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https://www.readbyqxmd.com/read/28546314/chronic-stress-induced-behavioral-changes-associated-with-subregion-selective-serotonin-cell-death-in-the-dorsal-raphe
#1
Reka Natarajan, Laura Forrester, Nicolas Chiaia, Bryan K Yamamoto
The current study examined the neurochemical mechanisms and neuroanatomical changes underlying co-existing behavioral effects associated with chronic stress-induced alterations in serotonin (5HT) neurons. Chronic unpredictable stress (CUS) to adult male rats produced depression-like changes with cognitive dysfunction and selective cell death in the interfascicular nucleus of the dorsal raphe (DRif) resulting in decreased 5HTergic innervation of medial prefrontal cortex (mPFC). Twenty-one days of CUS decreased basal plasma levels of corticosterone and produced a shorter latency to immobility and longer durations of immobility in the force-swim test that persisted for one month after CUS...
May 25, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28545490/glutamate-signaling-through-the-nmda-receptor-reduces-the-expression-of-scleraxis-in-plantaris-tendon-derived-cells
#2
Christoph Spang, Ludvig J Backman, Sandrine Le Roux, Jialin Chen, Patrik Danielson
BACKGROUND: A body of evidence demonstrating changes to the glutaminergic system in tendinopathy has recently emerged. This hypothesis was further tested by studying the effects of glutamate on the tenocyte phenotype, and the impact of loading and exposure to glucocorticoids on the glutamate signaling machinery. METHODS: Plantaris tendon tissue and cultured plantaris tendon derived cells were immunohisto-/cytochemically stained for glutamate, N-Methyl-D-Aspartate receptor 1 (NMDAR1) and vesicular glutamate transporter 2 (VGluT2)...
May 25, 2017: BMC Musculoskeletal Disorders
https://www.readbyqxmd.com/read/28542026/combination-drug-therapy-of-pioglitazone-and-d-cycloserine-attenuates-chronic-orofacial-neuropathic-pain-and-anxiety-by-improving-mitochondrial-function-following-trigeminal-nerve-injury
#3
Danielle N Lyons, Liping Zhang, Jignesh D Pandya, Robert J Danaher, Fei Ma, Craig S Miller, Patrick G Sullivan, Cristian Sirbu, Karin N Westlund
OBJECTIVES: The study aim was to determine how peripheral trigeminal nerve injury affects mitochondrial respiration and to test efficacy of combined treatment with two FDA approved drugs with potential for improving mitochondrial bioenergetics, pain and anxiety related behaviors in a chronic orofacial neuropathic pain mouse model. METHODS: Efficacy of (R)-(+)-4-amino-3-isoxazolidinone (D-cycloserine, DCS), an NMDA antagonist/agonist, and Pioglitazone (PIO), a selective agonist of nuclear receptor peroxisome proliferator-activated receptor gamma (PPARγ) was investigate in the trigeminal inflammatory compression (TIC) neuropathic nerve injury mouse model...
May 24, 2017: Clinical Journal of Pain
https://www.readbyqxmd.com/read/28536523/positive-modulatory-interactions-of-nmda-receptor-glun1-2b-ligand-binding-domains-attenuate-antagonists-activity
#4
Douglas Bledsoe, Ceyhun Tamer, Ivana Mesic, Christian Madry, Bradley G Klein, Bodo Laube, Blaise M Costa
N-methyl D-aspartate receptors (NMDAR) play crucial role in normal brain function and pathogenesis of neurodegenerative and psychiatric disorders. Functional tetra-heteromeric NMDAR contains two obligatory GluN1 subunits and two identical or different non-GluN1 subunits that include six different gene products; four GluN2 (A-D) and two GluN3 (A-B) subunits. The heterogeneity of subunit combination facilities the distinct function of NMDARs. All GluN subunits contain an extracellular N-terminal Domain (NTD) and ligand binding domain (LBD), transmembrane domain (TMD) and an intracellular C-terminal domain (CTD)...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28536503/epigenetic-activation-of-asct2-in-the-hippocampus-contributes-to-depression-like-behavior-by-regulating-d-serine-in-mice
#5
Jiesi Wang, Ke Zhang, Xiaojuan Chen, Xiaoqian Liu, Huajing Teng, Mei Zhao, Zhongsheng Sun
The roles of D-serine in depression are raised concerned recently as an intrinsic co-agonist for the NMDA receptor. However, the mechanisms underlying its regulation are not fully elucidated. ASCT2 is a Na(+)-dependent D-serine transporter. We found that decreased D-serine and increased hippocampal ASCT2 levels correlated with chronic social defeat stress (CSDS) in mice. Lentivirus-mediated shRNA-mediated knockdown of ASCT2 and the administration of exogenous D-serine in the hippocampus alleviated CSDS-induced social avoidance and immobility...
2017: Frontiers in Molecular Neuroscience
https://www.readbyqxmd.com/read/28526161/an-update-on-nonopioids-intravenous-or-oral-analgesics-for-perioperative-pain-management
#6
REVIEW
Alan D Kaye, Elyse M Cornett, Erik Helander, Bethany Menard, Eric Hsu, Brendon Hart, Andrew Brunk
Despite an appreciation for many unwanted physiologic effects from inadequate postoperative pain relief, moderate to severe postoperative pain remains commonplace. Although treatment options have evolved in recent years, the use of nonopioid analgesics agents can reduce acute pain-associated morbidity and mortality. This review focuses on the importance of effective postoperative nonopioid analgesic agents, such as acetaminophen, nonsteroidal anti-inflammatory agents, gabapentinoid agents, NMDA antagonists, alpha 2 agonists, and steroids, in opioid sparing and enhancing recovery...
June 2017: Anesthesiology Clinics
https://www.readbyqxmd.com/read/28514141/subtype-specific-agonists-for-nmda-receptor-glycine-binding-sites
#7
Alex Maolanon, Rune Risgaard, Shuang-Yan Wang, Yoran Snoep, Athanasios Papangelis, Feng Yi, David Holley, Anne F Barslund, Niels Svenstrup, Kasper B Hansen, Rasmus Prætorius Clausen
A series of analogues based on serine as lead structure were designed and their agonist activities were evaluated at recombinant NMDA receptor subtypes (GluN1/2A-D) using two-electrode voltage-clamp (TEVC) electrophysiology. Pronounced variation in subunit-selectivity, potency, and agonist efficacy was observed in a manner that was dependent on the GluN2 subunit in the NMDA receptor. In particular, compounds 15a and 16a are potent GluN2C-specific superagonists at the GluN1 subunit with agonist efficacies of 398% and 308% compared to glycine...
May 17, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28512009/combining-d-cycloserine-with-appetitive-extinction-learning-modulates-amygdala-activity-during-recall
#8
Claudia Ebrahimi, Stefan P Koch, Eva Friedel, Ilsoray Crespo, Thomas Fydrich, Andreas Ströhle, Andreas Heinz, Florian Schlagenhauf
Appetitive Pavlovian conditioning plays a crucial role in the pathogenesis of drug addiction and conditioned reward cues can trigger craving and relapse even after long phases of abstinence. Promising preclinical work showed that the NMDA-receptor partial agonist D-cycloserine (DCS) facilitates Pavlovian extinction learning of fear and drug cues. Furthermore, DCS-augmented exposure therapy seems to be beneficial in various anxiety disorders, while the supposed working mechanism of DCS during human appetitive or aversive extinction learning is still not confirmed...
May 13, 2017: Neurobiology of Learning and Memory
https://www.readbyqxmd.com/read/28511005/characterization-of-l-theanine-excitatory-actions-on-hippocampal-neurons-towards-the-generation-of-novel-n-methyl-d-aspartate-receptor-modulators-based-on-its-backbone
#9
Fatiha Sebih, Matthieu Rousset, Salima Bellahouel, Marc Rolland, Marie Celeste de Jesus Ferreira, Janique Guiramand, Catherine Cohen-Solal, Gérard Barbanel, Thierry Cens, Mohammed Abouazza, Adrien Tassou, Maud Gratuze, Céline Meunier, Pierre Charnet, Michel Vignes, Valérie Rolland
L-Theanine (or L-γ-N-ethyl-glutamine) is the major amino acid found in Camellia sinensis. It has received much attention because of its pleiotropic physiological and pharmacological activities leading to health benefits in humans, especially. We describe here a new, easy, efficient and environmentally-friendly chemical synthesis of L-Theanine and L-γ-N-propyl-Gln and their corresponding D isomers. L-Theanine, and its derivatives obtained so far, exhibited partial co-agonistic action at N-methyl-D-aspartate (NMDA) receptors, with no detectable agonist effect at other glutamate receptors, on cultured hippocampal neurons...
May 16, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28506554/selective-dopamine-receptor-4-activation-mediates-the-hippocampal-neuronal-calcium-response-via-ip3-and-ryanodine-receptors
#10
Ya-Li Wang, Jian-Gang Wang, Fang-Li Guo, Xia-Huan Gao, Dan-Dan Zhao, Lin Zhang, Jian-Zhi Wang, Cheng-Biao Lu
Intracellular calcium is a key factor in most cellular processes, including cell growth, differentiation, proliferation and neurotransmitter release. Dopamine (DA) mediates synaptic transmission by regulating the intracellular calcium content. It is not clear, however, which specific subunit of the DA receptor contributes to DA modulation of intracellular calcium content changes. Through the traditional technique of Fura-2 calcium imaging, this study demonstrated that the DA can induce transient calcium in cultured hippocampal neurons and that this response can be mimicked by a selective dopamine receptor 4 (DR4) agonist PD168077 (PD)...
May 12, 2017: Brain Research
https://www.readbyqxmd.com/read/28500623/simultaneous-inhibition-of-nmda-and-mglu1-5-receptors-by-levo-corydalmine-in-rat-spinal-cord-attenuates-bone-cancer-pain
#11
Wen-Ling Dai, Bing Yan, Nan Jiang, Juan-Juan Wu, Xiu-Feng Liu, Ji-Hua Liu, Bo-Yang Yu
Bone cancer pain is a challenge for its not completely clarified mechanism and broad clinical morbidity. Therefore, novel and more effective drugs are urgent needed for improvement of patients' quality of life. Glutamate receptors have been associated with the development of the central sensitization of chronic pain. Inhibition of N-methyl-D-aspartate (NMDA) and metabotropic glutamate (mGlu) receptors can effectively attenuate bone cancer pain respectively. Herein, our results indicated that levo-Corydalmine (l-CDL), a compound from Corydalis yanhusuo W...
May 13, 2017: International Journal of Cancer. Journal International du Cancer
https://www.readbyqxmd.com/read/28486923/kynurenic-acid-and-neuroprotective-activity-of-the-ketogenic-diet-in-the-eye
#12
Tomasz Żarnowski, Maria Tulidowicz-Bielak, Iwona Żarnowska, Krystyna Mitosek-Szewczyk, Artur Wnorowski, Krzysztof Jóźwiak, Maciej Gasior, Waldemar A Turski
There is growing evidence of the involvement of the kynurenine metabolic pathway and the enhancement of kynurenic acid (KYNA) production in the neuroprotective effects of the ketogenic diet (KD). KD and ketone bodies (KBs) that are elevated during exposure to the KD each have a neuroprotective effect on retinal ganglion cells in a rat model of N-methyl-D-aspartate (NMDA)-induced neuronal damage. Chronic exposure to KD also increases KYNA concentrations in discrete rat brain structures. A non-selective glutamate receptor agonist, glutamate, also decreases the production of KYNA in bovine retinal slices; this effect is attenuated by acetoacetate and β-hydroxybutyrate, two of three KBs overproduced during KD...
May 9, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28483393/activation-of-5-ht7-receptors-reverses-nmda-r-dependent-ltd-by-activating-pka-in-medial-vestibular-neurons
#13
Yan-Hai Li, Lei Han, Kenneth Lap-Kei Wu, Ying-Shing Chan
The medial vestibular nucleus (MVN) is a major output station for neurons that project to the vestibulo-spinal pathway. MVN neurons show capacity for long-term depression (LTD) during the juvenile period. We investigated LTD of MVN neurons using whole-cell patch-clamp recordings. High frequency stimulation (HFS) robustly induced LTD in 90% of type B neurons in the MVN, while only 10% of type A neurons were responsive, indicating that type B neurons are the major contributors to LTD in the MVN. The neuromodulator serotonin (5-HT) is known to modulate LTD in neural circuits of the cerebral cortex and the hippocampus...
May 5, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28479102/septal-cholinergic-neuromodulation-tunes-the-astrocyte-dependent-gating-of-hippocampal-nmda-receptors-to-wakefulness
#14
Thomas Papouin, Jaclyn M Dunphy, Michaela Tolman, Kelly T Dineley, Philip G Haydon
The activation of the N-methyl D-aspartate receptor (NMDAR) is controlled by a glutamate-binding site and a distinct, independently regulated, co-agonist-binding site. In most brain regions, the NMDAR co-agonist is the astrocyte-derived gliotransmitter D-serine. We found that D-serine levels oscillate in mouse hippocampus as a function of wakefulness, in vitro and in vivo. This causes a full saturation of the NMDAR co-agonist site in the dark (active) phase that dissipates to sub-saturating levels during the light (sleep) phase, and influences learning performance throughout the day...
May 17, 2017: Neuron
https://www.readbyqxmd.com/read/28475556/high-concentrations-of-tranexamic-acid-inhibit-ionotropic-glutamate-receptors
#15
Irene Lecker, Dian-Shi Wang, Kirusanthy Kaneshwaran, C David Mazer, Beverley A Orser
BACKGROUND: The antifibrinolytic drug tranexamic acid is structurally similar to the amino acid glycine and may cause seizures and myoclonus by acting as a competitive antagonist of glycine receptors. Glycine is an obligatory co-agonist of the N-methyl-D-aspartate (NMDA) subtype of glutamate receptors. Thus, it is plausible that tranexamic acid inhibits NMDA receptors by acting as a competitive antagonist at the glycine binding site. The aim of this study was to determine whether tranexamic acid inhibits NMDA receptors, as well as α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid and kainate subtypes of ionotropic glutamate receptors...
May 5, 2017: Anesthesiology
https://www.readbyqxmd.com/read/28468946/novel-mode-of-antagonist-binding-in-nmda-receptors-revealed-by-the-crystal-structure-of-the-glun1-glun2a-ligand-binding-domain-complexed-to-nvp-aam077
#16
Annabel Romero-Hernandez, Hiro Furukawa
Competitive antagonists against N-methyl-D-aspartate (NMDA) receptors have played critical roles throughout the history of neuropharmacology and basic neuroscience. There are currently numerous NMDA receptor antagonists containing a variety of chemical groups. Among those compounds, a GluN2-specific antagonist, (R)-[(S)-1-(4-bromo-phenyl)-ethylamino]-(2,3-dioxo-1,2,3,4-tetrahydroquinoxalin-5-yl)-methyl]-phosphonic acid (NVP-AAM077), contains a unique combination of a dioxoquinoxalinyl ring, a bromophenyl group, and a phosphono group...
May 3, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/28463241/serum-kynurenic-acid-is-reduced-in-affective-psychosis
#17
B E Wurfel, W C Drevets, S A Bliss, J R McMillin, H Suzuki, B N Ford, H M Morris, T K Teague, R Dantzer, J B Savitz
A subgroup of individuals with mood and psychotic disorders shows evidence of inflammation that leads to activation of the kynurenine pathway and the increased production of neuroactive kynurenine metabolites. Depression is hypothesized to be causally associated with an imbalance in the kynurenine pathway, with an increased metabolism down the 3-hydroxykynurenine (3HK) branch of the pathway leading to increased levels of the neurotoxic metabolite, quinolinic acid (QA), which is a putative N-methyl-d-aspartate (NMDA) receptor agonist...
May 2, 2017: Translational Psychiatry
https://www.readbyqxmd.com/read/28461248/simultaneous-triple-therapy-for-the-treatment-of-status-epilepticus
#18
Jerome Niquet, Roger Baldwin, Keith Norman, Lucie Suchomelova, Lucille Lumley, Claude G Wasterlain
Early maladaptive internalization of synaptic GABAA receptors (GABAAR) and externalization of NMDA receptors (NMDAR) may explain the time-dependent loss of potency of standard anti-epileptic drugs (AED) in refractory status epilepticus (SE). We hypothesized that correcting the effects of changes in GABAAR and NMDAR would terminate SE, even when treatment is delayed 40 minutes. SE was induced in adult Sprague-Dawley rats with a high dose of lithium and pilocarpine. The GABAAR agonist midazolam, the NMDAR antagonist ketamine and the AED valproate were injected 40 min after SE onset in combination or as monotherapy...
April 29, 2017: Neurobiology of Disease
https://www.readbyqxmd.com/read/28455101/sip-1-mutations-cause-disturbances-in-the-activity-of-nmda-and-ampa-but-not-kainate-receptors-of-neurons-in-the-cerebral-cortex
#19
Maria V Turovskaya, Alexei A Babaev, Valery P Zinchenko, Ekaterina A Epifanova, Ekaterina V Borisova, Victor S Tarabykin, Egor A Turovsky
Smad-interacting protein-1 (Sip1) [Zinc finger homeobox (Zfhx1b), Zeb2] is a transcription factor implicated in the genesis of Mowat-Wilson syndrome (MWS) in humans. MWS is a rare genetic autosomal dominant disease caused by a mutation in the Sip1 gene (aka Zeb2 or Zfhx1b) mapped to 2q22.3 locus. MWS affects 1 in every 50-100 newborns worldwide. It is characterized by mental retardation, small stature, typical facial abnormalities as well as disturbances in the development of the cardio-vascular and renal systems as well as some other organs...
April 25, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/28444173/tac1-signaling-is-required-for-sexual-maturation-and-responsiveness-of-gnrh-neurons-to-kisspeptin-in-the-male-mouse
#20
Caroline A Maguire, Yong Bhum Song, Min Wu, Silvia León, Rona S Carroll, Meenakshi Alreja, Ursula B Kaiser, Víctor M Navarro
The tachykinins substance P (SP) and neurokinin A (NKA) (Tac1) have emerged as novel regulators of kisspeptin/GnRH release. Recently, we documented that SP modulates reproductive function in the female mouse. Here, we extended this characterization to the male mouse. Tac1-/- male mice showed delayed puberty onset. They also presented significantly decreased expression levels of Pdyn (dynorphin) and Nos1 (nitric oxide synthase) in the mediobasal hypothalamus and elevated Gnrh1 levels. Unexpectedly, the response of Tac1-/- mice to central kisspeptin or senktide (neurokinin B receptor -NK3R- agonist) administration was significantly decreased compared with controls, despite the preserved ability of GnRH neurons to stimulate LH release as demonstrated by central NMDA administration, suggesting a deficit at the GnRH neuron level...
April 21, 2017: Endocrinology
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