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Gaba a inhibitor

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https://www.readbyqxmd.com/read/29339464/propionate-enters-gabaergic-neurons-inhibits-gaba-transaminase-causes-gaba-accumulation-and-lethargy-in-a-model-of-propionic-acidemia
#1
Cecilie Morland, Anne-Sofie Frøland, Mi Nyguyen Pettersen, Jon Storm-Mathisen, Vidar Gundersen, Frode Rise, Bjørnar Hassel
Propionic acidemia is the accumulation of propionate in blood due to dysfunction of propionyl-CoA carboxylase. The condition causes lethargy and striatal degeneration with motor impairment in humans. How propionate exerts its toxic effect is unclear. Here we show that intravenous administration of propionate causes dose-dependent propionate accumulation in the brain and transient lethargy in mice. Propionate, an inhibitor of histone deacetylase, entered GABAergic neurons, as could be seen from increased neuronal histone H4 acetylation in striatum and neocortex...
January 16, 2018: Biochemical Journal
https://www.readbyqxmd.com/read/29336266/design-synthesis-evaluation-and-computational-studies-of-nipecotic-acid-acetonaphthone-hybrids-as-potential-antiepileptic-agents
#2
Ankit Seth, Piyoosh A Sharma, Avanish Tripathi, Priyanka K Choubey, Pavan Srivastava, Prabhash N Tripathi, Sushant Kumar Shrivastava
BACKGROUND: Nipecotic acid is considered to be one of the most potent inhibitors of neuronal and glial γ- aminobutyric acid (GABA) uptake in vitro. However nipecotic acid does not readily cross the blood-brain barrier (BBB) following peripheral administration, owing to its hydrophilic nature. OBJECTIVE: A series of substituted acetonaphthones tethered nipecotic acid derivatives were designed and synthesized with an aim to improve the lipophilicity and the blood-brain barrier (BBB) permeation...
January 15, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29295561/exploring-the-mechanisms-of-electroacupuncture-induced-analgesia-through-rna-sequencing-of-the-periaqueductal-gray
#3
Man-Li Hu, Hong-Mei Zhu, Qiu-Lin Zhang, Jing-Jing Liu, Yi Ding, Ju-Ming Zhong, Vitaly Vodyanoy, Ming-Xing Ding
Electroacupuncture (EA) can relieve various pains. However, its mechanism in terms of the transcriptome is still not well-known. To explore the full profile of EA-induced molecular modification in the central nerve system, three twins of goats were selected for a match-paired experiment: EA stimulation (60 Hz, 30 min) and none-EA (control). Goats in the EA group showed an increased (p < 0.05) nociceptive threshold compared with the control goats. Experimental goats were sacrificed at 4 h of the experiment, and the periaqueductal grays were harvested for RNA sequencing...
December 25, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29295521/molecular-targets-for-components-of-essential-oils-in-the-insect-nervous-system-a-review
#4
REVIEW
Milena Jankowska, Justyna Rogalska, Joanna Wyszkowska, Maria Stankiewicz
Essential oils (EOs) are lipophilic secondary metabolites obtained from plants; terpenoids represent the main components of them. A lot of studies showed neurotoxic actions of EOs. In insects, they cause paralysis followed by death. This feature let us consider components of EOs as potential bioinsecticides. The inhibition of acetylcholinesterase (AChE) is the one of the most investigated mechanisms of action in EOs. However, EOs are rather weak inhibitors of AChE. Another proposed mechanism of EO action is a positive allosteric modulation of GABA receptors (GABArs)...
December 23, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29203576/dimethoxy-etomidate-a-non-hypnotic-etomidate-analog-that-potently-inhibits-steroidogenesis
#5
Megan McGrath, Celena Ma, Douglas Raines
Cushing's syndrome is characterized by the overproduction of adrenocortical steroids. Steroidogenesis inhibitors are mainstays of medical therapy for Cushing's syndrome; unfortunately, adverse side effects and treatment failures are common with currently available drugs. The general anesthetic induction agent etomidate is among the most potent inhibitors of adrenocortical steroidogenesis. However, its use as a treatment for Cushing's syndrome is complicated by its sedative-hypnotic activity and ability to produce myoclonus, central nervous system actions thought to be mediated by the GABAA receptor...
December 4, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29200913/developmental-changes-in-gabaa-tonic-inhibition-are-compromised-by-multiple-mechanisms-in-preadolescent-dentate-gyrus-granule-cells
#6
Sudip Pandit, Gyu Seung Lee, Jin Bong Park
The sustained tonic currents (Itonic) generated by γ-aminobutyric acid A receptors (GABAARs) are implicated in diverse age-dependent brain functions. While various mechanisms regulating Itonic in the hippocampus are known, their combined role in Itonic regulation is not well understood in different age groups. In this study, we demonstrated that a developmental increase in GABA transporter (GAT) expression, combined with gradual decrease in GABAAR α5 subunit, resulted in various Itonic in the dentate gyrus granule cells (DGGCs) of preadolescent rats...
November 2017: Korean Journal of Physiology & Pharmacology
https://www.readbyqxmd.com/read/29199177/inhibition-of-glycogen-phosphorylase-stimulates-ventromedial-hypothalamic-nucleus-amp-activated-protein-kinase-activity-and-neuronal-nitric-oxide-synthase-protein-expression-in-male-rats
#7
Hussain N Alhamami, Ayed Alshamrani, Karen P Briski
The glucose polymer glycogen is a vital fuel reserve in the brain. The mediobasal hypothalamic energy sensor AMP-activated protein kinase (AMPK) maintains glucostasis via neurotransmitter mechanisms that suppress [γ-aminobutyric acid; GABA] or stimulate [nitric oxide; steroidogenic factor-1 (SF1)] counter-regulatory outflow. This study investigated whether glycogen-derived fuel supply is a critical screened variable in ventromedial hypothalamic nucleus (VMN) monitoring of neuro-metabolic stability during glucostasis and/or insulin (I)-induced hypoglycemia...
December 2017: Physiological Reports
https://www.readbyqxmd.com/read/29183829/the-rodent-versus-wild-snake-paradigm-as-a-model-for-studying-anxiety-and-panic-like-behaviors-face-construct-and-predictive-validities
#8
Tatiana Paschoalin-Maurin, Tayllon Dos Anjos-Garcia, Luiz Luciano Falconi-Sobrinho, Renato Leonardo de Freitas, Jade Pissamiglio Cysne Coimbra, Carlos Júlio Laure, Norberto Cysne Coimbra
Using an innovative approach to study the neural bases of psychiatric disorders, this study investigated the behavioral, morphological and pharmacological bases of panic attack-induced responses in a prey-versus-coral snake paradigm. Mesocricetus auratus was chronically treated with intraperitoneal administration of the selective serotonin uptake inhibitor paroxetine or the gamma aminobutyric acid (GABA)/benzodiazepine receptor agonist alprazolam at three different doses and were then confronted with a venomous coral snake (Micrurus frontalis, Reptilia, Colubridae)...
November 25, 2017: Neuroscience
https://www.readbyqxmd.com/read/29182616/marble-burying-as-compulsive-behaviors-in-male-and-female-mice
#9
George T Taylor, Sandra Lerch, Sabine Chourbaji
Marble burying is considered an, albeit controversial, animal model of the compulsive like behaviors of obsessive-compulsive disorder (OCD). Hallmark features of OCD patients are similarities and, more prominent, differences from anxiety disorders, e.g., the absence of sex differences and resistance to spontaneous remission. We report an experiment on marble burying by male and female C57/BL6/N mice. Animals were administered either the classic anxiolytic drug, diazepam, that targets the GABA receptor or a "pure" inhibitor of the serotonin transporter, escitalopram, that has been reported to be particularly effective in OCD...
2017: Acta Neurobiologiae Experimentalis
https://www.readbyqxmd.com/read/29174531/can-we-increase-speed-and-efficacy-of-antidepressant-treatments-part-i-general-aspects-and-monoamine-based-strategies
#10
REVIEW
Francesc Artigas, Analia Bortolozzi, Pau Celada
Major depressive disorder (MDD) is a severe psychiatric syndrome with high prevalence and socioeconomic impact. Current antidepressant treatments are based on the blockade of serotonin (5-hydroxytryptamine, 5-HT) and/or noradrenaline transporters. These drugs show slow onset of clinical action and limited efficacy, partly due to the activation of physiological negative feed-back mechanisms operating through autoreceptors (5-HT1A, 5-HT1B, α2-adrenoceptors) and postsynaptic receptors (e.g., 5-HT3). As a result, clinically-relevant doses of reuptake inhibitors increase extracellular (active) 5-HT concentrations in the midbrain raphe nuclei but not in forebrain, as indicated by rodent microdialysis studies and by PET-scan studies in primate/human brain...
November 21, 2017: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/29167116/medullary-raphe-nuclei-activate-the-lumbosacral-defecation-center-through-the-descending-serotonergic-pathway-to-regulate-colorectal-motility-in-rats
#11
Hiroyuki Nakamori, Kiyotada Naitou, Yuuki Horii, Hiroki Shimaoka, Kazuhiro Horii, Hiroki Sakai, Akihiro Yamada, Hidemasa Furue, Takahiko Shiina, Yasutake Shimizu
Colorectal motility is regulated by two defecation centers located in the brain and spinal cord. In previous studies, we have shown that administration of serotonin into the lumbosacral spinal cord causes enhancement of colorectal motility. Since spinal serotonin is derived from neurons of the medullary raphe nuclei including the raphe magnus, raphe obscurus and raphe pallidus, we examined whether stimulation of the medullary raphe nuclei enhances colorectal motility via the lumbosacral defecation center. Colorectal pressure was recorded with a balloon in vivo in anesthetized rats...
November 22, 2017: American Journal of Physiology. Gastrointestinal and Liver Physiology
https://www.readbyqxmd.com/read/29148909/inhibition-of-gaba-transporters-fails-to-afford-significant-protection-following-focal-cerebral-ischemia
#12
Maria Ek Lie, Emma K Gowing, Rasmus P Clausen, Petrine Wellendorph, Andrew N Clarkson
Brain ischemia triggers excitotoxicity and cell death, yet no neuroprotective drugs have made it to the clinic. While enhancing GABAergic signaling to counterbalance excitotoxicity has shown promise in animal models, clinical studies have failed. Blockade of GABA transporters (GATs) offers an indirect approach to increase GABA inhibition to lower the excitation threshold of neurons. Among the GATs, GAT1 is known to promote neuroprotection, while the protective role of the extrasynaptic transporters GAT3 and BGT1 is elusive...
January 1, 2017: Journal of Cerebral Blood Flow and Metabolism
https://www.readbyqxmd.com/read/29146941/developmental-excitatory-to-inhibitory-gaba-polarity-switch-is-disrupted-in-22q11-2-deletion-syndrome-a-potential-target-for-clinical-therapeutics
#13
Hayder Amin, Federica Marinaro, Davide De Pietri Tonelli, Luca Berdondini
Individuals with 22q11.2 microdeletion syndrome (22q11.2 DS) show cognitive and behavioral dysfunctions, developmental delays in childhood and risk of developing schizophrenia and autism. Despite extensive previous studies in adult animal models, a possible embryonic root of this syndrome has not been determined. Here, in neurons from a 22q11.2 DS mouse model (Lgdel (+/-)), we found embryonic-premature alterations in the neuronal chloride cotransporters indicated by dysregulated NKCC1 and KCC2 protein expression levels...
November 16, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29131576/pharmacological-characterization-of-3h-atpca-as-a-substrate-for-studying-the-functional-role-of-the-betaine-gaba-transporter-1-and-the-creatine-transporter
#14
Anas Al-Khawaja, Anne S Haugaard, Ales Marek, Rebekka Löffler, Louise Thiesen, Monica Santiveri, Maria Damgaard, Christoffer Bundgaard, Bente Frølund, Petrine Wellendorph
The betaine/γ-aminobutyric acid (GABA) transporter 1 (BGT1) is one of the four GABA transporters (GATs) involved in the termination of GABAergic neurotransmission. Although suggested to be implicated in seizure management, the exact functional importance of BGT1 in the brain is still elusive. This is partly owing to the lack of potent and selective pharmacological tool compounds that can be used to probe its function. We previously reported the identification of 2-amino-1,4,5,6-tetrahydropyrimidine-5-carboxylic acid (ATPCA), a selective substrate for BGT1 over GAT1/GAT3, but also an agonist for GABAA receptors...
November 13, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29127598/gaba-uptake-inhibition-reduces-in-vivo-extraction-fraction-in-the-ventral-tegmental-area-of-long-evans-rats-measured-by-quantitative-microdialysis-under-transient-conditions
#15
Shannon L Zandy, Rueben A Gonzales
Inhibitory signaling in the ventral tegmental area (VTA) is involved in the mechanism of action for many drugs of abuse. Although drugs of abuse have been shown to alter extracellular γ-aminobutyric acid (GABA) concentration in the VTA, knowledge on how uptake mechanisms are regulated in vivo is limited. Quantitative (no-net-flux) microdialysis is commonly used to examine the extracellular concentration and clearance of monoamine neurotransmitters, however it is unclear whether this method is sensitive to changes in clearance for amino acid neurotransmitters such as GABA...
November 10, 2017: Neurochemical Research
https://www.readbyqxmd.com/read/29123263/nuclear-igf-1r-predicts-chemotherapy-and-targeted-therapy-resistance-in-metastatic-colorectal-cancer
#16
Jordi Codony-Servat, Miriam Cuatrecasas, Elena Asensio, Carla Montironi, Anna Martínez-Cardús, Mercedes Marín-Aguilera, Carlos Horndler, Eva Martínez-Balibrea, Michele Rubini, Pedro Jares, Oscar Reig, Iván Victoria, Lydia Gaba, Marta Martín-Richard, Vicente Alonso, Pilar Escudero, Carlos Fernández-Martos, Jaime Feliu, Jose Carlos Méndez, Miguel Méndez, Javier Gallego, Antonieta Salud, Federico Rojo, Antoni Castells, Aleix Prat, Rafael Rosell, Xabier García-Albéniz, Jordi Camps, Joan Maurel
BACKGROUND: Although chemotherapy is the cornerstone treatment for patients with metastatic colorectal cancer (mCRC), acquired chemoresistance is common and constitutes the main reason for treatment failure. Monoclonal antibodies against insulin-like growth factor-1 receptor (IGF-1R) have been tested in pre-treated mCRC patients, but results have been largely deceiving. METHODS: We analysed time to progression, overall survival, and the mutational status of RAS, BRAF and nuclear p-IGF-1R expression by immunohistochemistry, in 470 metastatic CRC patients...
November 9, 2017: British Journal of Cancer
https://www.readbyqxmd.com/read/29093445/blood-meal-acquisition-enhances-arbovirus-replication-in-mosquitoes-through-activation-of-the-gabaergic-system
#17
Yibin Zhu, Rudian Zhang, Bei Zhang, Tongyan Zhao, Penghua Wang, Guodong Liang, Gong Cheng
Mosquitoes are hematophagous insects that carry-on and transmit many human viruses. However, little information is available regarding the common mechanisms underlying the infection of mosquitoes by these viruses. In this study, we reveal that the hematophagous nature of mosquitoes contributes to arboviral infection after a blood meal, which suppresses antiviral innate immunity by activating the GABAergic pathway. dsRNA-mediated interruption of the GABA signaling and blockage of the GABAA receptor by the specific inhibitors both significantly impaired arbovirus replication...
November 2, 2017: Nature Communications
https://www.readbyqxmd.com/read/29089046/the-novel-isoxazoline-ectoparasiticide-lotilaner-credelio%C3%A2-a-non-competitive-antagonist-specific-to-invertebrates-%C3%AE-aminobutyric-acid-gated-chloride-channels-gabacls
#18
Lucien Rufener, Vanessa Danelli, Daniel Bertrand, Heinz Sager
BACKGROUND: The isoxazolines are a novel class of parasiticides that are potent inhibitors of γ-aminobutyric acid (GABA)-gated chloride channels (GABACls) and, to a lesser extent, of inhibitory glutamate-gated chloride channels (GluCls). Lotilaner (Credelio™), a novel representative of this chemical class, is currently evaluated for its excellent ectoparasiticide properties. METHODS: In this study, we investigated the molecular mode of action and pharmacology of lotilaner...
November 1, 2017: Parasites & Vectors
https://www.readbyqxmd.com/read/29054135/alterations-in-the-timing-of-huperzine-a-cerebral-pharmacodynamics-in-the-acute-traumatic-brain-injury-setting
#19
Ugur Damar, Roman Gersner, Joshua T Johnstone, Kush Kapur, Stephen Collins, Steven Schachter, Alexander Rotenberg
Traumatic brain injury (TBI) may affect the pharmacodynamics of centrally acting drugs. Paired-pulse transcranial magnetic stimulation (ppTMS) is a safe and noninvasive measure of cortical gamma-aminobutyric acid (GABA)-mediated cortical inhibition. Huperzine A (HupA) is a naturally occurring acetylcholinesterase inhibitor with newly discovered potent GABA-mediated antiepileptic capacity, which is reliably detected by ppTMS. To test whether TBI alters cerebral HupA pharmacodynamics, we exposed rats to fluid percussion injury (FPI) and tested whether ppTMS metrics of cortical inhibition differ in magnitude and temporal pattern in injured rats...
November 21, 2017: Journal of Neurotrauma
https://www.readbyqxmd.com/read/29054014/sex-differences-in-behavioral-and-neurochemical-effects-of-gonadectomy-and-aromatase-inhibition-in-rats
#20
N Kokras, N Pastromas, D Papasava, C de Bournonville, C A Cornil, C Dalla
Aromatase inhibitors, which are widely used for the treatment of estrogen-dependent cancers, have been associated with psychiatric side effects ranging from mania to depression. In the present study, we investigated sex differences in the behavioral and neurochemical effects of aromatase inhibition on male and female, sham-operated or gonadectomized adult rats. Three weeks after surgery, rats received chronic treatment with the aromatase inhibitor letrozole or vehicle and were then subjected to the open field test, which assesses general activity...
October 10, 2017: Psychoneuroendocrinology
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