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Nmda receptor antagonist

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https://www.readbyqxmd.com/read/29353374/bdnf-activates-mtor-to-upregulate-nr2b-expression-in-the-rostral-anterior-cingulate-cortex-required-for-inflammatory-pain-related-aversion-in-rats
#1
Yuangui Zhang, Fanceng Ji, Gongming Wang, Dong He, Le Yang, Mengyuan Zhang
The mechanistic target of rapamycin (mTOR) has been demonstrated to mediate pain-related aversion induced by formalin in the rostral anterior cingulate cortex (rACC). However, it remains unclear the signaling pathways and regulatory proteins involved. In the rACC, brain-derived neurotrophic factor (BDNF), an activity-dependent neuromodulator, has been shown to play a role in the development and persistence of chronic pain. In this study, we used a rat formalin-induced inflammatory pain model to demonstrate BDNF up-regulation in the rACC...
January 20, 2018: Neurochemical Research
https://www.readbyqxmd.com/read/29339324/oscillatory-synchronous-inhibition-in-the-basolateral-amygdala-and-its-primary-dependence-on-nr2a-containing-nmda-receptors
#2
Vassiliki Aroniadou-Anderjaska, Volodymyr I Pidoplichko, Taiza H Figueiredo, Maria F M Braga
Synchronous, rhythmic firing of GABAergic interneurons is a fundamental mechanism underlying the generation of brain oscillations, and evidence suggests that NMDA receptors (NMDARs) play a key role in oscillatory activity by regulating the activity of interneurons. Consistent with this, derangement of brain rhythms in certain neuropsychiatric disorders, notably schizophrenia and autism, is associated with NMDAR hypofunction and loss of inhibitory interneurons. In the basolateral amygdala (BLA)-dysfunction of which is involved in a host of neuropsychiatric diseases-, principal neurons display spontaneous, rhythmic "bursts" of inhibitory activity, which could potentially be involved in the orchestration of oscillations in the BLA network; here, we investigated the role of NMDARs in these inhibitory oscillations...
January 12, 2018: Neuroscience
https://www.readbyqxmd.com/read/29339173/neuroprotective-effects-of-topiramate-and-memantine-in-combination-with-hypothermia-in-hypoxic-ischemic-brain-injury-in-vitro-and-in-vivo
#3
Elisa Landucci, Luca Filippi, Elisabetta Gerace, Serena Catarzi, Renzo Guerrini, Domenico E Pellegrini-Giampietro
Hypoxic-ischemic encephalopathy (HIE) is a major cause of perinatal mortality and subsequent severe neurological sequelae. Mild hypothermia is a standard therapy for HIE, but is used only in selected Reference Centers and in neonates >1800 g. Since neuronal death following HIE occurs by a cascade of events triggered by activation of glutamate receptors, we used in vitro and in vivo models of HIE to examine whether the AMPA/kainate receptor antagonist topiramate and the NMDA receptor antagonist memantine could exert neuroprotective effects, alone or in combination with hypothermia...
January 12, 2018: Neuroscience Letters
https://www.readbyqxmd.com/read/29339170/sub-anesthetic-doses-of-ketamine-attenuate-nicotine-self-administration-in-rats
#4
Amir H Rezvani, Yousef Tizabi, Susan Slade, Bruk Getachew, Edward D Levin
Smoking cessation strategies are of prime medical importance. Despite availability of various pharmacological agents in combating addiction to nicotine, more effective medications are needed. Based on recent findings, the glutamatergic system in the brain may provide novel targets. Here, we evaluated the effects of acute administration of sub-anesthetic doses of ketamine, an NMDA receptor antagonist, in both male and female Sprague-Dawley rats trained to self-administer nicotine. Animals were injected subcutaneously with 5, 7...
January 12, 2018: Neuroscience Letters
https://www.readbyqxmd.com/read/29335819/nmda-receptor-glun2-subtypes-control-epileptiform-events-in-the-hippocampus
#5
Pradeep Punnakkal, Deity Dominic
NMDA receptors (NMDARs) play a key role in synaptic plasticity and excitotoxicity. Subtype-specific role of NMDAR in neural disorders is an emerging area. Recent studies have revealed that mutations in NMDARs are a cause for epilepsy. Hippocampus is a known focal point for epilepsy. In hippocampus, expression of the NMDAR subtypes GluN1/GluN2A and GluN1/GluN2B is temporally regulated. However, the pharmacological significance of these subtypes is not well understood in epileptic context/models. To investigate this, epilepsy was induced in hippocampal slices by the application of artificial cerebrospinal fluid that contained high potassium but no magnesium...
January 15, 2018: Neuromolecular Medicine
https://www.readbyqxmd.com/read/29330003/effects-of-5-ht5a-receptor-blockade-on-amnesia-or-forgetting
#6
L Aparicio-Nava, L A Márquez-García, A Meneses
Previously the effects (0.01-3.0 mg/kg) of post-training SB-699551 (a 5-HT5A receptor antagonist) were reported in the associative learning task of autoshaping, showing that SB-699551 (0.1 mg/kg) decreased lever-press conditioned responses (CR) during short-term (STM; 1.5-h) or (3.0 mg/kg) long-term memory (LTM; 24-h); relative to the vehicle animals. Moreover, as pro-cognitive efficacy of SB-699551 was reported in the ketamine-model of schizophrenia. Hence, firstly aiming improving performance (conditioned response, CR), in this work autoshaping lever-press vs...
January 9, 2018: Behavioural Brain Research
https://www.readbyqxmd.com/read/29329983/attenuation-of-noise-induced-hyperactivity-in-the-dorsal-cochlear-nucleus-by-pre-treatment-with-mk-801
#7
M W Criddle, D A Godfrey, J A Kaltenbach
It has previously been hypothesized that hyperactivity of central auditory neurons following exposure to intense noise is a consequence of synaptic alterations. Recent studies suggest the involvement of NMDA receptors in the induction of this hyperactive state. NMDA receptors can mediate long term changes in the excitability of neurons through their involvement in excitotoxic injury and long term potentiation and depression. In this study, we examined the effect of administering an NMDA receptor blocker on the induction of hyperactivity in the dorsal cochlear nucleus (DCN) following intense sound exposure...
January 9, 2018: Brain Research
https://www.readbyqxmd.com/read/29323417/loss-of-ethanol-inhibition-of-nmdar-mediated-currents-and-plasticity-of-cerebellar-synapses-in-mice-expressing-the-glun1-f639a-subunit
#8
Paula A Zamudio-Bulcock, Gregg E Homanics, John J Woodward
BACKGROUND: Glutamatergic N-methyl-D-aspartate receptors (NMDARs) are well known for their sensitivity to ethanol inhibition. However, the specific manner in which ethanol inhibits channel activity and how such inhibition affects neurotransmission, and ultimately behavior, remain unclear. Replacement of phenylalanine 639 with alanine (F639A) in the GluN1 subunit reduces ethanol inhibition of recombinant NMDA receptors. Mice expressing this subunit show reduced ethanol-induced anxiolysis, blunted locomotor stimulation following low dose ethanol administration and faster recovery of motor function after moderate doses of ethanol suggesting that cerebellar dysfunction may contribute to some of these behaviors...
January 11, 2018: Alcoholism, Clinical and Experimental Research
https://www.readbyqxmd.com/read/29318854/-effect-of-electroacupuncture-on-intracellular-calcium-ion-concentration-and-expression-of-calcium-calmodulin-dependent-protein-kinase-%C3%A2-in-lumbar-spinal-cord-in-rats-with-neuropathic-pain
#9
Xin-Tian Wu, Wei Liang, Li-Ping Yan, Ling-Ling Wang, Cheng Ma
OBJECTIVE: To observe the changes of intracellular calcium ([Ca2+]i) concentration and expression of calcium/calmodulin dependent protein kinaseⅡ (CaMKⅡ) in spinal dorsal horn neurons of spared nerve injury (SNI) rats, so as to explore its mechanisms underlying improvement of neuropathic pain. METHODS: One hundred and ten SD rats were randomly divided into 5 groups: sham control, model, EA, AP-5 and L-NAME groups. The sham group underwent only a simple separation of the sciatic nerve but without ligation and abscission...
December 25, 2017: Zhen Ci Yan Jiu, Acupuncture Research
https://www.readbyqxmd.com/read/29315577/bidirectional-variation-in-glutamate-efflux-in-the-medial-prefrontal-cortex-induced-by-selective-positive-and-negative-allosteric-mglur5-modulators
#10
Sarah N Isherwood, Trevor W Robbins, Jeffrey W Dalley, Anton Pekcec
Dysregulation of prefrontal cortical glutamatergic signalling via NMDA receptor hypofunction has been implicated in cognitive dysfunction and impaired inhibitory control in such neuropsychiatric disorders as schizophrenia, attention deficit hyperactivity disorder and drug addiction. Although NMDA receptors functionally interact with metabotropic glutamate receptor 5 (mGluR5), the consequence of this interaction for glutamate release in the prefrontal cortex (PFC) is unknown. We therefore investigated the effects of positive and negative allosteric mGluR5 modulation on changes in extracellular glutamate efflux in the medial PFC (mPFC) induced by systemic administration of the non-competitive NMDA receptor antagonist dizocilpine (or MK801) in rats...
January 6, 2018: Journal of Neurochemistry
https://www.readbyqxmd.com/read/29305627/antagonism-at-the-nr2b-subunit-of-nmda-receptors-induces-increased-connectivity-of-the-prefrontal-and-subcortical-regions-regulating-reward-behavior
#11
Natalia Gass, Robert Becker, Markus Sack, Adam J Schwarz, Jonathan Reinwald, Alejandro Cosa-Linan, Lei Zheng, Christian Clemm von Hohenberg, Dragos Inta, Andreas Meyer-Lindenberg, Wolfgang Weber-Fahr, Peter Gass, Alexander Sartorius
RATIONALE: Evidence indicates that ketamine's rapid antidepressant efficacy likely results from its antagonism of NR2B-subunit-containing NMDA receptors (NMDAR). Since ketamine equally blocks NR2A- and NR2B-containing NMDAR, and has affinity to other receptors, NR2B-selective drugs might have improved therapeutic efficiency and side effect profile. OBJECTIVES: We aimed to compare the effects of (S)-ketamine and two different types of NR2B-selective antagonists on functional brain networks in rats, in order to find common circuits, where their effects intersect, and that might explain their antidepressant action...
January 5, 2018: Psychopharmacology
https://www.readbyqxmd.com/read/29302750/decreased-plasma-agmatine-levels-in-autistic-subjects
#12
Erman Esnafoglu, İlhan İrende
Agmatine is a polyamine endogenously synthesized from arginine and is considered to be a new neurotransmitter. Agmatine has been implicated in the pathophysiology of several diseases such as anxiety disorder, depression, and schizophrenia. Agmatine also possesses anticonvulsant, neuroprotective, antiapoptotic, antioxidant, anxiolytic, and antidepressant effects. Furthermore, agmatine inhibits the nitric oxide synthase enzyme and exerts antagonist effects on NMDA, alpha-2, and imidazoline receptors. Considering these characteristics, the present study investigated whether agmatine plays a role in the pathogenesis of autistic spectrum disorders (ASDs)...
January 4, 2018: Journal of Neural Transmission
https://www.readbyqxmd.com/read/29289890/hydroxymethyl-bioisosteres-of-phenolic-glun2b-selective-nmda-receptor-antagonists-design-synthesis-and-pharmacological-evaluation
#13
Louisa Temme, Bastian Frehland, Dirk Schepmann, Dina Robaa, Wolfgang Sippl, Bernhard Wünsch
Antagonists addressing selectively NMDA receptors containing the GluN2B subunit are of particular interest for the treatment of various neurological disorders including neurodegenerative diseases. With the aim to bioisosterically replace the metabolically labile phenol of 7-amino-6,7,8,9-tetrahydro-5H-benzo[7]annulen-2-ols, several analogs were docked into the ifenprodil binding site leading to the hydroxymethyl derivatives 4 as promising candidates. They display the same binding pose as Ro 25-6981 and the same H-bond interactions with Gln110 and Glu236 within the GluN2B subunit...
December 18, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29288725/both-ketamine-and-nbqx-attenuate-alcohol-drinking-in-male-wistar-rats
#14
Jana Ruda-Kucerova, Zuzana Babinska, Matej Luptak, Bruk Getachew, Yousef Tizabi
The devastating consequences of alcohol-use disorder (AUD) on the individual and the society are well established. Current treatments of AUD encompass various strategies, all of which have only modest effectiveness. Hence, there is a critical need to develop more efficacious therapies. Recently, specific glutamatergic receptors have been identified as potential novel targets for intervention in AUD. Thus, the current study was designed to evaluate the effects of acute administration of sub-anesthetic doses of ketamine, an NMDA receptor antagonist, as well as NBQX, an AMPA/kainate receptor antagonist on alcohol intake and its possible behavioural consequences...
December 27, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/29277306/design-synthesis-and-evaluation-of-polyamine-memantine-hybrids-as-nmda-channel-blockers
#15
Takuya Kumamoto, Marie Nakajima, Reina Uga, Naoko Ihayazak, Haruna Kashihara, Kazuaki Katakawa, Tsutomu Ishikawa, Ryotaro Saiki, Kazuhiro Nishimura, Kazuei Igarashi
N-Methyl-d-aspartate (NMDA) receptors have been implicated in learning and memory, and may also play a central role in various conditions leading to neuronal degradation. NMDA receptor antagonists could therefore be of therapeutic benefit for a number of neurological disorders. We have designed hybrid compounds of polyamines and memantine, both of which function as NMDA channel blockers. The triamine derivative with a guanidine moiety showed more potent antagonistic activity than memantine.
December 16, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29276474/experimental-gene-therapy-with-serine-histogranin-and-endomorphin-1-for-the-treatment-of-chronic-neuropathic-pain
#16
Stanislava Jergova, Catherine E Gordon, Shyam Gajavelli, Jacqueline Sagen
The insufficient pain relief provided by current pharmacotherapy for chronic neuropathic pain is a serious medical problem. The enhanced glutamate signaling via NMDA receptors appears to be one of the key events in the development of chronic pain. Although effective, clinical use of systemic NMDA antagonists is limited by adverse effects such as hallucinations and motor dysfunction. Opioids are also potent analgesics but their chronic use is accompanied by tolerance and risk of addiction. However, combination of NMDA antagonists and opioids seems to provide a stable pain relieve at subthreshold doses of both substances, eliminating development of side effects...
2017: Frontiers in Molecular Neuroscience
https://www.readbyqxmd.com/read/29273965/effects-of-%C3%AE-7-nicotinic-receptor-activation-on-cell-survival-in-rat-organotypic-hippocampal-slice-cultures
#17
Denise F Happ, R Andrew Tasker
Glutamatergic signaling via N-methyl-D-aspartate receptors (NMDARs) is important for physiological functioning, but can also induce cell death via excitotoxic mechanisms in many neuropathological diseases, such as stroke. Altering the cellular response to excitotoxic insults by modulating the downstream effects of NMDAR activation represents a promising therapeutic approach. For example, α7 nicotinic acetylcholine receptors (α7 nAChRs) signaling has been shown to be able to change NMDA-induced neurotoxicity in some models...
December 22, 2017: Neurotoxicity Research
https://www.readbyqxmd.com/read/29262336/hippocampus-and-entorhinal-cortex-recruit-cholinergic-and-nmda-receptors-separately-to-generate-hippocampal-theta-oscillations
#18
Zhenglin Gu, Georgia M Alexander, Serena M Dudek, Jerrel L Yakel
Although much progress has been made in understanding type II theta rhythm generation under urethane anesthesia, less is known about the mechanisms underlying type I theta generation during active exploration. To better understand the contributions of cholinergic and NMDA receptor activation to type I theta generation, we recorded hippocampal theta oscillations from freely moving mice with local infusion of cholinergic or NMDA receptor antagonists to either the hippocampus or the entorhinal cortex (EC). We found that cholinergic receptors in the hippocampus, but not the EC, and NMDA receptors in the EC, but not the hippocampus, are critical for open-field theta generation and Y-maze performance...
December 19, 2017: Cell Reports
https://www.readbyqxmd.com/read/29250595/comparison-of-nmda-and-ampa-channel-expression-and-function-between-embryonic-and-adult-neurons-utilizing-microelectrode-array-systems
#19
Darin Edwards, Frank Sommerhage, Bonnie Berry, Hanna Nummer, Martina Raquet, Brad Clymer, Maria Stancescu, James J Hickman
Microelectrode arrays (MEAs) are innovative tools used to perform electrophysiological experiments for the study of electrical activity and connectivity in populations of neurons from dissociated cultures. Reliance upon neurons derived from embryonic tissue is a common limitation of neuronal/MEA hybrid systems and perhaps of neuroscience research in general, and the use of adult neurons could model fully functional in vivo parameters more closely. Spontaneous network activity was concurrently recorded from both embryonic and adult rat neurons cultured on MEAs for up to 10 weeks in vitro to characterize the synaptic connections between cell types...
December 11, 2017: ACS Biomaterials Science & Engineering
https://www.readbyqxmd.com/read/29249806/cortical-high-gamma-network-oscillations-and-connectivity-a-translational-index-for-antipsychotics-to-normalize-aberrant-neurophysiological-activity
#20
A Ahnaou, H Huysmans, T Van de Casteele, W H I M Drinkenburg
Oscillatory activity in the gamma frequency range is a critical mechanism, which integrates neural networks within and across brain structures during cognitive processes. In schizophrenia, abnormalities in high gamma oscillations are ubiquitous and most likely reflect dysfunction in neuronal networks. In conscious rats, disturbed network oscillations associated with positive symptoms and cognitive deficits were modeled in different cortical areas by the dopaminergic agonist (amphetamine) and the N-methyl-D-aspartate (NMDA) receptor antagonists (PCP and MK801)...
December 18, 2017: Translational Psychiatry
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