keyword
MENU ▼
Read by QxMD icon Read
search

NMDA antagonist

keyword
https://www.readbyqxmd.com/read/28222314/systematic-variation-of-the-benzenesulfonamide-part-of-the-glun2a-selective-nmda-receptor-antagonist-tcn-201
#1
Sebastian L Müller, Julian A Schreiber, Dirk Schepmann, Nathalie Strutz-Seebohm, Guiscard Seebohm, Bernhard Wünsch
GluN2A subunit containing N-methyl-d-aspartate receptors (NMDARs) are highly involved in various physiological processes in the central nervous system, but also in some diseases, such as anxiety, depression and schizophrenia. However, the role of GluN2A subunit containing NMDARs in pathological processes is not exactly elucidated. In order to obtain potent and selective inhibitors of GluN2A subunit containing NMDARs, the selective negative allosteric modulator 2 was systematically modified at the benzenesulfonamide part...
February 14, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28221080/blockade-of-glutamatergic-transmission-in-the-primate-basolateral-amygdala-suppresses-active-behavior-without-altering-social-interaction
#2
Patrick A Forcelli, Laurie L Wellman, Ludise Malkova
The amygdala is an integrator of affective processing, and a key component of a network regulating social behavior. While decades of lesion studies in nonhuman primates have shown alterations in social interactions after amygdala damage, acute manipulations of the amygdala in primates have been underexplored. We recently reported (Wellman, Forcelli, Aguilar, & Malkova, 2016) that acute pharmacological inhibition of the basolateral complex of the amygdala (BLA) or the central nucleus of the amygdala increased affiliative social interactions in experimental dyads of macaques; this was achieved through microinjection of a GABA-A receptor agonist...
February 20, 2017: Behavioral Neuroscience
https://www.readbyqxmd.com/read/28218498/optimization-of-bicyclic-lactam-derivatives-as-nmda-receptor-antagonists
#3
Margarida Espadinha, Jorge Dourado, Rocio Lajarin-Cuesta, Clara Herrera-Arozamena, Lidia Gonçalves, Maria Isabel Rodríguez-Franco, Cristobal de Los Rios, Maria M M Santos
N-Methyl-D-aspartate (NMDA) receptors are fundamental for the normal function of the central nerve system, and play an important role in memory and learning. An overactivation of these receptors will lead to neuronal loss associated with major neurological disorders, such as Parkinson's disease, Alzheimer's disease, schizophrenia, and epilepsy. Herein, twenty two novel enantiopure bicyclic lactams were designed, synthesized, and evaluated as NMDA receptor antagonists. Most of the new compounds displayed NMDA receptor antagonism and, the most promising compound showed IC50 value in the same order of magnitude of memantine, a NMDA receptor antagonist used in the clinic for the treatment of Alzheimer's disease...
February 20, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28214516/saturation-of-long-term-potentiation-in-the-dorsal-cochlear-nucleus-and-its-pharmacological-reversal-in-an-experimental-model-of-tinnitus
#4
Thomas Tagoe, Daniel Deeping, Martine Hamann
Animal models have demonstrated that tinnitus is a pathology of dysfunctional excitability in the central auditory system, in particular in the dorsal cochlear nucleus (DCN) of the brainstem. We used a murine model and studied whether acoustic over-exposure leading to hearing loss and tinnitus, affects long-term potentiation (LTP) at DCN multisensory synapses. Whole cell and field potential recordings were used to study the effects on release probability and synaptic plasticity, respectively in brainstem slices...
February 15, 2017: Experimental Neurology
https://www.readbyqxmd.com/read/28204809/ketamine-suppresses-the-substance-p-induced-production-of-il-6-and-il-8-by-human-u373mg-glioblastoma-astrocytoma-cells
#5
Keisuke Yamaguchi, Seiichiro Kumakura, Taisuke Murakami, Akimasa Someya, Eiichi Inada, Isao Nagaoka
The neuropeptide substance P (SP) is an important mediator of neurogenic inflammation within the central and peripheral nervous systems. SP has been shown to induce the expression of pro-inflammatory cytokines implicated in the pathogenesis of several disorders of the human brain via the neurokinin-1 receptor (NK-1R). Ketamine, an intravenous anesthetic agent, functions as a competitive antagonist of the excitatory neurotransmission N-methyl-D‑aspartate (NMDA) receptor, and also antagonizes the NK-1R by interfering with the binding of SP...
March 2017: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/28198211/both-n-methyl-d-aspartate-and-non-n-methyl-d-aspartate-glutamate-receptors-in-the-bed-nucleus-of-the-stria-terminalis-modulate-the-cardiovascular-responses-to-acute-restraint-stress-in-rats
#6
Mariane B Adami, Lucas Barretto-de-Souza, Josiane O Duarte, Jeferson Almeida, Carlos C Crestani
The bed nucleus of the stria terminalis (BNST) is a forebrain structure that has been implicated on cardiovascular responses evoked by emotional stress. However, the local neurochemical mechanisms mediating the BNST control of stress responses are not fully described. In our study we investigated the involvement of glutamatergic neurotransmission within the BNST in cardiovascular changes evoked by acute restraint stress in rats. For this study, we investigated the effects of bilateral microinjections of selective antagonists of either N-methyl-D-aspartate (NMDA) or non-NMDA glutamate receptors into the BNST on the arterial pressure and heart rate increase and the decrease in tail skin temperature induced by acute restraint stress...
February 1, 2017: Journal of Psychopharmacology
https://www.readbyqxmd.com/read/28192174/does-genetic-bdnf-deficiency-in-rats-interact-with-neurotransmitter-control-of-prepulse-inhibition-implications-for-schizophrenia
#7
Maarten van den Buuse, Davina Biel, Kathrin Radscheit
Several studies have suggested a role of BDNF in the development of schizophrenia. For example, post-mortem studies have shown significantly reduced levels of BDNF protein expression in the brain of schizophrenia patients. We investigated the relationship between reduced levels of BDNF in the brain and the regulation of prepulse inhibition (PPI), a behavioral endophenotype of schizophrenia. We used BDNF heterozygous mutant rats which display a 50% decrease of mature BDNF protein levels. Previously, we observed normal baseline PPI and responses to the dopamine D1/D2 receptor agonist, apomorphine, in these rats...
February 10, 2017: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/28178624/agmatine-enhances-the-antidepressant-like-effect-of-lithium-in-mouse-forced-swimming-test-through-nmda-pathway
#8
Gholmreza Mohseni, Sattar Ostadhadi, Muhammad Imran-Khan, Abbas Norouzi-Javidan, Samira Zolfaghari, Nazgol-Sadat Haddadi, Ahmad-Reza Dehpour
Depression is one the world leading global burdens leading to various comorbidities. Lithium as a mainstay in the treatment of depression is still considered gold standard treatment. Similar to lithium another agent agmatine has also central protective role against depression. Since, both agmatine and lithium modulate various effects through interaction with NMDA receptor, therefore, in current study we aimed to investigate the synergistic antidepressant-like effect of agmatine with lithium in mouse force swimming test...
February 5, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28177160/learning-new-sequential-stepping-patterns-requires-striatal-plasticity-during-the-earliest-phase-of-acquisition
#9
Toru Nakamura, Masatoshi Nagata, Takeshi Yagi, Ann M Graybiel, Tetsuo Yamamori, Takashi Kitsukawa
Animals including humans execute motor behavior to reach their goals. For this purpose, they must choose correct strategies according to environmental conditions and shape many parameters of their movements, including their serial order and timing. To investigate the neurobiology underlying such skills, we used a multi-sensor equipped, motor-driven running wheel with adjustable sequences of foothold pegs on which mice ran to obtain water reward. When the peg patterns changed from a familiar pattern to a new pattern, the mice had to learn and implement new locomotor strategies in order to receive reward...
February 8, 2017: European Journal of Neuroscience
https://www.readbyqxmd.com/read/28176276/maintained-ltp-and-memory-are-lost-by-zn-2-influx-into-dentate-granule-cells-but-not-ca-2-influx
#10
Atsushi Takeda, Haruna Tamano, Marie Hisatsune, Taku Murakami, Hiroyuki Nakada, Hiroaki Fujii
The idea that maintained LTP and memory are lost by either increase in intracellular Zn(2+) in dentate granule cells or increase in intracellular Ca(2+) was examined to clarify significance of the increases induced by excess synapse excitation. Both maintained LTP and space memory were impaired by injection of high K(+) into the dentate gyrus, but rescued by co-injection of CaEDTA, which blocked high K(+)-induced increase in intracellular Zn(2+) but not high K(+)-induced increase in intracellular Ca(2+). High K(+)-induced disturbances of LTP and intracellular Zn(2+) are rescued by co-injection of 6-cyano-7-nitroquinoxakine-2,3-dione, an α-amino-3-hydroxy-5-methyl-4-isoxazolepropionate (AMPA) receptor antagonist, but not by co-injection of blockers of NMDA receptors, metabotropic glutamate receptors, and voltage-dependent calcium channels...
February 7, 2017: Molecular Neurobiology
https://www.readbyqxmd.com/read/28167638/effects-of-repeated-ropinirole-treatment-on-phencyclidine-induced-hyperlocomotion-prepulse-inhibition-deficits-and-social-avoidance-in-rats
#11
Amanda M Maple, Tanessa Call, Phylicia C Kimmel, Ronald P Hammer
Phencyclidine (PCP), a noncompetitive N-methyl D-aspartate (NMDA) receptor antagonist, provides the most complete pharmacological model of schizophrenia in humans and animals. Acute PCP causes hyperlocomotion, disrupts prepulse inhibition (PPI), and increases social avoidance in rats. We previously showed that repeated treatment with the dopamine (DA) D2-like receptor agonists, quinpirole or ropinirole, prevents agonist-induced PPI disruption. The present study examines whether repeated ropinirole treatment similarly attenuates the effects of PCP in a more complete model of schizophrenia symptoms...
February 6, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28167259/memantine-reduces-the-production-of-amyloid-%C3%AE-peptides-through-modulation-of-amyloid-precursor-protein-trafficking
#12
Kaori Ito, Takuya Tatebe, Kunimichi Suzuki, Takashi Hirayama, Maki Hayakawa, Hideo Kubo, Taisuke Tomita, Mitsuhiro Makino
Memantine, an uncompetitive glutamatergic N-methyl-D-aspartate (NMDA) receptor antagonist, is widely used as medication for the treatment of Alzheimer's disease (AD). It has been reported that memantine reduces amyloid-β peptide (Aβ) levels in both neuronal cultures and in brains of animal models of AD. However, the underlying mechanism of these effects is unclear. Here we examined the effect of memantine on Aβ production. Memantine was administered to 9-month-old Tg2576 mice, a transgenic mouse model of AD, at 10 or 20mg/kg/day in drinking water for 1 month...
February 4, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28167133/nmda-receptor-adjusted-co-administration-of-ecstasy-and-cannabinoid-receptor-1-agonist-in-the-amygdala-via-stimulation-of-bdnf-trk-b-creb-pathway-in-adult-male-rats
#13
Ghorbangol Ashabi, Mitra-Sadat Sadat-Shirazi, Solmaz Khalifeh, Laleh Elhampour, Mohammad-Reza Zarrindast
Consumption of cannabinoid receptor-1 (CB-1) agonist such as cannabis is widely taken in 3,4- methylenedioxymethamphetamine (MDMA) or ecstasy users; it has been hypothesized that co-consumption of CB-1 agonist might protect neurons against MDMA toxicity. N-methyl-d-aspartate (NMDA) receptors regulate neuronal plasticity and firing rate in the brain through Tyrosine-kinase B (Trk-B) activation. The molecular and electrophysiological association among NMDA and MDMA/Arachidonylcyclopropylamide (ACPA, a selective CB-1 receptor agonist) co-consumption was not well-known...
February 3, 2017: Brain Research Bulletin
https://www.readbyqxmd.com/read/28163142/fmri-study-of-the-role-of-glutamate-nmda-receptor-in-the-olfactory-adaptation-in-rats-insights-into-cellular-and-molecular-mechanisms-of-olfactory-adaptation
#14
Fuqiang Zhao, Xiaohai Wang, Hatim A Zariwala, Jason M Uslaner, Andrea K Houghton, Jeffrey L Evelhoch, Eric Hostetler, Christopher T Winkelmann, Catherine D G Hines
Olfactory adaptation, characterized by attenuation of response to repeated odor stimulations or continuous odor exposure, is an intrinsic feature of olfactory processing. Adaptation can be induced by either "synaptic depression" due to depletion of neurotransmitters, or "enhanced inhibition" onto principle neurons by local inhibitory interneurons in olfactory structures. It is not clear which mechanism plays a major role in olfactory adaptation. More importantly, molecular sources of enhanced inhibition have not been identified...
February 3, 2017: NeuroImage
https://www.readbyqxmd.com/read/28161375/receptor-stimulated-transamidation-induces-activation-of-rac1-and-cdc42-and-the-regulation-of-dendritic-spines
#15
Zhen Mi, Tuda Si, Khushboo Kapadia, Qian Li, Nancy A Muma
Regulation of dendritic spines is an important component of synaptic function and plasticity whereas dendritic spine dysregulation is related to several psychiatric and neurological diseases. In the present study, we tested the hypothesis that serotonin (5-HT)2A/2C receptor-induced Rho family transamidation and activation regulates dendritic spine morphology and that activation of multiple types of receptors can induce transglutaminase (TGase)-catalyzed transamidation of small G proteins. We previously reported a novel 5-HT2A receptor downstream effector, TGase-catalyzed serotonylation of the small G protein Rac1 in A1A1v cells, a rat embryonic cortical cell line...
February 1, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28161374/chronic-gabaergic-blockade-in-the-spinal-cord-in%C3%A2-vivo-induces-motor-alterations-and-neurodegeneration
#16
Uri Nimrod Ramírez-Jarquín, Ricardo Tapia
Inhibitory GABAergic and glycinergic neurotransmission in the spinal cord play a central role in the regulation of neuronal excitability, by maintaining a balance with the glutamate-mediated excitatory transmission. Glutamatergic agonists infusion in the spinal cord induce motor neuron death by excitotoxicity, leading to motor deficits and paralysis, but little is known on the effect of the blockade of inhibitory transmission. In this work we studied the effects of GABAergic and glycinergic blockade, by means of microdialysis perfusion (acute administration) and osmotic minipumps infusion (chronic administration) of GABA and glycine receptors antagonists directly in the lumbar spinal cord...
February 1, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28154892/differential-effects-of-antipsychotic-and-propsychotic-drugs-on-prepulse-inhibition-and-locomotor-activity-in-roman-high-rha-and-low-avoidance-rla-rats
#17
Ignasi Oliveras, Ana Sánchez-González, Daniel Sampedro-Viana, Maria Antonietta Piludu, Cristóbal Río-Alamos, Osvaldo Giorgi, Maria G Corda, Susana Aznar, Javier González-Maeso, Cristina Gerbolés, Gloria Blázquez, Toni Cañete, Adolf Tobeña, Alberto Fernández-Teruel
RATIONALE: Animal models with predictive and construct validity are necessary for developing novel and efficient therapeutics for psychiatric disorders. OBJECTIVES: We have carried out a pharmacological characterization of the Roman high- (RHA-I) and low-avoidance (RLA-I) rat strains with different acutely administered propsychotic (DOI, MK-801) and antipsychotic drugs (haloperidol, clozapine), as well as apomorphine, on prepulse inhibition (PPI) of startle and locomotor activity (activity cages)...
February 2, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28139961/functional-comparison-of-neuronal-cells-differentiated-from-human-induced-pluripotent-stem-cell-derived-neural-stem-cells-under-different-oxygen-and-medium-conditions
#18
Kazuto Yamazaki, Kazuyuki Fukushima, Michiko Sugawara, Yoshikuni Tabata, Yoichi Imaizumi, Yasuharu Ishihara, Masashi Ito, Kappei Tsukahara, Jun Kohyama, Hideyuki Okano
Because neurons are difficult to obtain from humans, generating functional neurons from human induced pluripotent stem cells (hiPSCs) is important for establishing physiological or disease-relevant screening systems for drug discovery. To examine the culture conditions leading to efficient differentiation of functional neural cells, we investigated the effects of oxygen stress (2% or 20% O2) and differentiation medium (DMEM/F12:Neurobasal-based [DN] or commercial [PhoenixSongs Biologicals; PS]) on the expression of genes related to neural differentiation, glutamate receptor function, and the formation of networks of neurons differentiated from hiPSCs (201B7) via long-term self-renewing neuroepithelial-like stem (lt-NES) cells...
December 2016: Journal of Biomolecular Screening
https://www.readbyqxmd.com/read/28138895/the-impact-of-cb2-receptor-ligands-on-the-mk-801-induced-hyperactivity-in-mice
#19
Marta Kruk-Slomka, Izabela Banaszkiewicz, Grazyna Biala
It has been known that there is a relationship between cannabis use and schizophrenia-related symptoms; however, it can be a subject of controversy. The involvement of CB1 receptor ligands in the schizophrenia has already been revealed and confirmed. However, there is still lack of information concerning the role of CB2 receptors in the psychosis-like effects in mice and the further studies are needed.The aim of the present research was to study the role of the CB2 receptor ligands in the symptoms typical for schizophrenia...
January 30, 2017: Neurotoxicity Research
https://www.readbyqxmd.com/read/28138040/comparative-effects-of-ly3020371-a-potent-and-selective-mglu2-3-receptor-antagonist-and-ketamine-a-non-competitive-nmda-receptor-antagonist-in-rodents-evidence-supporting-use-for-the-treatment-of-depression
#20
Jeffrey M Witkin, Stephen Mitchell, Keith Wafford, Guy Carter, Gary Gilmour, Jennifer Li, Brian Eastwood, Carl Overshiner, Xia Li, Linda Rorick-Kehn, Kurt Rasmussen, Wesley Anderson, Alexander Nikolayev, Vladamir Tolstikov, Ming-Shang Kuo, John Catlow, Renhua Li, Stephen Smith, Charles Mitch, Paul Ornstein, Stephen Swanson, James Monn
The ability of the NMDA receptor antagonist ketamine to alleviate symptoms in patients suffering from treatment resistant depression (TRD) is well documented. In this report, we directly compare in vivo biological responses in rodents elicited by a recently discovered mGlu2/3 receptor antagonist (LY3020371) with those produced by ketamine. Both LY3020371 and ketamine increased the number of spontaneously active DA cells in the ventral tegmental area of anesthetized rats, increased O2 in the anterior cingulate cortex, promoted wakefulness, enhanced the efflux of biogenic amines in the prefrontal cortex, and produced antidepressant-related behavioral effects in SSRI-sensitive and -insensitive rodent models...
January 30, 2017: Journal of Pharmacology and Experimental Therapeutics
keyword
keyword
69628
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"