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https://www.readbyqxmd.com/read/29792150/synthesis-and-biological-evaluation-of-novel-2-3-disubstituted-benzofuran-analogues-of-gaba-as-neurotropic-agents
#1
Arturo Coaviche-Yoval, Hector Luna, Ricardo Tovar-Miranda, Marvin Antonio Soriano-Ursua, Jose G Trujillo-Ferrara
BACKGROUND: Benzofurans are heterocyclic compounds with neurotropic activity. Some have been developed for the treatment of acute and degenerative neuronal injuries. OBJECTIVE: To evaluate the in silico binding of some promising benzofurans on the GABA receptors, and the in vivo neurotropic activity of benzofuran analogues (BZF 6-10) of gamma-aminobutyric acid (GABA) on a seizure model. METHODS: The ligands with the best physicochemical attributes were docked on two GABA receptors (the alpha-1 subunit of GABAA-R and GBR1 subunit of GABAB-R)...
May 23, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29790025/ampar-mediated-interictal-discharges-in-neurons-of-entorhinal-cortex-experiment-and-model
#2
A V Chizhov, D V Amakhin, A V Zaizev, L G Magazanik
The mechanisms of interictal discharges (IID) were studied under the conditions of the 4-aminopyridine model of spontaneous epileptiform activity in surviving rat brain slice preparations. Addition of the agents blocking GABA and NMDA receptors failed to inhibit IID generation in the entorhinal cortex. A mathematical model of IID has been developed on the basis of the excitatory neuron interaction mediated by the AMPA receptor. Short-term synaptic depression and slow afterspike-hyperpolarization are the key factors required to terminate a single IID...
March 2018: Doklady Biological Sciences: Proceedings of the Academy of Sciences of the USSR, Biological Sciences Sections
https://www.readbyqxmd.com/read/29787855/dysbiosis-of-microbiome-and-probiotic-treatment-in-a-genetic-model-of-autism-spectrum-disorders
#3
Tabouy Laure, Getselter Dimitry, Ziv Oren, Karpuj Marcela, Tabouy Timothée, Maayouf Rasha, Werbner Nir, Ben-Amram Hila, Nuriel-Ohayon Meital, Koren Omry, Elliott Evan
Recent studies have determined that the microbiome has direct effects on behavior, and may be dysregulated in neurodevelopmental conditions. Considering that neurodevelopmental conditions, such as autism, have a strong genetic etiology, it is necessary to understand if genes associated with neurodevelopmental disorders, such as Shank3, can influence the gut microbiome, and if probiotics can be a therapeutic tool. In this study, we have identified dysregulation of several genera and species of bacteria in the gut and colon of both male and female Shank3 KO mice...
May 19, 2018: Brain, Behavior, and Immunity
https://www.readbyqxmd.com/read/29785777/paradoxical-effect-of-baclofen-on-social-behavior-in-the-fragile-x-syndrome-mouse-model
#4
Shimriet Zeidler, Andreea S Pop, Israa A Jaafar, Helen de Boer, Ronald A M Buijsen, Celine E F de Esch, Ingeborg Nieuwenhuizen-Bakker, Renate K Hukema, Rob Willemsen
INTRODUCTION: Fragile X syndrome (FXS) is a common monogenetic cause of intellectual disability, autism spectrum features, and a broad range of other psychiatric and medical problems. FXS is caused by the lack of the fragile X mental retardation protein (FMRP), a translational regulator of specific mRNAs at the postsynaptic compartment. The absence of FMRP leads to aberrant synaptic plasticity, which is believed to be caused by an imbalance in excitatory and inhibitory network functioning of the synapse...
April 26, 2018: Brain and Behavior
https://www.readbyqxmd.com/read/29785705/association-of-gabaa-receptor-gene-with-epilepsy-syndromes
#5
Musadiq Ahmad Bhat, Sameer Ahmad Guru, Rashid Mir, Ajaz Ahmad Waza, Mariyam Zuberi, Mamta Pervin Sumi, Shaam Bodeliwala, Vinod Puri, Alpana Saxena
GABA has always been an inviting target in the etiology and treatment of epilepsy. The GABRA1, GABRG2, and GABRD genes provide instructions for making α1, ϒ2, and δ subunits of GABAA receptor protein respectively. GABAA is considered as one of the most important proteins and has found to play an important role in many neurological disorders. We explored the association of GABAA receptor gene mutation/SNPs in JME and LGS patients in Indian population. A total of 100 epilepsy syndrome patients (50 JME and 50 LGS) and 100 healthy control subjects were recruited and analyzed by AS-PCR and RFLP-PCR techniques...
May 21, 2018: Journal of Molecular Neuroscience: MN
https://www.readbyqxmd.com/read/29782207/the-benzodiazepine-anesthetic-midazolam-prevents-hyperglycemia-induced-microvascular-leakage-in-the-retinas-of-diabetic-mice
#6
Yeon-Ju Lee, Minsoo Kim, Jee-Yeon Lee, Se-Hui Jung, Hye-Yoon Jeon, Seung Ah Lee, Seongsik Kang, Eun-Taek Han, Won Sun Park, Seok-Ho Hong, Young-Myeong Kim, Kwon-Soo Ha
We investigated the beneficial effects of midazolam against vascular endothelial growth factor (VEGF)-induced vascular leakage and its molecular mechanism of action in human retinal endothelial cells (HRECs) and the retinas of diabetic mice. Midazolam inhibited VEGF-induced elevation of intracellular Ca2+ , generation of reactive oxygen species (ROS), and transglutaminase activation in HRECs; these effects were reversed by the GABA, type A (GABAA ) receptor antagonist flumazenil but not by the translocator protein antagonist PK11195...
May 21, 2018: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/29781560/conditioned-reward-of-opioids-but-not-psychostimulants-is-impaired-in-gaba-a-receptor-%C3%AE-subunit-knockout-mice
#7
Milo S Siivonen, Elena de Miguel, Juho Aaltio, Aino K Manner, Mikko Vahermo, Jari Yli-Kauhaluoma, Anni-Maija Linden, Teemu Aitta-Aho, Esa R Korpi
Extrasynaptic δ subunit-containing γ-aminobutyric acid type A receptors (δ-GABAA Rs) are emerging as targets for a number of neuropsychopharmacological drugs, including the direct GABA-site agonist gaboxadol and neuroactive steroids. Among other regions, these δ-GABAA Rs are functionally expressed in the ventral tegmental area (VTA), the cell body region of mesocorticolimbic dopamine (DA) system important for motivated behaviors, and in the target region, the nucleus accumbens. Gaboxadol and neurosteroids induce VTA DA neuron plasticity ex vivo, by inhibiting the VTA GABA neurons, and aversive place conditioning, which are absent in the δ-GABAA R knockout mice (δ-KO)...
May 21, 2018: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/29778948/bioisosteres-of-ethyl-8-ethynyl-6-pyridin-2-yl-4h-benzo-f-imidazo-1-5-a-1-4-diazepine-3-carboxylate-hz-166-as-novel-alpha-2-3-selective-potentiators-of-gaba-a-receptors-improved-bioavailability-enhances-anticonvulsant-efficacy
#8
J M Witkin, J L Smith, X Ping, S D Gleason, M M Poe, G Li, X Jin, J Hobbs, J M Schkeryantz, J S McDermott, A I Alatorre, J N Siemian, J W Cramer, D C Airey, K R Methuku, V V N P B Tiruveedhula, T M Jones, J Crawford, M J Krambis, J L Fisher, J M Cook, R Cerne
HZ-166 has previously been characterized as an α2,3-selective GABAA receptor modulator with anticonvulsant, anxiolytic, and anti-nociceptive properties but reduced motor effects. We discovered a series of ester bioisosteres with reduced metabolic liabilities, leading to improved efficacy as anxiolytic-like compounds in rats. In the present study, we evaluated the anticonvulsant effects KRM-II-81 across several rodent models. In some models we also evaluated key structural analogs. KRM-II-81 suppressed hyper-excitation in a network of cultured cortical neurons without affecting the basal neuronal activity...
May 3, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29778944/activation-and-blockade-of-basolateral-amygdala-5-ht-6-receptor-produce-anxiolytic-like-behaviors-in-an-experimental-model-of-parkinson-s-disease
#9
Yi-Na Sun, Lu Yao, Li-Bo Li, Yong Wang, Cheng-Xue Du, Yuan Guo, Jian Liu
Although the basolateral amygdala (BLA) and serotonin6 (5-HT6 ) receptor are involved in modulation of anxiety, their roles in Parkinson' disease (PD)-related anxiety are still unknown. Thus we perform this study to examine the involvement of BLA 5-HT6 receptor on anxiety in unilateral 6-hydroxydopamine-induced PD rats. The lesion of the medial forebrain bundle (MFB) induced anxiety-like behaviors, and decreased the basal firing rate of BLA glutamate neurons and dopamine (DA) levels in tissues of the medial prefrontal cortex (mPFC), amygdala and ventral part of hippocampus (vHip) in rats...
May 17, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29778933/neurotoxic-impact-of-acute-tio-2-nanoparticle-exposure-on-a-benthic-marine-bivalve-mollusk-tegillarca-granosa
#10
Xiaofan Guan, Wei Shi, Shanjie Zha, Jiahuan Rong, Wenhao Su, Guangxu Liu
The release of nanoparticles (NPs) into the ocean inevitably poses a threat to marine organisms. However, to date, the neurotoxic effects of NPs remains poorly understood in marine bivalve species. Therefore, in order to gain a better understanding of the physiological effects of NPs, the impact of acute (96 h) TiO2 NP exposure on the in vivo concentrations of three major neurotransmitters, the activity of AChE, and the expression of neurotransmitter-related genes was investigated in the blood clam, Tegillarca granosa...
May 17, 2018: Aquatic Toxicology
https://www.readbyqxmd.com/read/29778459/bisphenol-a-inhibits-improvement-of-testosterone-in-anxiety-and-depression-like-behaviors-in-gonadectomied-male-mice
#11
Yvfeng Liang, Jiahong Li, Tao Jin, Ting Gu, Qingjie Zhu, Yizhong Hu, Yang Yang, Jisui Li, Donghong Wu, Kesheng Jiang, Xiaohong Xu
Bisphenol-A (BPA) is a well-known environmental endocrine disruptor. Developmental exposure to BPA affected a variety of behaviors in multiple model organisms. Our recent study found that exposure to BPA during adulthood aggravated anxiety- and depression-like states in male mice but not in females. In this study, 11-w-old gonadectomied (GDX) male mice daily received subcutaneous injections of testosterone propionate (TP, 0.5 mg/kg), TP and BPA (0.04, 0.4, or 4 mg/kg), or vehicle for 45 days. BPA (0.4 or 4 mg/kg) did not affect the elevated plus maze task of GDX mice but shortened the time on open arms and decreased the frequency of head dips of sham and TP-GDX mice...
May 17, 2018: Hormones and Behavior
https://www.readbyqxmd.com/read/29777728/testosterone-induced-downregulation-of-migration-and-proliferation-in-human-umbilical-vein-endothelial-cells-by-androgen-receptor-dependent-and-independent-mechanisms
#12
Aulona Gaba, Mario Mairhofer, Zyhdi Zhegu, Nadja Leditznig, Ladislaus Szabo, Walter Tschugguel, Christian Schneeberger, Iveta Yotova
Recent research has emphasized the potential unfavorable effects of declining testosterone (T) levels in men and the putative beneficial effect of androgen therapy in select women. Some controversy surrounding the mechanism of action and the effects of T on endothelium remains. In this study, we evaluated the mechanism of T action on pooled primary Human Umbilical Vein Endothelial Cells (HUVEC) of mixed gender by focusing on two important processes, proliferation and migration. In our in vitro model system, we found that only the supra-physiological dose of T affected these two processes irrespective of the ratio of male to female cells in the pools...
May 16, 2018: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/29775659/%C3%AE-2-receptors-in-the-lateral-parabrachial-nucleus-generates-the-pressor-response-of-the-cardiovascular-chemoreflex-effects-of-gaba-a-receptor
#13
Nafiseh Mirzaei Damabi, Gholam Reza Namvar, Fahimeh Yeganeh, Masoumeh Hatam
The lateral parabrachial nucleus (LPBN) is a pontine area involved in cardiovascular chemoreflex. This study was performed to find the effects of reversible synaptic blockade of the LPBN on the chemoreflex responses, and to find the roles of GABAA receptor and α2 -adenoreceptor (α2 -AR) in chemoreflex. It also aimed to seek possible interaction between GABA and noradrenergic systems of the LPBN in urethane-anesthetized male rats. Cardiovascular chemoreflex was activated by intravenous injection of potassium cyanide (KCN, 80 μg/kg)...
May 15, 2018: Brain Research Bulletin
https://www.readbyqxmd.com/read/29767950/different-benzodiazepines-bind-with-distinct-binding-modes-to-gaba-a-receptors
#14
Alshaimaa A Elgarf, David C B Siebert, Friederike Steudle, Angelika Draxler, Guanguan Li, Shengming Huang, James M Cook, Margot Ernst, Petra Scholze
Benzodiazepines are clinically relevant drugs, which bind to GABAA neurotransmitter receptors at the α+/γ2- interfaces and thereby enhance GABA induced chloride ion flux leading to neuronal hyperpolarization. However, the structural basis of benzodiazepine interactions with their high affinity site at GABAA receptors is controversially debated in the literature and in silico studies led to discrepant binding mode hypotheses. In the current study computational docking of diazepam into α+/γ2- homology models suggested that a chiral methyl group, which is known to promote preferred binding to α5-containing GABAA receptors (position 3 of the 7-membered diazepine ring), could possibly provide experimental evidence in favor of or against the so far proposed binding modes...
May 16, 2018: ACS Chemical Biology
https://www.readbyqxmd.com/read/29766792/gabaa-receptors-various-stoichiometrics-of-subunit-arrangement-in-%C3%AE-1%C3%AE-3-and-%C3%AE-1%C3%AE-3%C3%AE%C2%B5-receptors
#15
Ahmad Tarmizi Che Has, Mary Chebib
GABAA receptors (GABAARs) are members of the Cys-loop ligand-gated ion channel (LGIC) superfamily, which includes nicotinic acetylcholine, glycine, and serotonin (5HT3) receptors [1,2,3,4]. LGICs typically mediate fast synaptic transmission via the movement of ions through channels gated by neurotransmitters, such as acetylcholine for nicotinic receptors and GABA for GABAARs [5]. The term Cys-loop receptors originates from the presence of a conserved disulphide bond (or bridge) which holds together two cysteine amino acids of the loop that forms from the structure of polypeptides in the extracellular domain of the receptor's subunit [6]...
May 15, 2018: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/29763549/development-of-positron-emission-tomography-pet-radiotracers-for-the-gaba-transporter-1-gat-1
#16
Alexandra R Sowa, Allen F Brooks, Xia Shao, Bradford D Henderson, Phillip S Sherman, Janna Arteaga, Jenelle Stauff, Adam C Lee, Robert A Koeppe, Peter J H Scott, Michael R Kilbourn
In vivo PET imaging of the γ-aminobutyric acid (GABA) receptor complex has been accomplished using radiolabeled benzodiazepine derivatives, but development of specific presynaptic radioligands targeting the neuronal membrane GABA transporter type 1 (GAT-1) has been less successful. The availability of new structure-activity studies of GAT-1 inhibitors and the introduction of a GAT-1 inhibitor (tiagabine, Gabatril® ) into clinical use prompted us to reinvestigate the syntheses of PET ligands for this transporter...
May 15, 2018: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29758348/effect-of-prenatal-stress-on-%C3%A9-5-gaba-a-receptor-subunit-gene-expression-in-hippocampus-and-pilocarpine-induced-seizure-in-rats
#17
Mehrdad Nejatbakhsh, Ehsan Saboory, Morteza Bagheri
The GABAergic synapses go through structural and functional maturation during early brain development. Maternal stress alters GABAergic synapses in developing brain, which are associated with the pathophysiology of neuropsychiatric disorders in adults. The present study aimed to investigate the effect of prenatal restraint stress (PS) on pilocarpine-induced seizure and ɑ5 subunit of γ-amino butyric acid type A (GABAA ) receptor expression in hippocampus. Pregnant Wistar rats were subjected to PS at gestational days 15-17 and the pups were examined for susceptibility to seizure and ɑ5 subunit of GABAA receptor expression in hippocampus at postnatal days 14 and 21 (P14 and PND 21)...
May 11, 2018: International Journal of Developmental Neuroscience
https://www.readbyqxmd.com/read/29758302/plasminogen-binding-inhibitors-demonstrate-unwanted-activities-on-gaba-a-and-glycine-receptors-in-human-ipsc-derived-neurons
#18
Lisbeth Kristensson, Anders Lundin, David Gustafsson, Jan Fryklund, Tomas Fex, Delsing Louise, Erik Ryberg
Plasminogen binding inhibitors (PBIs) reduce the risk of bleeding in hemorrhagic conditions. However, generic PBIs are also associated with an increased risk of seizures, an adverse effect linked to unwanted activities towards inhibitory neuronal receptors. Development of novel PBIs serve to remove compounds with such properties, but progress is limited by a lack of higher throughput methods with human translatability. Herein we apply human induced pluripotent stem cell (hiPSC) derived neurons in combination with dynamic mass redistribution (DMR) technology to demonstrate robust and reproducible modulation of both GABAA and glycine receptors...
May 11, 2018: Neuroscience Letters
https://www.readbyqxmd.com/read/29758086/cholinergic-excitation-complements-glutamate-in-coding-visual-information-in-retinal-ganglion-cells
#19
Santhosh Sethuramanujam, Gautam B Awatramani, Malcolm M Slaughter
Starburst amacrine cells release GABA and acetylcholine This study explores the coordinated function of starburst mediated cholinergic excitation and GABAergic inhibition to bistratified retinal ganglion cells, predominantly direction-selective ganglion cells (DSGCs) In rat retina, under our recording conditions, starbursts were found to provide the major excitatory drive to a sub-population of ganglion cells whose dendrites co-stratify with starburst dendrites (putative DSGCs) In mouse retina, recordings from genetically identified DSGCs at physiological temperatures reveal that ACh inputs dominate the response to small spot-high contrast light stimuli, with preferential addition of bipolar cell input shifting the balance towards glutamate for larger spot stimuli In addition, starbursts also appear to gate glutamatergic excitation to DSGCs by postsynaptic and possibly presynaptic inhibitory processes ABSTRACT: Starburst amacrine cells release both GABA and acetylcholine (ACh), allowing them to simultaneously mediate inhibition and excitation...
May 14, 2018: Journal of Physiology
https://www.readbyqxmd.com/read/29755370/effects-of-ethanol-on-sensory-inputs-to-the-medial-giant-interneurons-of-crayfish
#20
Matthew E Swierzbinski, Jens Herberholz
Crayfish are capable of two rapid, escape reflexes that are mediated by two pairs of giant interneurons, the lateral giants (LG) and the medial giants (MG), which respond to threats presented to the abdomen or head and thorax, respectively. The LG has been the focus of study for many decades and the role of GABAergic inhibition on the escape circuit is well-described. More recently, we demonstrated that the LG circuit is sensitive to the acute effects of ethanol and this sensitivity is likely mediated by interactions between ethanol and the GABAergic system...
2018: Frontiers in Physiology
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