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https://www.readbyqxmd.com/read/28533163/grin2b-gain-of-function-mutations-are-sensitive-to-radiprodil-a-negative-allosteric-modulator-of-glun2b-containing-nmda-receptors
#1
Brice Mullier, Christian Wolff, Zara Amanda Sands, Philippe Ghisdal, Pierandrea Muglia, Rafal Marian Kaminski, Véronique Marie André
De novo gain of function mutations in GRIN2B encoding the GluN2B subunit of the N-methyl-D-aspartate (NMDA) receptor have been linked with epileptic encephalopathies, including infantile spasms. We investigated the effects of radiprodil, a selective GluN2B negative allosteric modulator and other non-selective NMDA receptor inhibitors on glutamate currents mediated by NMDA receptors containing mutated GluN2B subunits. The experiments were performed in Xenopus oocytes co-injected with the following human mRNAs: GRIN1/GRIN2B, GRIN1/GRIN2B-R540H, GRIN1/GRIN2B-N615I and GRIN1/GRIN2B-V618G...
May 19, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28526161/an-update-on-nonopioids-intravenous-or-oral-analgesics-for-perioperative-pain-management
#2
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/28525360/role-of-sigma-1-receptor-in-high-fat-diet-induced-peripheral-neuropathy
#3
Tieying Song, Jianhui Zhao, Xiaojing Ma, Zaiwang Zhang, Bo Jiang, Yunliang Yang
The neurobiological mechanisms of obesity-induced peripheral neuropathy are poorly understood. We evaluated the role of Sigma-1 receptor (Sig-1R) and NMDA receptor (NMDARs) in the spinal cord in peripheral neuropathy using an animal model of high fat diet-induced diabetes. We examined the expression of Sig-1R and NMDAR subunits GluN2A and GluN2B along with postsynaptic density protein 95 (PSD-95) in the spinal cord after 24- week HFD treatment in both wild-type and Sig-1R-/- mice. Finally, we examined the effects of repeated intrathecal administrations of selective Sig-1R antagonists BD1047 in HFD-fed wild-type mice on peripheral neuropathy...
May 19, 2017: Biological Chemistry
https://www.readbyqxmd.com/read/28522210/novel-trigeminal-slice-preparation-method-for-studying-mechanisms-of-nociception-transmission
#4
Mikiko Hirahara, Naoshi Fujiwara, Kenji Seo
BACKGROUND: The trigeminal subnucleus caudalis (Vc) plays a critical role in transmission and modulation of nociceptive afferent inputs, and exhibits a similar layer construction to the spinal dorsal horn. However, afferent inputs enter the brainstem and project to a separately located nucleus. It has previously been difficult to record responses of the Vc to afferent fiber activation in a brainstem slice preparation. The aim of the present study was to establish a novel brainstem slice preparation method to study trigeminal nociceptive transmission mechanisms...
May 15, 2017: Journal of Neuroscience Methods
https://www.readbyqxmd.com/read/28511693/antagonistic-action-on-nmda-glun2b-mediated-currents-of-two-peptides-that-were-conantokin-g-structure-based-designed
#5
Edwin A Reyes-Guzman, Nohora Vega-Castro, Edgar A Reyes-Montaño, Esperanza Recio-Pinto
BACKGROUND: The GluN2B subunit of the N-methyl-D-aspartate receptor (NMDAr) modulates many physiological processes including learning, memory, and pain. Excessive increase in NMDAr/GluN2B activity has been associated with various disorders such neuropathic pain and neuronal death following hypoxia. Thus there is an interest in identifying NMDAr antagonists that interact specifically with the GluN2B subunit. Recently based on structural analysis between the GluN2B subunit and conantokin-G, a toxin that interacts selectively with the GluN2B subunit, we designed various peptides that are predicted to act as NMDAr antagonists by interacting with the GluN2B subunit...
May 16, 2017: BMC Neuroscience
https://www.readbyqxmd.com/read/28507036/medial-prefrontal-cortex-and-dorsomedial-striatum-are-necessary-for-the-trial-unique-delayed-nonmatching-to-location-tunl-task-in-rats-role-of-nmda-receptors
#6
Don A Davies, Jessica L Hurtubise, Quentin Greba, John G Howland
The trial-unique, delayed nonmatching-to-location (TUNL) task is a recently developed behavioral task that measures spatial working memory and a form of pattern separation in touchscreen-equipped operant conditioning chambers. Limited information exists regarding the neurotransmitters and neural substrates involved in the task. The present experiments tested the effects of systemic and intracranial injections of NMDA receptor antagonists on the TUNL task. After training, male Long Evans rats systemically injected with the competitive NMDA receptor antagonist CPP (10 mg/kg) had impaired accuracy regardless of the degree of stimuli separation or length of delay between the sample and test phases...
June 2017: Learning & Memory
https://www.readbyqxmd.com/read/28507031/memory-consolidation-within-the-central-amygdala-is-not-necessary-for-modulation-of-cerebellar-learning
#7
Adam B Steinmetz, Ka H Ng, John H Freeman
Amygdala lesions impair, but do not prevent, acquisition of cerebellum-dependent eyeblink conditioning suggesting that the amygdala modulates cerebellar learning. Two-factor theories of eyeblink conditioning posit that a fast-developing memory within the amygdala facilitates slower-developing memory within the cerebellum. The current study tested this hypothesis by impairing memory consolidation within the amygdala with inhibition of protein synthesis, transcription, and NMDA receptors in rats. Rats given infusions of anisomycin or DRB into the central amygdala (CeA) immediately after each eyeblink conditioning session were severely impaired in contextual and cued fear conditioning, but were completely unimpaired in eyeblink conditioning...
June 2017: Learning & Memory
https://www.readbyqxmd.com/read/28506554/selective-dopamine-receptor-4-activation-mediates-the-hippocampal-neuronal-calcium-response-via-ip3-and-ryanodine-receptors
#8
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/28495142/n-methyl-d-aspartate-receptor-mediated-calcium-overload-and-endoplasmic-reticulum-stress-are-involved-in-interleukin-1beta-induced-neuronal-apoptosis-in-rat-hippocampus
#9
Yilong Dong, Allan V Kalueff, Cai Song
Increased levels of interleukin (IL)-1β and its gene expression are implicated in the etiology of Alzheimer's disease (AD). IL-1β activates microglia and stimulates glutamatergic N-methyl-d-aspartate receptor NMDA receptor expression, thereby disturbing intracellular Ca(2+) homeostasis. Ca(2+) disequilibrium, in turn, may trigger endoplasmic reticulum (ER) stress, contributing to overall excitotoxicity and neuronal death that evoke AD. However, it is unclear whether IL-1β-induced neuronal apoptosis is mediated by the glutamatergic system, ER stress and/or Ca(2+) dysfunction...
June 15, 2017: Journal of Neuroimmunology
https://www.readbyqxmd.com/read/28491480/new-treatment-strategies-of-depression-based-on-mechanisms-related-to-neuroplasticity
#10
REVIEW
Yu-Jhen Huang, Hsien-Yuan Lane, Chieh-Hsin Lin
Major depressive disorder is a severe and complex mental disorder. Impaired neurotransmission and disrupted signalling pathways may influence neuroplasticity, which is involved in the brain dysfunction in depression. Traditional neurobiological theories of depression, such as monoamine hypothesis, cannot fully explain the whole picture of depressive disorders. In this review, we discussed new treatment directions of depression, including modulation of glutamatergic system and noninvasive brain stimulation. Dysfunction of glutamatergic neurotransmission plays an important role in the pathophysiology of depression...
2017: Neural Plasticity
https://www.readbyqxmd.com/read/28483393/activation-of-5-ht7-receptors-reverses-nmda-r-dependent-ltd-by-activating-pka-in-medial-vestibular-neurons
#11
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/28479266/involvement-of-hippocampal-nmda-receptors-in-encoding-and-consolidation-but-not-retrieval-processes-of-spontaneous-object-location-memory-in-rats
#12
Kazuo Yamada, Misaki Arai, Toshiko Suenaga, Yukio Ichitani
The hippocampus is thought to be involved in object location recognition memory, yet the contribution of hippocampal NMDA receptors to the memory processes, such as encoding, retention and retrieval, is unknown. First, we confirmed that hippocampal infusion of a competitive NMDA receptor antagonist, AP5 (2-amino-5-phosphonopentanoic acid, 20-40nmol), impaired performance of spontaneous object location recognition test but not that of novel object recognition test in Wistar rats. Next, the effects of hippocampal AP5 treatment on each process of object location recognition memory were examined with three different injection times using a 120min delay-interposed test: 15min before the sample phase (Time I), immediately after the sample phase (Time II), and 15min before the test phase (Time III)...
May 4, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28475556/high-concentrations-of-tranexamic-acid-inhibit-ionotropic-glutamate-receptors
#13
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/28473645/dopamine-receptors-differentially-control-binge-alcohol-drinking-mediated-synaptic-plasticity-of-the-core-nucleus-accumbens-direct-and-indirect-pathways
#14
Xincai Ji, Sucharita Saha, Jenya Kolpakova, Melissa Guildford, Andrew R Tapper, Gilles E Martin
Binge alcohol drinking, a behavior characterized by rapid repeated alcohol intakes, is most prevalent in young adults and a risk factor for excessive alcohol consumption and alcohol dependence. Although alteration of synaptic plasticity is thought to contribute to this behavior, there is currently little evidence that this is the case. We used drinking-in-the-dark (DID) as a model of binge alcohol drinking to assess its effects on spike-timing-dependent plasticity (STDP) in medium spiny neurons (MSNs) of the core nucleus accumbens (NAc) by combining patch clamp recordings with calcium imaging and optogenetics...
May 4, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28472639/post-injury-administration-of-a-combination-of-memantine-and-17%C3%AE-estradiol-is-protective-in-a-rat-model-of-traumatic-brain-injury
#15
Nicole L Day, Matthew S Carle, Candace L Floyd
Traumatic brain injury (TBI) often leads to substantial adverse cognitive and health outcomes, including permanent disability and death. Preventing these outcomes requires attenuation of the secondary biochemical damage that follows the initial biomechanical insult, but a clinically proven pharmacotherapeutic capable of such has not been identified. In fact, the heterogeneous nature of TBI and the complexity of secondary injury cascades suggest a polytherapeutic approach that targets multiple pathways might be necessary...
May 1, 2017: Neurochemistry International
https://www.readbyqxmd.com/read/28468999/ketamine-induced-converged-synchronous-gamma-oscillations-in-the-cortico-basal-ganglia-network-of-non-human-primates
#16
Maya Slovik, Boris Rosin, Shay Moshel, Rea Mitelman, Eitan Schechtman, Renana Eitan, Aeyal Raz, Hagai Bergman
NMDA (N-methyl-D-aspartate) antagonists are widely used in anesthesia, pain management, schizophrenia animal model studies and recently as potential antidepressants. However the mechanisms underlying their anesthetic, psychotic, cognitive and emotional effects are still elusive. The basal-ganglia (BG) integrate input from different cortical domains through its dopamine modulated connections, to achieve optimal behavior control. NMDA antagonists have been shown to induce gamma oscillations in human EEG recordings and in rodents cortical and BG networks...
May 3, 2017: Journal of Neurophysiology
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
#17
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/28466069/early-social-isolation-stress-and-perinatal-nmda-receptor-antagonist-treatment-induce-changes-in-the-structure-and-neurochemistry-of-inhibitory-neurons-of-the-adult-amygdala-and-prefrontal-cortex
#18
Esther Castillo-Gómez, Marta Pérez-Rando, María Bellés, Javier Gilabert-Juan, José Vicente Llorens, Héctor Carceller, Clara Bueno-Fernández, Clara García-Mompó, Beatriz Ripoll-Martínez, Yasmina Curto, Noelia Sebastiá-Ortega, María Dolores Moltó, Julio Sanjuan, Juan Nacher
The exposure to aversive experiences during early life influences brain development and leads to altered behavior. Moreover, the combination of these experiences with subtle alterations in neurodevelopment may contribute to the emergence of psychiatric disorders, such as schizophrenia. Recent hypotheses suggest that imbalances between excitatory and inhibitory (E/I) neurotransmission, especially in the prefrontal cortex and the amygdala, may underlie their etiopathology. In order to understand better the neurobiological bases of these alterations, we studied the impact of altered neurodevelopment and chronic early-life stress on these two brain regions...
March 2017: ENeuro
https://www.readbyqxmd.com/read/28463241/serum-kynurenic-acid-is-reduced-in-affective-psychosis
#19
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/28462695/differential-mechanisms-underlying-antidepressant-responses-of-ketamine-and-imipramine
#20
Zhisheng Wei, Ke Zhang, Qinji Zhou, Mingfa Huang, Ting Xu, Jianyang Dong, Yu Zheng, Xiang Cai
Ketamine, a noncompetitive NMDA receptor antagonist, exhibits a rapid antidepressant effect, but the underlying mechanism remains obscure. Ketamine and imipramine, a tricyclic antidepressant, share the same targets on AMPA receptors and CREB, whereas ketamine exerts fast-actioning responses compared to traditional antidepressants' slow onset. To figure out why there is a significant discrepancy of their antidepressant efficiency is important for elucidating the mechanisms underlying ketamine's antidepressant effects as well as discovering new rapid antidepressants...
April 28, 2017: CNS & Neurological Disorders Drug Targets
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