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Gaba a inhibitor

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https://www.readbyqxmd.com/read/28900387/social-isolation-in-early-versus-late-adolescent-mice-is-associated-with-persistent-behavioral-deficits-that-can-be-improved-by-neurosteroid-based-treatment
#1
Andrea Locci, Philippe Geoffroy, Michel Miesch, Ayikoe-Guy Mensah-Nyagan, Graziano Pinna
Early trauma and stress exposure during a critical period of life may increase the risk of major depressive disorder (MDD) and post-traumatic stress disorder (PTSD) in adulthood. The first-choice treatment for MDD and PTSD are selective serotonin reuptake inhibitor (SSRI) antidepressants. Unfortunately, half of MDD and PTSD patients show resistance to the therapeutic effects of these drugs and more efficient treatments are essential. Both MDD and PTSD patients present reduced levels of allopregnanolone (Allo), a potent endogenous positive allosteric modulator of GABA action at GABAA receptors which are normalized by SSRIs in treatment responders...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/28885452/mirna-mediated-downregulation-of-kcc2-and-vgat-expression-in-spinal-cord-contributes-to-neonatal-cystitis-induced-visceral-pain-in-rats
#2
Jian Zhang, James Yu, Pradeep Kannampalli, Linghui Nie, Hui Meng, Bidyut Medda, Reza Shaker, Jyoti N Sengupta, Banani Banerjee
Loss of GABAergic inhibition in pain pathways has been considered to be a key component in the development of chronic pain. In the present study, we intended to examine if miR-92b-mediated post-transcriptional dysregulation of spinal potassium chloride cotransporter (KCC2) and vesicular GABA transporter (VGAT) plays a major role in the development and maintenance of long-term visceral hyperalgesia in neonatal zymosan-treated rats. Neonatal cystitis was induced by transurethral zymosan administration from postnatal (P) days 14-16 (protocol 1)...
September 1, 2017: Pain
https://www.readbyqxmd.com/read/28881432/protein-4-1r-is-involved-in-the-transport-of-5-aminolevulinic-acid-by-interaction-with-gats-in-mef-cells
#3
Shuwei Ning, Qiaozhen Kang, Dandan Fan, Jingjing Liu, Chaoyue Xue, Xiaolin Zhang, Cong Ding, Jianying Zhang, Qian Peng, Zhenyu Ji
5-aminolevulinic acid (5-ALA)-based photodynamic therapy (PDT) has been successfully used in the treatment of cancers. However, the mechanism of 5-ALA transportation into cancer cells is still not fully elucidated. Previous studies have confirmed that the efficiency of 5-ALA-PDT could be affected by the membrane skeleton protein 4.1R. In this study we investigated the role of 4.1R in the transport of 5-ALA into cells. Wild-type (4.1R(+/+) ) and 4.1R gene knockout (4.1R(-/-) ) mouse embryonic fibroblast (MEF) cells were incubated with 1 mM 5-ALA and different concentrations of specific inhibitors of GABA transporters GAT(1-3)...
September 7, 2017: Photochemistry and Photobiology
https://www.readbyqxmd.com/read/28878016/enantiomeric-barbiturates-bind-distinct-inter-and-intra-subunit-binding-sites-in-a-nicotinic-acetylcholine-receptor-nachr
#4
Zhiyi Yu, Jonathan B Cohen
Nicotinic acetylcholine receptors (nAChRs) and γ-aminobutyric acid type A receptors (GABAARs) are members of the pentameric ligand-gated ion channel superfamily. Drugs acting as positive allosteric modulators of muscle-type α2βγδ nAChRs, of use in treatment of neuromuscular disorders, have been hard to identify. However, identification of nAChR allosteric modulator binding sites has been facilitated by using drugs developed as photoreactive GABAAR modulators. Recently, R-mTFD-MPAB (R-1-methyl-5-allyl-5-(m-trifluoromethyl-diazirinylphenyl) barbituric acid), an anesthetic and GABAAR potentiator, has been shown to inhibit Torpedo α2βγδ nAChRs, binding in the ion channel and to a γ(+)-α(-) subunit interface site similar to its GABAAR intersubunit binding site...
September 6, 2017: Journal of Biological Chemistry
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/28855287/gaba-transporters-regulate-tonic-and-synaptic-gabaa-receptor-mediated-currents-in-the-suprachiasmatic-nucleus-neurons
#7
Michael G Moldavan, Olga Cravetchi, Charles N Allen
GABA is a principal neurotransmitter in the hypothalamic suprachiasmatic nucleus (SCN) that contributes to intercellular communication between individual circadian oscillators within the SCN network and the stability and precision of the circadian rhythms. GABA transporters (GAT) regulate the extracellular GABA concentration and modulate GABAA receptor (GABAAR)-mediated currents. GABA transport inhibitors were applied to study how GABAAR-mediated currents depend on the expression and function of GAT. Nipecotic acid inhibits GABA transport and induced an inward tonic current in concentration-dependent manner during whole-cell patch clamp recordings from SCN neurons...
August 30, 2017: Journal of Neurophysiology
https://www.readbyqxmd.com/read/28841161/disease-modifying-effects-of-the-spider-toxin-parawixin2-in-the-experimental-epilepsy-model
#8
Lívea Dornela Godoy, José Luiz Liberato, Marcus Vinícius Batista Celani, Leonardo Gobbo-Neto, Norberto Peporine Lopes, Wagner Ferreira Dos Santos
(1) Background: Temporal lobe epilepsy (TLE) is the most common type of epilepsy in adults. It is also the one with the highest percentage of drug-resistance to the current available anti-epileptic drugs (AED). Additionaly, most antiepileptic drugs are only able to control seizures in epileptogenesis, but do not decrease the hippocampal neurodegenerative process. TLE patients have a reduced population of interneuronal cells, which express Parvalbumin (PV) proteins. This reduction is directly linked to seizure frequency and severity in the chronic period of epilepsy...
August 25, 2017: Toxins
https://www.readbyqxmd.com/read/28835252/neuroinflammation-contributes-to-autophagy-flux-blockage-in-the-neurons-of-rostral-ventrolateral-medulla-in-stress-induced-hypertension-rats
#9
Dongshu Du, Li Hu, Jiaxiang Wu, Qin Wu, Wenjing Cheng, Yuhong Guo, Ruijuan Guan, Yahui Wang, Xingxin Chen, Xanxia Yan, Danian Zhu, Jijiang Wang, Shutian Zhang, Yanfang Guo, Chunmei Xia
BACKGROUND: Neuroinflammation plays hypertensive roles in the uninjured autonomic nuclei of the central nervous system, while its mechanisms remain unclear. The present study is to investigate the effect of neuroinflammation on autophagy in the neurons of the rostral ventrolateral medulla (RVLM), where sympathetic premotor neurons for the maintenance of vasomotor tone reside. METHODS: Stress-induced hypertension (SIH) was induced by electric foot-shock stressors with noise interventions in rats...
August 23, 2017: Journal of Neuroinflammation
https://www.readbyqxmd.com/read/28828616/astrocytic-gaba-transporters-pharmacological-properties-and-targets-for-antiepileptic-drugs
#10
Arne Schousboe, Petrine Wellendorph, Bente Frølund, Rasmus P Clausen, Povl Krogsgaard-Larsen
Inactivation of GABA-mediated neurotransmission is achieved by high-affinity transporters located at both GABAergic neurons and the surrounding astrocytes. Early studies of the pharmacological properties of neuronal and glial GABA transporters suggested that different types of transporters might be expressed in the two cell types, and such a scenario was confirmed by the cloning of four distinctly different GABA transporters from a number of different species. These GABA-transport entities have been extensively characterized using a large number of GABA analogues of restricted conformation, and several of these compounds have been shown to exhibit pronounced anticonvulsant activity in a variety of animal seizure models...
2017: Advances in Neurobiology
https://www.readbyqxmd.com/read/28818421/erbb-signaling-antagonist-ameliorates-behavioral-deficit-induced-by-phencyclidine-pcp-in-mice-without-affecting-metabolic-syndrome-markers
#11
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/28808187/g-aminobutyric-acid-promotes-methionine-choline-deficient-diet-induced-nonalcoholic-steatohepatitis
#12
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/28807873/neurophysiologically-informed-markers-of-individual-variability-and-pharmacological-manipulation-of-human-cortical-gamma
#13
A D Shaw, R J Moran, S D Muthukumaraswamy, J Brealy, D E Linden, K J Friston, K D Singh
The ability to quantify synaptic function at the level of cortical microcircuits from non-invasive data would be enormously useful in the study of neuronal processing in humans and the pathophysiology that attends many neuropsychiatric disorders. Here, we provide proof of principle that one can estimate inter-and intra-laminar interactions among specific neuronal populations using induced gamma responses in the visual cortex of human subjects - using dynamic causal modelling based upon the canonical microcircuit (CMC; a simplistic model of a cortical column)...
August 12, 2017: NeuroImage
https://www.readbyqxmd.com/read/28807671/selective-inhibition-of-extra-synaptic-%C3%AE-5-gabaa-receptors-by-s44819-a-new-therapeutic-agent
#14
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/28793908/transcriptomic-analysis-comparing-mouse-strains-with-extreme-total-lung-capacities-identifies-novel-candidate-genes-for-pulmonary-function
#15
Leema George, Ankita Mitra, Tania A Thimraj, Martin Irmler, Sangeetha Vishweswaraiah, Lars Lunding, Dorothea Hühn, Alicia Madurga, Johannes Beckers, Heinz Fehrenbach, Swapna Upadhyay, Holger Schulz, George D Leikauf, Koustav Ganguly
BACKGROUND: Failure to attain peak lung function by early adulthood is a risk factor for chronic lung diseases. Previously, we reported that C3H/HeJ mice have about twice total lung capacity (TLC) compared to JF1/MsJ mice. We identified seven lung function quantitative trait loci (QTL: Lfnq1-Lfnq7) in backcross/intercross mice derived from these inbred strains. We further demonstrated, superoxide dismutase 3, extracellular (Sod3), Kit oncogene (Kit) and secreted phosphoprotein 1 (Spp1) located on these Lfnqs as lung function determinants...
August 9, 2017: Respiratory Research
https://www.readbyqxmd.com/read/28782641/nitric-oxide-cgmp-signaling-via-guanylyl-cyclase-isoform-1-modulates-glutamate-and-gaba-release-in-somatosensory-cortex-of-mice
#16
Qi Wang, Evanthia Mergia, Doris Koesling, Thomas Mittmann
In hippocampus, two guanylyl cyclases (NO-GC1 and NO-GC2) are involved in the transduction of the effects of nitric oxide (NO) on synaptic transmission. However, the respective roles of the NO-GC isoforms on synaptic transmission are less clear in other regions of the brain. In the present study, we used knock-out mice deficient for the NO-GC1 isoform (NO-GC1 KO) to analyze its role in the glutamatergic and GABAergic neurotransmission at pyramidal neurons in layers II/III of somatosensory cortex. NO-GC1 KO slices revealed reduced frequencies of miniature excitatory- and inhibitory-postsynaptic currents, increased paired-pulse ratios and decreased input-output curves of evoked signals, which indicated the reduction of glutamate and GABA release in NO-GC1 KO mice...
August 4, 2017: Neuroscience
https://www.readbyqxmd.com/read/28775328/inhibition-of-glutamate-decarboxylase-gad-by-ethyl-ketopentenoate-ekp-induces-treatment-resistant-epileptic-seizures-in-zebrafish
#17
Yifan Zhang, Michiel Vanmeert, Aleksandra Siekierska, Annelii Ny, Jubi John, Geert Callewaert, Eveline Lescrinier, Wim Dehaen, Peter A M de Witte, Rafal M Kaminski
Epilepsy is a chronic brain disorder characterized by recurrent seizures due to abnormal, excessive and synchronous neuronal activities in the brain. It affects approximately 65 million people worldwide, one third of which are still estimated to suffer from refractory seizures. Glutamic acid decarboxylase (GAD) that converts glutamate into GABA is a key enzyme in the dynamic regulation of neural network excitability. Importantly, clinical evidence shows that lowered GAD activity is associated with several forms of epilepsy which are often treatment resistant...
August 3, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28741622/in-vivo-detection-of-cpp-115-target-engagement-in-human-brain
#18
Andrew P Prescot, Steven R Miller, Gary Ingenito, Rebekah S Huber, Douglas G Kondo, Perry F Renshaw
CPP-115, a next-generation γ-amino butyric acid (GABA)-aminotransferase (AT) inhibitor, shows comparable pharmacokinetics, improved safety and tolerability, and a more favorable toxicity profile when compared to vigabatrin. The pharmacodynamic characteristics of CPP-115 remain to be evaluated. The present study employed state-of-the-art proton magnetic resonance spectroscopy techniques to measure changes in brain GABA+ (the composite resonance of GABA, homocarnosine, and macromolecules) concentrations in healthy subjects receiving oral daily doses of CPP-115 or placebo...
July 25, 2017: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28735749/initiation-of-behavioral-response-to-antidepressants-by-cholecystokinin-neurons-of-the-dentate-gyrus
#19
Lucian Medrihan, Yotam Sagi, Zintis Inde, Oleh Krupa, Chelsea Daniels, Adrien Peyrache, Paul Greengard
Selective serotonin reuptake inhibitors (SSRIs) are the most commonly used class of antidepressant drugs, but the cellular and molecular mechanisms by which their therapeutic action is initiated are poorly understood. Here we show that serotonin 5-HT1B receptors in cholecystokinin (CCK) inhibitory interneurons of the mammalian dentate gyrus (DG) initiate the therapeutic response to antidepressants. In these neurons, 5-HT1B receptors are expressed presynaptically, and their activation inhibits GABA release. Inhibition of GABA release from CCK neurons disinhibits parvalbumin (PV) interneurons and, as a consequence, reduces the neuronal activity of the granule cells...
August 2, 2017: Neuron
https://www.readbyqxmd.com/read/28734674/retinal-exposure-to-high-glucose-condition-modifies-the-gabaergic-system-regulation-by-nitric-oxide
#20
R Carpi-Santos, R S Maggesissi, M P von Seehausen, K C Calaza
Diabetic retinopathy is a severe retinal complication that diabetic patients are susceptible to present. Although this disease is currently characterized as a microvascular disease, there is growing evidence that neural changes occur and maybe precede vascular impairments. Using chicken retina, an avascular tissue with no direct contact with blood vessels and neural retina, this study aimed to evaluate the influence of acute exposure to high glucose concentration in the retinal GABAergic system, and the role of nitric oxide (NO) in this modulation...
September 2017: Experimental Eye Research
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