keyword
MENU ▼
Read by QxMD icon Read
search

nmda agonist

keyword
https://www.readbyqxmd.com/read/29331922/minimum-alveolar-concentration-key-concepts-and-a-review-of-its-pharmacological-reduction-in-dogs-part-1
#1
REVIEW
Rachel Reed, Thomas Doherty
OBJECTIVE: To outline the major components of the minimum alveolar concentration (MAC) and review the literature in regard to pharmacological manipulation of the MAC of halothane, isoflurane, sevoflurane, enflurane, and desflurane in dogs. The pharmacologic agents included are alpha-2 agonists, benzodiazepines, propofol, maropitant, opioids, lidocaine, acepromazine, non-steroidal anti-inflammatory agents, and NMDA antagonists. Part 1 will focus on summarizing the relevance, measurement, and mechanisms of MAC and review the effects of alpha-2 agonists, benzodiazepines, and propofol on MAC...
January 9, 2018: Research in Veterinary Science
https://www.readbyqxmd.com/read/29317600/altered-avalanche-dynamics-in-a-developmental-nmdar-hypofunction-model-of-cognitive-impairment
#2
Saurav Seshadri, Andreas Klaus, Daniel E Winkowski, Patrick O Kanold, Dietmar Plenz
Disturbed activity patterns in cortical networks contribute to the pathophysiology of schizophrenia (SZ). Several lines of evidence implicate NMDA receptor hypofunction in SZ, and blocking NMDA receptor signaling during early neurodevelopment produces cognitive deficits in rodent models that resemble those seen in schizophrenic patients. However, the altered network dynamics underlying these cognitive impairments largely remain to be characterized, especially at the cellular level. Here, we use in vivo two-photon calcium imaging to describe pathological dynamics, occurring in parallel with cognitive dysfunction, in a developmental NMDA receptor hypofunction model...
January 10, 2018: Translational Psychiatry
https://www.readbyqxmd.com/read/29297151/liver-x-receptor-agonist-gw3965-regulates-synaptic-function-upon-amyloid-beta-exposure-in-hippocampal-neurons
#3
C Báez-Becerra, F Filipello, A Sandoval-Hernández, H Arboleda, G Arboleda
Alzheimer's disease (AD) is a devastating neurodegenerative disease characterized by beta-amyloid (Aβ) accumulation and neurofibrillary tangles formation in the brain which are associated to synaptic deficits and dementia. Liver X receptor (LXR) agonists have been demonstrated to revert of pathologic and cognitive defects in murine models of AD through the regulation of Apolipoprotein E, ATP-Binding Cassette A1 (ABCA1), by dampening neuroinflammation and also by reducing the levels of amyloid-β (Aβ) accumulation in the brain...
January 3, 2018: Neurotoxicity Research
https://www.readbyqxmd.com/read/29277459/design-synthesis-and-evaluation-of-novel-inhibitors-for-wild-type-human-serine-racemase
#4
Satoyuki Takahara, Kiyomi Nakagawa, Tsugumi Uchiyama, Tomoyuki Yoshida, Kazunori Matsumoto, Yasuo Kawasumi, Mineyuki Mizuguchi, Takayuki Obita, Yurie Watanabe, Daichi Hayakawa, Hiroaki Gouda, Hisashi Mori, Naoki Toyooka
Most of the endogenous free d-serine (about 90%) in the brain is produced by serine racemase (SR). d-Serine in the brain is involved in neurodegenerative disorders and epileptic states as an endogenous co-agonist of the NMDA-type glutamate receptor. Thus, SR inhibitors are expected to be novel therapeutic candidates for the treatment of these disorders. In this study, we solved the crystal structure of wild-type SR, and tried to identify a new inhibitor of SR by in silico screening using the structural information...
December 13, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29273965/effects-of-%C3%AE-7-nicotinic-receptor-activation-on-cell-survival-in-rat-organotypic-hippocampal-slice-cultures
#5
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/29249806/cortical-high-gamma-network-oscillations-and-connectivity-a-translational-index-for-antipsychotics-to-normalize-aberrant-neurophysiological-activity
#6
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
https://www.readbyqxmd.com/read/29242355/the-bioactive-protein-ligand-conformation-of-glun2c-selective-positive-allosteric-modulators-bound-to-the-nmda-receptor
#7
Thomas Maxwell Kaiser, Steven A Kell, Hirofumi Kusumoto, Gil Shaulsky, Subhrajit Bhattacharya, Matthew P Epplin, Katie L Strong, Eric J Miller, Bryan D Cox, David S Menaldino, Dennis C Liotta, Stephen F Traynelis, Pieter Buys Burger
NMDA receptors are ligand-gated, cation-selective channels that mediate a slow component of excitatory synaptic transmission. Subunit-selective positive allosteric modulators of NMDA receptor function have therapeutically-relevant effects on multiple processes in the brain. A series of pyrrolidinones, such as PYD-106, that selectively potentiate NMDA receptors that contain the GluN2C subunit have structural determinants of activity that reside between the GluN2C amino terminal domain and the GluN2C agonist binding domain, suggesting a unique site of action...
December 14, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/29239974/additive-and-subadditive-antiallodynic-interactions-between-%C3%AE-opioid-agonists-and-n-methyl-d-aspartate-antagonists-in-male-rhesus-monkeys
#8
Jeremy C Cornelissen, Floyd F Steele, Kenner C Rice, Katherine L Nicholson, Matthew L Banks
μ-Opioid agonists are clinically effective analgesics, but also produce undesirable effects such as sedation and abuse potential that limit their clinical utility. Glutamatergic systems also modulate nociception and N-methyl D-aspartate (NMDA) receptor antagonists have been proposed as one useful adjunct to enhance the therapeutic effects and/or attenuate the undesirable effects of μ-opioid agonists. Whether NMDA antagonists enhance the antiallodynic effects of μ-agonists in preclinical models of thermal hypersensitivity (i...
December 12, 2017: Behavioural Pharmacology
https://www.readbyqxmd.com/read/29229558/enhanced-activities-of-%C3%AE-subunit-containing-gabaa-receptors-blocked-spinal-long-term-potentiation-and-attenuated-formalin-induced-spontaneous-pain
#9
Jiang-Ping Liu, Yong-Tao He, Xing-Lian Duan, Zhan-Wei Suo, Xian Yang, Xiao-Dong Hu
The δ subunit-containing γ-Aminobutyric acid type A receptors (δ-GABAARs) are located at extrasynaptic sites and persistently active in the control of neuronal excitability. Here we recorded primary afferent C fiber-evoked field potentials in the superficial dorsal horn of rat spinal cords in vivo, and investigated the possible influence of δ-GABAARs activities on nociceptive synaptic transmission. We found that δ-GABAARs-preferring agonist THIP, when topically applied onto spinal cord dorsum, inhibited the basal synaptic responses in a dose-dependent manner...
December 8, 2017: Neuroscience
https://www.readbyqxmd.com/read/29203848/bdnf-release-and-signaling-are-required-for-the-antidepressant-actions-of-glyx-13
#10
T Kato, M V Fogaça, S Deyama, X-Y Li, K Fukumoto, R S Duman
Conventional antidepressant medications, which act on monoaminergic systems, display significant limitations, including a time lag of weeks to months and low rates of therapeutic efficacy. GLYX-13 is a novel glutamatergic compound that acts as an N-methyl-d-aspartate (NMDA) modulator with glycine-like partial agonist properties; like the NMDA receptor antagonist ketamine GLYX-13 produces rapid antidepressant actions in depressed patients and in preclinical rodent models. However, the mechanisms underlying the antidepressant actions of GLYX-13 have not been characterized...
December 5, 2017: Molecular Psychiatry
https://www.readbyqxmd.com/read/29200911/dual-control-of-the-vestibulosympathetic-reflex-following-hypotension-in-rats
#11
Sang Eon Park, Yuan-Zhe Jin, Byung Rim Park
Orthostatic hypotension (OH) is associated with symptoms including headache, dizziness, and syncope. The incidence of OH increases with age. Attenuation of the vestibulosympathetic reflex (VSR) is also associated with an increased incidence of OH. In order to understand the pathophysiology of OH, we investigated the physiological characteristics of the VSR in the disorder. We applied sodium nitroprusside (SNP) to conscious rats with sinoaortic denervation in order to induce hypotension. Expression of pERK in the intermediolateral cell column (IMC) of the T4~7 thoracic spinal regions, blood epinephrine levels, and blood pressure were evaluated following the administration of glutamate and/or SNP...
November 2017: Korean Journal of Physiology & Pharmacology
https://www.readbyqxmd.com/read/29195907/presynaptic-%C3%AE-2-adrenoceptor-modulates-glutamatergic-synaptic-transmission-in-rat-nucleus-accumbens-in-vitro
#12
Shi-Yu Peng, Bin Li, Kang Xi, Jian-Jun Wang, Jing-Ning Zhu
The nucleus accumbens (NAc), integrating information from the prefrontal cortex and limbic structures, plays a critical role in reward and emotion regulation. Previous studies have reported that the NAc shell receives direct noradrenergic projections, and activation of α2-adrenoceptor (α2-AR) in the NAc shell decreases the fear or anxiety level of rats. However, the underlying mechanism is still little known. Intriguingly, glutamatergic neurotransmission in the NAc shell is closely related to reward and emotion...
November 30, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/29191857/evaluation-of-11c-me-nb1-as-a-potential-pet-radioligand-for-measuring-glun2b-containing-nmda-receptors-drug-occupancy-and-receptor-crosstalk
#13
Stefanie D Krämer, Thomas Betzel, Linjing Mu, Ahmed Haider, Adrienne Herde Müller, Anna K Boninsegni, Claudia Keller, Marina Szermerski, Roger Schibli, Bernhard Wünsch, Simon M Ametamey
Clinical and preclinical research with modulators binding to the NMDA receptor GluN2B N-terminal domain (NTD) aim for the treatment of various neurological diseases. However, the interpretation of the results is hampered by the lack of a suitable NMDA PET tracer for assessing the receptor occupancy of candidate drugs. We have developed [11C]Me-NB1 as a PET tracer for imaging GluN1/GluN2B-containing NMDA receptors and used it to investigate in rats the dose-dependent receptor occupancy of eliprodil, a GluN2B NTD modulator...
November 30, 2017: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/29176858/sepsis-induced-selective-loss-of-nmda-receptors-modulates-hippocampal-neuropathology-in-surviving-septic-mice
#14
Shuibing Zhang, Xueqin Wang, Sha Ai, Wen Ouyang, Yuan Le, Jianbin Tong
BACKGROUND: Sepsis-induced neuroinflammation plays an important role in sepsis-related brain dysfunction. However, the molecules that are targeted during neuroinflammation resulting from sepsis-induced brain dysfunction remain unclear. Herein, we tried to investigate the expression and roles of NMDA receptor subunits during sepsis-related brain dysfunction. METHODS: Sepsis was induced by cecal ligation and perforation (CLP) or by a single intraperitoneal injection of lipopolysaccharide (LPS, 8 mg/kg) in C57BL/6J mice...
2017: PloS One
https://www.readbyqxmd.com/read/29161500/a-small-molecule-mimetic-of-the-humanin-peptide-as-a-candidate-for-modulating-nmda-induced-neurotoxicity
#15
Mohammad Parvez Alam, Tina Bilousova, Patricia Spilman, Kanagasabai Vadivel, Dongsheng Bai, Denis Evseenko, Varghese John
Humanin (HN), a 24-amino acid bioactive peptide, has been shown to increase cell survival of neurons after exposure to Aβ and NMDA-induced toxicity and thus could be beneficial in the treatment of Alzheimer's disease (AD). The neuroprotection by HN is reported to be primarily through its agonist binding properties to the gp130 receptor. However, peptidic nature of HN presents challenges in its development as a therapeutic for AD. We report here for the first time the elucidation of the binding site of Humanin (HN) peptide to gp130 receptor extracellular domain through modeling and the synthesis of small molecule mimetics that interact with the HN binding site on the gp130 receptor that provides protection against NMDA-induced neurotoxicity in primary hippocampal neurons...
November 21, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29128144/the-antipsychotic-drug-brexpiprazole-reverses-phencyclidine-induced-disruptions-of-thalamocortical-networks
#16
Hanna E van den Munkhof, Jørn Arnt, Pau Celada, Francesc Artigas
Brexpiprazole (BREX), a recently approved antipsychotic drug in the US and Canada, improves cognitive dysfunction in animal models, by still largely unknown mechanisms. BREX is a partial agonist at 5-HT1A and D2 receptors and antagonist at α1B- and α2C-adrenergic and 5-HT2A receptors all with a similar potency. The NMDA receptor antagonist phencyclidine (PCP), used as pharmacological model of schizophrenia, activates thalamocortical networks and decreases low frequency oscillations (LFO; <4 Hz). These effects are reversed by antipsychotics...
November 8, 2017: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/29127015/oxotremorine-m-potentiates-nmda-receptors-by-muscarinic-receptor-dependent-and-independent-mechanisms
#17
Ruud Zwart, Hannah Reed, Emanuele Sher
Muscarinic acetylcholine M1 receptors play an important role in synaptic plasticity in the hippocampus and cortex. Potentiation of NMDA receptors as a consequence of muscarinic acetylcholine M1 receptor activation is a crucial event mediating the cholinergic modulation of synaptic plasticity, which is a cellular mechanism for learning and memory. In Alzheimer's disease, the cholinergic input to the hippocampus and cortex is severely degenerated, and agonists or positive allosteric modulators of M1 receptors are therefore thought to be of potential use to treat the deficits in cognitive functions in Alzheimer's disease...
November 7, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29121294/low-dose-buprenorphine-infusion-to-prevent-postoperative-hyperalgesia-in-patients-undergoing-major-lung-surgery-and-remifentanil-infusion-a-double-blind-randomized-active-controlled-trial
#18
Marco Mercieri, Stefano Palmisani, Roberto A De Blasi, Antonio D'Andrilli, Alessia Naccarato, Barbara Silvestri, Sara Tigano, Domenico Massullo, Monica Rocco, Roberto Arcioni
Background: Postoperative secondary hyperalgesia arises from central sensitization due to pain pathways facilitation and/or acute opioid exposure. The latter is also known as opioid-induced hyperalgesia (OIH). Remifentanil, a potent μ-opioid agonist, reportedly induces postoperative hyperalgesia and increases postoperative pain scores and opioid consumption. The pathophysiology underlying secondary hyperalgesia involves N-methyl-D-aspartate (NMDA)-mediated pain pathways. In this study, we investigated whether perioperatively infusing low-dose buprenorphine, an opioid with anti-NMDA activity, in patients receiving remifentanil infusion prevents postoperative secondary hyperalgesia...
October 1, 2017: British Journal of Anaesthesia
https://www.readbyqxmd.com/read/29106899/vinpocetine-protects-inner-retinal-neurons-with-functional-nmda-glutamate-receptors-against-retinal-ischemia
#19
Lisa Nivison-Smith, Pauline Khoo, Monica L Acosta, Michael Kalloniatis
Retinal ischemia is involved in the pathogenesis of many major vision threatening diseases. Vinpocetine is a natural drug, which has a range of neuroprotective actions against retinal ischemia including modulating cation flow, improving metabolic activity and preventing apoptosis. The exact mechanism behind these actions remains unknown but may involve glutamate receptors, major components of the ischemic cascade. This study examined the effects of vinpocetine in association with specific ionotropic glutamate receptor agonists: N-methyl-D-aspartate (NMDA) and kainate...
November 4, 2017: Experimental Eye Research
https://www.readbyqxmd.com/read/29106383/s-sulfocysteine-nmda-receptor-dependent-signaling-underlies-neurodegeneration-in-molybdenum-cofactor-deficiency
#20
Avadh Kumar, Borislav Dejanovic, Florian Hetsch, Marcus Semtner, Debora Fusca, Sita Arjune, Jose Angel Santamaria-Araujo, Aline Winkelmann, Scott Ayton, Ashley I Bush, Peter Kloppenburg, Jochen C Meier, Guenter Schwarz, Abdel Ali Belaidi
Molybdenum cofactor deficiency (MoCD) is an autosomal recessive inborn error of metabolism characterized by neurodegeneration and death in early childhood. The rapid and progressive neurodegeneration in MoCD presents a major clinical challenge and may relate to the poor understanding of the molecular mechanisms involved. Recently, we reported that treating patients with cyclic pyranopterin monophosphate (cPMP) is a successful therapy for a subset of infants with MoCD and prevents irreversible brain damage. Here, we studied S-sulfocysteine (SSC), a structural analog of glutamate that accumulates in the plasma and urine of patients with MoCD, and demonstrated that it acts as an N-methyl D-aspartate receptor (NMDA-R) agonist, leading to calcium influx and downstream cell signaling events and neurotoxicity...
November 6, 2017: Journal of Clinical Investigation
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"