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https://www.readbyqxmd.com/read/28221080/blockade-of-glutamatergic-transmission-in-the-primate-basolateral-amygdala-suppresses-active-behavior-without-altering-social-interaction
#1
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/28220045/paternal-cocaine-taking-elicits-epigenetic-remodeling-and-memory-deficits-in-male-progeny
#2
M E Wimmer, L A Briand, B Fant, L A Guercio, A C Arreola, H D Schmidt, S Sidoli, Y Han, B A Garcia, R C Pierce
Paternal environmental perturbations including exposure to drugs of abuse can produce profound effects on the physiology and behavior of offspring via epigenetic modifications. Here we show that adult drug-naive male offspring of cocaine-exposed sires have memory formation deficits and associated reductions in NMDA receptor-mediated hippocampal synaptic plasticity. Reduced levels of the endogenous NMDA receptor co-agonist d-serine were accompanied by increased expression of the d-serine degrading enzyme d-amino acid oxidase (Dao1) in the hippocampus of cocaine-sired male progeny...
February 21, 2017: Molecular Psychiatry
https://www.readbyqxmd.com/read/28218838/design-and-synthesis-of-enantiomerically-pure-decahydroquinoxalines-as-potent-and-selective-%C3%AE%C2%BA-opioid-receptor-agonists-with-anti-inflammatory-activity-in-vivo
#3
Michael Soeberdt, Peter Molenveld, Roy P M Storcken, Renaud Bouzanne des Mazery, Geert Jan Sterk, Reshma Autar, Marjon G Bolster, Clemens Wagner, Sebastianus N H Aerts, Frank R van Holst, Anita Wegert, Giovanni Tangherlini, Bastian Frehland, Dirk Schepmann, Dieter Metze, Tobias Lotts, Ulrich Knie, Kun-Yuan Lin, Tai-Yu Huang, Chih-Ching Lai, Sonja Ständer, Bernhard Wünsch, Christoph Abels
In order to develop novel κ agonists restricted to the periphery, a diastereo- and enantioselective synthesis of (4aR,5S,8aS)-configured decahydroquinoxalines 5-8 was developed. Physicochemical and pharmacological properties were fine-tuned by structural modifications in the arylacetamide and amine part of the pharmacophore as well as in the amine part outside the pharmacophore. The decahydroquinoxalines 5-8 show single-digit nanomolar to subnanomolar κ-opioid receptor affinity, full κ agonistic activity in the [(35)S]GTPγS assay, and high selectivity over μ, δ, σ1, and σ2 receptors as well as the PCP binding site of the NMDA receptor...
February 20, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28202572/differential-regulation-of-nmda-receptors-by-d-serine-and-glycine-in-mammalian-spinal-locomotor-networks
#4
David Acton, Gareth Brian Miles
Activation of N-methyl-D-aspartate receptors (NMDARs) requires the binding of a co-agonist, either D-serine or glycine, in addition to glutamate. Changes in occupancy of the co-agonist binding site are proposed to modulate neural networks including those controlling swimming in frog tadpoles. Here, we characterize regulation of the NMDAR co-agonist binding site in mammalian spinal locomotor networks. Blockade of NMDARs by D(-)-2-amino-5-phosphonopentanoic acid (D-APV) or 5,7-dichlorokynurenic acid reduced the frequency and amplitude of pharmacologically induced locomotor-related activity recorded from the ventral roots of spinal-cord preparations from neonatal mice...
February 15, 2017: Journal of Neurophysiology
https://www.readbyqxmd.com/read/28202437/oscillation-patterns-are-enhanced-and-firing-threshold-is-lowered-in-medullary-respiratory-neuron-discharges-by-threshold-doses-of-a-%C3%AE-opioid-receptor-agonist
#5
Peter M Lalley, Steve W Mifflin
μ-Opioid receptors are distributed widely in the brainstem respiratory network, and opioids with selectivity for μ-type receptors slow in-vivo respiratory rhythm in lowest effective doses. Several studies have reported μ-opioid receptor effects on the three-phase rhythm of respiratory neurons, but there are until now no reports of opioid effects on oscillatory activity within respiratory discharges. In this study, effects of the μ-opioid receptor agonist fentanyl on spike train discharge properties of several different types of rhythm-modulating medullary respiratory neuron discharges were analyzed...
February 15, 2017: American Journal of Physiology. Regulatory, Integrative and Comparative Physiology
https://www.readbyqxmd.com/read/28192174/does-genetic-bdnf-deficiency-in-rats-interact-with-neurotransmitter-control-of-prepulse-inhibition-implications-for-schizophrenia
#6
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/28182698/prevention-of-remifentanil-induced-postoperative-hyperalgesia-by-dexmedetomidine-via-regulating-the-trafficking-and-function-of-spinal-nmda-receptors-as-well-as-pkc-and-camkii-level-in-vivo-and-in-vitro
#7
Yuan Yuan, Zhe Sun, Yi Chen, Yuxin Zheng, Ke-Liang Xie, Ying He, Zhifen Wang, Guo-Lin Wang, Yong-Hao Yu
Remifentanil-induced secondary hyperalgesia has been demonstrated in both animal experiments and clinical trials. Enhancement of N-methyl-D-aspartate (NMDA) receptor trafficking as well as protein kinase C (PKC) and calmodulin-dependent protein kinase II (CaMKII) have been reported to be involved in the induction and maintenance of central sensitization. In the current study, it was demonstrated that dexmedetomidine could prevent remifentanil-induced hyperalgesia (RIH) via regulating spinal NMDAR-PKC-Ca2+/ CaMKII pathway in vivo and in vitro...
2017: PloS One
https://www.readbyqxmd.com/read/28167638/effects-of-repeated-ropinirole-treatment-on-phencyclidine-induced-hyperlocomotion-prepulse-inhibition-deficits-and-social-avoidance-in-rats
#8
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/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
#9
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/28161374/chronic-gabaergic-blockade-in-the-spinal-cord-in%C3%A2-vivo-induces-motor-alterations-and-neurodegeneration
#10
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
#11
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
#12
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
#13
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/28134447/t-type-calcium-channels-contribute-to-nmda-receptor-independent-synaptic-plasticity-in-hippocampal-regular-spiking-oriens-alveus-interneurons
#14
Elizabeth Nicholson, Dimitri M Kullmann
NMDA receptor-independent long-term potentiation (LTP) in hippocampal stratum oriens-alveus (O/A) interneurons requires co-activation of postsynaptic group I metabotropic glutamate receptors (mGluRs) and Ca(2+) -permeable AMPA receptors. The rectification properties of such AMPA receptors contribute to the preferential induction of LTP at hyperpolarized potentials. A persistent increase in excitatory transmission can also be triggered by exogenous activation of group I mGluRs while the interneuron is hyperpolarized, or by postsynaptic trains of action potentials in the absence of presynaptic stimulation...
January 30, 2017: Journal of Physiology
https://www.readbyqxmd.com/read/28132136/multimodal-analgesia-current-concepts-and-acute-pain-considerations
#15
REVIEW
Erik M Helander, Bethany L Menard, Chris M Harmon, Ben K Homra, Alexander V Allain, Gregory J Bordelon, Melville Q Wyche, Ira W Padnos, Anna Lavrova, Alan D Kaye
PURPOSE OF REVIEW: Management of acute pain following surgery using a multimodal approach is recommended by the American Society of Anesthesiologists whenever possible. In addition to opioids, drugs with differing mechanisms of actions target pain pathways resulting in additive and/or synergistic effects. Some of these agents include alpha 2 agonists, NMDA receptor antagonists, gabapentinoids, dexamethasone, NSAIDs, acetaminophen, and duloxetine. RECENT FINDINGS: Alpha 2 agonists have been shown to have opioid-sparing effects, but can cause hypotension and bradycardia and must be taken into consideration when administered...
January 2017: Current Pain and Headache Reports
https://www.readbyqxmd.com/read/28119997/peripheral-nmda-receptor-no-system-blockage-inhibits-itch-responses-induced-by-chloroquine-in-mice
#16
Nazgol-Sadat Haddadi, Arash Foroutan, Sattar Ostadhadi, Ehsan Azimi, Nastaran Rahimi, Mehdi Nateghpour, Ethan A Lerner, Ahmad Reza Dehpour
Intradermal administration of chloroquine (CQ) provokes scratching behavior in mice. Chloroquine-induced itch is histamine-independent and we have reported that the nitric oxide (NO)/cyclic guanosine monophosphate (cGMP) pathway is involved in CQ-induced scratching behavior in mice. Previous studies have demonstrated that activation of N-methyl-d-aspartate receptors (NMDARs) induces NO production. Here we show that NMDAR antagonists significantly decrease CQ-induced scratching in mice while a non-effective dose of an NMDAR agonist potentiates the scratching behavior provoked by sub-effective doses of CQ...
January 25, 2017: Acta Dermato-venereologica
https://www.readbyqxmd.com/read/28112265/excessive-activation-of-ionotropic-glutamate-receptors-induces-apoptotic-hair-cell-death-independent-of-afferent-and-efferent-innervation
#17
Lavinia Sheets
Accumulation of excess glutamate plays a central role in eliciting the pathological events that follow intensely loud noise exposures and ischemia-reperfusion injury. Glutamate excitotoxicity has been characterized in cochlear nerve terminals, but much less is known about whether excess glutamate signaling also contributes to pathological changes in sensory hair cells. I therefore examined whether glutamate excitotoxicity damages hair cells in zebrafish larvae exposed to drugs that mimic excitotoxic trauma...
January 23, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28112061/inflammation-and-depression-a-causal-or-coincidental-link-to-the-pathophysiology
#18
Brian E Leonard
This review summarises the evidence that chronic low grade inflammation triggers changes that contribute to the mental and physical ill health of patients with major depression. Inflammation, and the activation of the hypothalamic pituitary axis by stress, are normal components of the stress response but when stress is prolonged and the endocrine and immune system become chronic resulting in the activation of the peripheral macrophages, the central microglia and hypercortisolemia, the neuronal networks are damaged and become dysfunctional...
January 23, 2017: Acta Neuropsychiatrica
https://www.readbyqxmd.com/read/28108357/sigma-1-receptor-deficiency-reduces-gabaergic-inhibition-in-the-basolateral-amygdala-leading-to-ltd-impairment-and-depressive-like-behaviors
#19
Baofeng Zhang, Ling Wang, Tingting Chen, Juan Hong, Sha Sha, Jun Wang, Hang Xiao, Ling Chen
Sigma-1 receptor knockout (σ1R(-/-)) in male mice causes depressive-like phenotype. We observed the expression of σ1R in principal neurons of basolateral amygdala (BLA), a main region for affective regulation. The present study investigated the influence of σ1R deficiency in BLA neurons on synaptic properties and plasticity at cortico-BLA pathway. In comparison with wild-type (WT) mice, the slopes of field excitatory postsynaptic potentials (fEPSP) were reduced in σ1R(-/-) mice with the increases in paired-pulse facilitation (PPF) and paired-pulse inhibition (PPI) values...
January 17, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28095420/molecular-mechanism-of-disease-associated-mutations-in-the-pre-m1-helix-of-nmda-receptors-and-potential-rescue-pharmacology
#20
Kevin K Ogden, Wenjuan Chen, Sharon A Swanger, Miranda J McDaniel, Linlin Z Fan, Chun Hu, Anel Tankovic, Hirofumi Kusumoto, Gabrielle J Kosobucki, Anthony J Schulien, Zhuocheng Su, Joseph Pecha, Subhrajit Bhattacharya, Slavé Petrovski, Adam E Cohen, Elias Aizenman, Stephen F Traynelis, Hongjie Yuan
N-methyl-D-aspartate receptors (NMDARs), ligand-gated ionotropic glutamate receptors, play key roles in normal brain development and various neurological disorders. Here we use standing variation data from the human population to assess which protein domains within NMDAR GluN1, GluN2A and GluN2B subunits show the strongest signal for being depleted of missense variants. We find that this includes the GluN2 pre-M1 helix and linker between the agonist-binding domain (ABD) and first transmembrane domain (M1). We then evaluate the functional changes of multiple missense mutations in the NMDAR pre-M1 helix found in children with epilepsy and developmental delay...
January 2017: PLoS Genetics
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