keyword
MENU ▼
Read by QxMD icon Read
search

nmda agonist

keyword
https://www.readbyqxmd.com/read/29793153/effects-of-mg-2-on-recovery-of-nmda-receptors-from-inhibition-by-memantine-and-ketamine-reveal-properties-of-a-second-site
#1
Nathan G Glasgow, Madeleine R Wilcox, Jon W Johnson
Memantine and ketamine are NMDA receptor (NMDAR) open channel blockers that are thought to act via similar mechanisms at NMDARs, but exhibit divergent clinical effects. Both drugs act by entering open NMDARs and binding at a site deep within the ion channel (the deep site) at which the endogenous NMDAR channel blocker Mg2+ also binds. Under physiological conditions, Mg2+ increases the IC50 s of memantine and ketamine through competition for binding at the deep site. Memantine also can inhibit NMDARs after associating with a second site accessible in the absence of agonist, a process termed second site inhibition (SSI) that is not observed with ketamine...
May 12, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29763637/neurosteroid-pregnenolone-sulfate-alone-and-as-augmentation-of-lurasidone-or-tandospirone-rescues-phencyclidine-induced-deficits-in-cognitive-function-and-social-interaction
#2
L Rajagopal, D Soni, H Y Meltzer
BACKGROUND: Pregnenolone sulfate (PregS), an endogenous neurosteroid, which negatively and positively modulates gamma amino butyric acid subunit A (GABAA ) and N-methyl D-aspartate (NMDA) receptors (R) respectively, among other potential neuroplastic changes on synaptic processes, has shown some beneficial effects on treating cognitive impairment associated with schizophrenia (CIAS) and negative symptoms. Lurasidone (Lur), an atypical antipsychotic drug (AAPD), and tandospirone (Tan), a 5-HT1A  R partial agonist, have also been reported to improve cognitive or negative symptoms, or both, in some schizophrenia patients...
May 12, 2018: Behavioural Brain Research
https://www.readbyqxmd.com/read/29763633/estradiol-induced-enhancement-of-fear-extinction-in-female-rats-the-role-of-nmda-receptor-activation
#3
Bronwyn M Graham, Elliot Scott
Converging cross-species evidence indicates that fear extinction (the laboratory basis of exposure therapy for anxiety disorders) in females is modulated by endogenous and exogenous estradiol. The mechanisms underlying estradiol's influences on fear extinction are largely undefined. However, one likely candidate is the NMDA-receptor (NMDAr), activation of which is necessary for estradiol-mediated enhancements in structural and functional neural plasticity, as well as extinction consolidation in males. Here, we demonstrate that systemic co-administration of the non-competitive NMDAr antagonist, MK801, blocked the enhancement of fear extinction by systemic estradiol in ovariectomized rats...
May 12, 2018: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/29749988/amelioration-of-pentylenetetrazole-induced-seizures-by-modulators-of-sigma-n-methyl-d-aspartate-and-ryanodine-receptors-in-mice
#4
Mojtaba Keshavarz, Behdad Yekzaman
Background: Sigma receptors, N-methyl-D-aspartate (NMDA) antagonist, and modulators of intracellular calcium may be useful for seizure control. Therefore, we aimed to evaluate the antiepileptic effects of opipramol, a sigma receptor agonist, against pentylenetetrazole (PTZ)-induced seizures in mice and assess ketamine and caffeine interaction with the antiepileptic effects of opipramol. Methods: PTZ (100 mg/kg) was used for the induction of seizure in 72 male albino Swiss strain of mice (n=8)...
March 2018: Iranian Journal of Medical Sciences
https://www.readbyqxmd.com/read/29699895/association-between-increased-serum-d-serine-and-cognitive-gains-induced-by-intensive-cognitive-training-in-schizophrenia
#5
Rogerio Panizzutti, Melissa Fisher, Coleman Garrett, Wai Hong Man, Walter Sena, Caroline Madeira, Sophia Vinogradov
Neuroscience-guided cognitive training induces significant improvement in cognition in schizophrenia subjects, but the biological mechanisms associated with these changes are unknown. In animals, intensive cognitive activity induces increased brain levels of the NMDA-receptor co-agonist d-serine, a molecular system that plays a role in learning-induced neuroplasticity and that may be hypoactive in schizophrenia. Here, we investigated whether training-induced gains in cognition were associated with increases in serum d-serine in outpatients with schizophrenia...
April 23, 2018: Schizophrenia Research
https://www.readbyqxmd.com/read/29690796/spontaneous-bold-waves-a-novel-hemodynamic-activity-in-sprague-dawley-rat-brain-detected-by-functional-magnetic-resonance-imaging
#6
Artem Shatillo, Arto Lipponen, Raimo A Salo, Heikki Tanila, Alexei Verkhratsky, Rashid Giniatullin, Olli H Gröhn
We report spontaneous hemodynamic activity termed "Spontaneous BOLD Waves" (SBWs) detected by BOLD fMRI in Sprague-Dawley rats under medetomidine anesthesia. These SBWs, which lasted several minutes, were observed in cortex, thalamus and hippocampus. The SBWs' correlates were undetectable in electrophysiological recordings, suggesting an exclusive gliovascular phenomenon dissociated from neuronal activity. SBWs were insensitive to the NMDA receptors antagonist MK-801 but were inhibited by the α1-adrenoceptor blocker prazosin...
January 1, 2018: Journal of Cerebral Blood Flow and Metabolism
https://www.readbyqxmd.com/read/29681798/the-lili-motif-of-m3-s2-linkers-is-a-component-of-the-nmda-receptor-channel-gate
#7
Marek Ladislav, Jiri Cerny, Jan Krusek, Martin Horak, Ales Balik, Ladislav Vyklicky
N-methyl-D-aspartate receptors (NMDARs) mediate excitatory synaptic transmission in the central nervous system, underlie the induction of synaptic plasticity, and their malfunction is associated with human diseases. Native NMDARs are tetramers composed of two obligatory GluN1 subunits and various combinations of GluN2A-D or, more rarely, GluN3A-B subunits. Each subunit consists of an amino-terminal, ligand-binding, transmembrane and carboxyl-terminal domain. The ligand-binding and transmembrane domains are interconnected via polypeptide chains (linkers)...
2018: Frontiers in Molecular Neuroscience
https://www.readbyqxmd.com/read/29681796/surface-expression-function-and-pharmacology-of-disease-associated-mutations-in-the-membrane-domain-of-the-human-glun2b-subunit
#8
Vojtech Vyklicky, Barbora Krausova, Jiri Cerny, Marek Ladislav, Tereza Smejkalova, Bohdan Kysilov, Miloslav Korinek, Sarka Danacikova, Martin Horak, Hana Chodounska, Eva Kudova, Ladislav Vyklicky
N-methyl-D-aspartate receptors (NMDARs), glutamate-gated ion channels, mediate signaling at the majority of excitatory synapses in the nervous system. Recent sequencing data for neurological and psychiatric patients have indicated numerous mutations in genes encoding for NMDAR subunits. Here, we present surface expression, functional, and pharmacological analysis of 11 de novo missense mutations of the human hGluN2B subunit (P553L; V558I; W607C; N615I; V618G; S628F; E657G; G820E; G820A; M824R; L825V) located in the pre-M1, M1, M2, M3, and M4 membrane regions...
2018: Frontiers in Molecular Neuroscience
https://www.readbyqxmd.com/read/29679289/cross-state-dependency-of-learning-between-tramadol-and-mk-801-in-the-mouse-dorsal-hippocampus-involvement-of-nitric-oxide-no-signaling-pathway
#9
Majid Jafari-Sabet, Shiva Amiri, Ramin Ataee
RATIONALE: Tramadol, an atypical μ-opioid receptor agonist, as a psychoactive drug, is frequently abused by human beings. Understanding the neurobiological mechanisms of drug-associated learning and memory formation may help prevent drug addiction and relapse. Previous study revealed that dorsal hippocampus (CA1) plays a crucial role in the retrieval of tramadol-associated memory and that its role depends on the expression of CA1 N-methyl-D-aspartate (NMDA) receptors (Jafari-Sabet et al...
April 21, 2018: Psychopharmacology
https://www.readbyqxmd.com/read/29663387/muscarinic-and-nicotinic-acetylcholine-receptor-agonists-current-scenario-in-alzheimer-s-disease-therapy
#10
REVIEW
Stuti Verma, Ashwini Kumar, Timir Tripathi, Awanish Kumar
OBJECTIVES: Alzheimer's disease (AD) has become the primary cause of dementia. It shows a progressive cognitive dysfunction with degenerating neurons. Acetylcholine receptors (AChRs) propagate the cognitive ability and it consists of two primary members namely muscarinic (mAChRs) and nicotinic receptors (nAChRs). Where mAChRs is G-protein coupled receptor, (nAChRs) are ligand-gated ion channels. The conventional therapeutic regimen for AD consists of three acetylcholinestearse inhibitors while a single NMDA receptor antagonist...
April 16, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29653257/%C3%AE-adrenergic-receptors-reduce-the-threshold-for-induction-and-stabilization-of-ltp-and-enhance-its-magnitude-via-multiple-mechanisms-in-the-ventral-but-not-the-dorsal-hippocampus
#11
Vassilios Papaleonidopoulos, Costas Papatheodoropoulos
The hippocampus is a functionally heterogeneous structure with the cognitive and emotional signal processing ascribed to the dorsal (DH) and the ventral hippocampus (VH) respectively. However, the underlying mechanisms are poorly understood. Noradrenaline is released in hippocampus during emotional arousal modulating synaptic plasticity and memory consolidation through activation of β adrenergic receptors (β-ARs). Using recordings of field excitatory postsynaptic potentials from the CA1 field of adult rat hippocampal slices we demonstrate that long-term potentiation (LTP) induced either by theta-burst stimulation (TBS) that mimics a physiological firing pattern of hippocampal neurons or by high-frequency stimulation is remarkably more sensitive to β-AR activation in VH than in DH...
April 10, 2018: Neurobiology of Learning and Memory
https://www.readbyqxmd.com/read/29648983/enhancement-of-brain-d-serine-mediates-recovery-of-cognitive-function-after-tbi
#12
Sigal Liraz-Zaltsman, Barbara Slusher, Dana Atrakchi-Baranes, Kinneret Rosenblatt, Yael Friedman Levi, Efrat Leah Kesner, Alcino J Silva, Anat Biegon, Esther Shohami
Cognitive deficits, especially memory loss, are common and devastating neuropsychiatric sequelae of traumatic brain injury (TBI). The deficits may persist for a long time and may be accompanied by increased risk of developing early onset dementia. Past attempts to reverse the neuropsychological effects of brain injury with glutamate-N-methyl-D-aspartate (NMDA) antagonists failed to show any benefits or worsened the outcome, suggesting activation, rather than blockage, of the NMDA receptor (NMDAR) may be useful in the sub-acute period after TBI and stroke...
March 14, 2018: Journal of Neurotrauma
https://www.readbyqxmd.com/read/29644724/a-novel-missense-mutation-in-grin2a-causes-a-nonepileptic-neurodevelopmental-disorder
#13
Ana Fernández-Marmiesse, Hirofumi Kusumoto, Saray Rekarte, Iria Roca, Jin Zhang, Scott J Myers, Stephen F Traynelis, Mª Luz Couce, Luis Gutierrez-Solana, Hongjie Yuan
BACKGROUND: Mutations in the GRIN2A gene, which encodes the GluN2A (glutamate [NMDA] receptor subunit epsilon-1) subunit of the N-methyl-d-aspartate receptor, have been identified in patients with epilepsy-aphasia spectrum disorders, idiopathic focal epilepsies with centrotemporal spikes, and epileptic encephalopathies with severe developmental delay. However, thus far, mutations in this gene have not been associated with a nonepileptic neurodevelopmental disorder with dystonia. OBJECTIVES: The objective of this study was to identify the disease-causing gene in 2 siblings with neurodevelopmental and movement disorders with no epileptiform abnormalities...
April 11, 2018: Movement Disorders: Official Journal of the Movement Disorder Society
https://www.readbyqxmd.com/read/29623852/potential-future-of-new-glutamate-agonists-and-antagonists-development
#14
Dariusz Matosiuk
Receptors of glutamic acid are known for over 30 years for their action and for about 20 years for their structure. Presence of at least three classes of ionotropic receptors was confirmed at the beginning of 80' [1]. Recognition of the sequence [2,3] and first cloning were done at the beginning of 90' [4-6]. In 1994 ligand binding site was recognized at the junction of two subunits S1-S2 in the ligand binding domain [7]. Since then many subtypes of ionotropic and metabotropic glutamate receptors were recognized, together with their localization and functions...
April 4, 2018: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29616344/novel-pharmacological-nonopioid-therapies-in-chronic-pain
#15
REVIEW
Alan David Kaye, Elyse M Cornett, Brendon Hart, Shilpadevi Patil, Andrew Pham, Matthew Spalitta, Kenneth F Mancuso
PURPOSE OF REVIEW: Opioid use and abuse has led to a worldwide opioid epidemic. And while opioids are clinically useful when appropriately indicated, they are associated with a wide range of dangerous side effects and whether they are effective at treating or eliminating chronic pain is controversial. There has long been a need for the development of nonopioid alternative treatments for patients that live in pain, and until recently, only a few effective treatments were available. Today, there are a wide range of nonopioid treatments available including NSAIDs, acetaminophen, corticosteroids, nerve blocks, SSRIs, neurostimulators, and anticonvulsants...
April 3, 2018: Current Pain and Headache Reports
https://www.readbyqxmd.com/read/29603470/a-silent-eligibility-trace-enables-dopamine-dependent-synaptic-plasticity-for-reinforcement-learning-in-the-mouse-striatum
#16
Tomomi Shindou, Mayumi Shindou, Sakurako Watanabe, Jeffery Wickens
Dopamine-dependent synaptic plasticity is a candidate mechanism for reinforcement learning. A silent eligibility trace - initiated by synaptic activity and transformed into synaptic strengthening by later action of dopamine - has been hypothesized to explain the retroactive effect of dopamine in reinforcing past behaviour. We tested this hypothesis by measuring time-dependent modulation of synaptic plasticity by dopamine in adult mouse striatum, using whole-cell recordings. Presynaptic activity followed by postsynaptic action potentials (pre-post) caused spike-timing-dependent long-term depression in D1-expressing neurons, but not in D2 neurons, and not if postsynaptic activity followed presynaptic activity...
March 30, 2018: European Journal of Neuroscience
https://www.readbyqxmd.com/read/29596901/periaqueductal-gray-glutamatergic-cannabinoid-and-vanilloid-receptor-interplay-in-defensive-behavior-and-aversive-memory-formation
#17
Franklin P Back, Antonio P Carobrez
Stimulation of the midbrain periaqueductal gray matter (PAG) in humans elicits sensations of fear and impending terror, and mediates predator defensive responses in rodents. In rats, pharmacological stimulation of the dorsolateral portion of the PAG (dlPAG) with N-Methyl-d-Aspartate (NMDA) induces aversive conditioning that acts as an unconditioned stimulus (US). In the present work, we investigated the interplay between the vanilloid TRPV1 and cannabinoid CB1 receptors in the NMDA-dlPAG defensive response and in subsequent aversive learning...
March 26, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29580893/d-cycloserine-facilitates-reversal-in-an-animal-model-of-post-traumatic-stress-disorder
#18
Sophie A George, Mariana Rodriguez-Santiago, John Riley, James L Abelson, Stan B Floresco, Israel Liberzon
Many psychiatric disorders are associated with cognitive dysfunction that is ineffectively treated by existing pharmacotherapies and which may contribute to poor real-world functioning. D-cycloserine (DCS) is a partial N-methyl-D-aspartate (NMDA) agonist that has attracted attention because of its cognitive enhancing properties, including in people with post-traumatic stress disorder (PTSD). Here, we examined the effect of DCS on reversal learning - a type of cognitive flexibility - following exposure to single prolonged stress (SPS), a rodent model of PTSD...
March 23, 2018: Behavioural Brain Research
https://www.readbyqxmd.com/read/29564482/group-ii-metabotropic-glutamate-receptor-agonist-prodrugs-ly2979165-and-ly2140023-attenuate-the-functional-imaging-response-to-ketamine-in-healthy-subjects
#19
Mitul A Mehta, Anne Schmechtig, Vasileia Kotoula, Juliet McColm, Kimberley Jackson, Claire Brittain, Sitra Tauscher-Wisniewski, Bruce J Kinon, Paul D Morrison, Thomas Pollak, Timothy Mant, Steven C R Williams, Adam J Schwarz
BACKGROUND: Aberrant glutamate neurotransmission, and in particular dysfunction of the N-methyl-D-aspartate receptor (NMDAR), has been implicated in psychiatric disorders and represents a novel therapeutic target. Low-dose administration of the NMDA antagonist ketamine in healthy volunteers elicits a strong blood oxygenation level dependent (BOLD) imaging signal that can be attenuated by pretreatment with single, therapeutically effective doses of marketed medicines interacting with the glutamate system...
March 21, 2018: Psychopharmacology
https://www.readbyqxmd.com/read/29559851/role-of-plant-derived-alkaloids-and-their-mechanism-in-neurodegenerative-disorders
#20
REVIEW
Ghulam Hussain, Azhar Rasul, Haseeb Anwar, Nimra Aziz, Aroona Razzaq, Wei Wei, Muhammad Ali, Jiang Li, Xiaomeng Li
Neurodegenerative diseases are conventionally demarcated as disorders with selective loss of neurons. Conventional as well as newer molecules have been tested but they offer just symptomatic advantages along with abundant side effects. The discovery of more compelling molecules that can halt the pathology of these diseases will be considered as a miracle of present time. Several synthetic compounds are available but they may cause several other health issues. Therefore, natural molecules from the plants and other sources are being discovered to replace available medicines...
2018: International Journal of Biological Sciences
keyword
keyword
97312
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"