Tsuda
Inhibitory interneurons in the spinal dorsal horn (SDH) are crucial for processing somatosensory information originating in the periphery. However, the effects of the acute and selective inactivation of GABAergic SDH interneurons on pain processing are not fully understood. In this study, we used designer receptors exclusively activated by designer drugs (DREADD) technology and vesicular GABA transporter-Cre (Vgat-Cre) mice to selectively express a modified human muscarinic Gi protein-coupled receptor (hM4Di) in Vgat-Cre (+) GABAergic SDH interneurons in the fourth lumbar segment...
July 5, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28678402/inhibitory-modulation-of-medial-prefrontal-cortical-activation-on-lateral-orbitofrontal-cortex-amygdala-information-flow
#17
Chun-Hui Chang, Ta-Wen Ho
Several neocortical projections converge onto the basolateral complex of the amygdala (BLA), including the lateral orbitofrontal cortex (lOFC) and medial prefrontal cortex (mPFC). Lateral orbitofrontal input to BLA is important for cue-outcome contingencies, while medial prefrontal input is essential for emotion control. In this study, we examined how mPFC, specifically the infralimbic (IL) division of mPFC, modulates the lOFC-BLA information flow, using combined in vivo extracellular single-unit recordings and pharmacological manipulations in anesthetized rats...
July 5, 2017: Journal of Physiology
https://www.readbyqxmd.com/read/28676743/differential-alteration-in-expression-of-striatal-gabaar-subunits-in-mouse-models-of-huntington-s-disease
#18
Zhuowei Du, Margot Tertrais, Gilles Courtand, Thierry Leste-Lasserre, Laura Cardoit, Frédérique Masmejean, Christophe Halgand, Yoon H Cho, Maurice Garret
Huntington's disease (HD) is a neurodegenerative disorder characterized by progressive motor symptoms that are preceded by cognitive deficits and is considered as a disorder that primarily affects forebrain striatal neurons. To gain a better understanding of the molecular and cellular mechanisms associated with disease progression, we analyzed the expression of proteins involved in GABAergic neurotransmission in the striatum of the R6/1 transgenic mouse model. Western blot, quantitative PCR and immunohistochemical analyses were conducted on male R6/1 mice and age-matched wild type littermates...
2017: Frontiers in Molecular Neuroscience
https://www.readbyqxmd.com/read/28676256/neurotoxicity-of-propofol-on-rat-hypoglossal-motoneurons-in-vitro
#19
Laura Monni, Filippo Ghezzi, Silvia Corsini, Andrea Nistri
Although propofol is a widely used intravenous general anaesthetic, many studies report its toxic potential, particularly on the developing central nervous system. We investigated its action on hypoglossal motoneurons (HMs) that control two critical functions in neonates, namely tongue muscle activity and airway patency. Thus, clinically relevant concentrations of propofol (1 and 5μM) were applied (4h) to neonatal rat brainstem slices to evaluate the expression of apoptosis-inducing factor (AIF) as biomarker of toxicity...
July 1, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/28674483/hypotensive-response-to-angiotensin-ii-type-2-receptor-stimulation-in-the-rostral-ventrolateral-medulla-requires-functional-gaba-a-receptors
#20
Laura Légat, Sofie Brouwers, Ilse J Smolders, Alain G Dupont
Objectives: Angiotensin II, glutamate and gamma-aminobutyric acid (GABA) interact within the rostral ventrolateral medulla (RVLM) and the paraventricular nucleus (PVN) modulating the central regulation of blood pressure and sympathetic tone. Our aim was to assess the effects of local angiotensin II type 2 receptor stimulation within the RVLM and the PVN on neurotransmitter concentrations and mean arterial pressure (MAP). Methods:In vivo microdialysis was used for measurement of extracellular glutamate and GABA levels and for local infusion of the angiotensin II type 2 receptor agonist Compound 21 in the RVLM and the PVN of conscious normotensive Wistar rats...
2017: Frontiers in Neuroscience
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