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Topic: AMPA receptor


  
  AMPA Receptor Pharmacology
AMPA and Kainate receptors are built from closely related subunits (AMPA - GluR1-4; Kainate - GluR5-7, KA-1,2).
However, this compound, based on the decxahydroisoquinoline structural motif is active at GluR5 homomeric receptor channels with a similar Ki to AMPA receptor channels.
This compound is selective for GluR5 comtaining receptor complexes and is inactive at AMPA receptors, GluR6 homomeric receptors and GluR7/KA-2 heteromers.
www.bris.ac.uk /Depts/Synaptic/info/pharmacology/AMPA.html   (831 words)

  
 AMPA
Kainate receptors were previously believed to be largely presynaptic, for example they are expressed in the dorsal root ganglia, and activation of these kainate receptors has been shown to facilitate transmitter release (Schmitz et al., 2001).
In general AMPA receptor flip isoforms show somewhat slower desensitization kinetics (Mosbacher et al., 1994) and are more sensitive to the positive modulatory effects of cyclothiazide (Partin et al., 1996).
Moreover, Ca -permeable AMPA receptors seem to have an important role for correct structural and functional relations between Bergman glia and glutamatergic synapses in the cerebellum such as the removal of synaptically released glutamate (Iino et al., 2001).
www.chrisparsons.de /Chris/ampa.htm   (837 words)

  
 CNC
Glutamate receptors mediate the majority of excitatory neurotransmission in the central nervous system, and changes in the characteristics and cellular localization of these receptors are thought to underlie the mechanisms for synaptic plasticity.
We are studying the regulation of the GluR4 subunit of AMPA receptors by phosphorylation, and find that GluR4 is phosphorylated, and its phosphorylation regulates receptor activity (Carvalho et al, 1998 J. Neurochem., 1999 J. Neurosci., 2002 Eur.
We have particular interest for interacting partners of GluR4, since this AMPA receptor subunit is the first to be targeted to functional synapses in the hippocampus during development, and its synaptic targeting relies on synaptic activity.
www.uc.pt /cnc/GroupsEng/glutamate.php   (346 words)

  
 AMPA Receptor Transgenic Models
In the absence of the GluR2 subunit, AMPA receptor- and NMDA receptor-dependent LTP are additive phenomena whereas this is not the case in the presence of unedited, calcium permeable subunits.
It is possible that this reflects a role for GluR2 in the synaptic targetting of AMPA receptors (cf GluR1 global knockout), with fewer calcium permeable receptors being targetted to the synapse in the absence of a GluR2 subunit.
Alternatively, receptors may not be expressed on the cell surface due to the loss of intracellular interactions such as that with NSF.
www.bris.ac.uk /depts/Synaptic/info/transgenic/AMPAtransgenic.html   (1402 words)

  
 AMPA receptor potentiation to combat depression
Positive allosteric modulators of AMPA receptors increase brain levels of brain-derived neurotrophic factor (BDNF) that impacts the viability and generation of neurons in key brain structures.
AMPA receptor potentiators are active in rodent models predictive of antidepressant efficacy.
Thus, AMPA receptor potentiation might be a general mechanism through which the clinical outcome of antidepressant efficacy is achieved.
biopsychiatry.com /ampa.html   (270 words)

  
 Assistant Telethon Scientist
Many reports have shown that glutamate receptors play a critical role in synaptic activity, plasticity, synaptogenesis and excitoxicity in CNS synapses.
However, the precise role of glutamate receptors in regulating spines morphology is not clear.
2)Function of AMPA receptors and associated proteins in regulating synapse and dendritic spines formation.
www.telethon.it /dti/researcher.asp?idPersona=13   (480 words)

  
 Lu Chen
By focusing on the glutamate receptor family, we are attempting to understand the mechanisms of receptor targeting during synapse formation and plasticity.
We have found that when AMPA receptor subunits, PSD-95 and stargazin are co-transfected into HEK cells, they form distinctive patch-like surface clusters that are not observed when only two of the three proteins are introduced.
Taken together, these findings suggest that if we transfect AMPA receptor subunits, PSD-95, stargazin and neuroligin together into HEK cells, the AMPA receptors may preferentially cluster at sites opposing differentiated presynaptic terminals originating from nearby pontine explants, forming an "artificial synapse." We are establishing such a system and examining its structural and electrophysiological properties.
mcb.berkeley.edu /faculty/NEU/chenl.html   (576 words)

  
 Modulation of AMPA receptor activity by associated proteins
AMPA receptors are ionotropic glutamate receptors present throughout the mammalian brain, which carry the bulk of normal fast synaptic transmission.
AMPA receptor activity is dictated in part by its subunit composition and the phosphorylation state of these subunits.
Expression of stargazin with AMPA receptors caused a large increase in the current recorded from the channel, which was much greater than the increase in the surface expression of the receptor.
www.cellscience.com /Reviews5/Modulation_AMPA_receptor_associated_proteins.html   (2867 words)

  
 The Systemically Administered Competitive AMPA Receptor Antagonist, YM872, has Analgesic Effects on Thermal or ...
Hunter JC, Singh L. Role of excitatory amino acid receptors in the mediation of the nociceptive response to formalin in the rat.
Kainate GluR5 receptor subtype mediates the nociceptive response to formalin.
The role of NMDA and non-NMDA excitatory amino acid receptors in the excitation of primate spinothalamic tract neurons by mechanical, chemical, thermal and electrical stimuli.
www.anesthesia-analgesia.org /cgi/content/full/89/6/1534   (2012 words)

  
 AMPA receptor activation and phosphatase inhibition affect neonatal rat respiratory rhythm generation -- Ge and Feldman ...
Therefore, kainate receptors, while present in the respiratory neurones, are unlikely to be the principal mediator of excitatory synaptic transmission in respiratory rhythmogenesis, since both the respiratory-modulated synaptic currents and rhythmic XII nerve motor discharge were completely blocked by bath or local application of GYKI.
We hypothesize that AMPA receptor function is modulated in respiratory neurones to regulate the net inward inspiratory or expiratory current that is produced for a given amount of presynaptic inspiratory or expiratory activity, ultimately to affect the strength and timing of respiratory muscle contractions that produce breathing movements appropriate for blood gas homeostasis.
Control of the phosphorylation state of AMPA receptor subunits or associated proteins may be an essential component of the mechanisms regulating respiration, and a target site of various neuromodulators, such as serotonin, noradrenaline and various peptides that affect breathing.
jp.physoc.org /cgi/content/full/509/1/255   (6049 words)

  
 Cannabinoids in vitro and in vivo
he discovery of endocannabinoids such as anandamide and the wide spread localization of cannabinoid receptors in the brain and peripheral tissues, suggests that the cannabinoid system represents a previously unrecognized ubiquitous net work in the nervous system, whose physiology and function is unfolding.
In the voltage clamp studies we investigated the effects of anandamide on recombinant AMPA GluR3 subunit currents generated by kainic acid in oocytes expressing the AMPA glutamate receptor.
In the in-vivo studies, SR141716A, the CB1 antagonist, induced anxiolysis, that was dependent on the mouse strain used in the anxiety model and blocked the anxiogenic effects of anandamide or methanandamide whereas SR141716A had no effect on the anandamide inhibition of kainate activated currents in-vitro.
biopsychiatry.com /canbrain.htm   (272 words)

  
 AMPA receptor potentiators as smart drugs
AMPA (alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid) receptors have been demonstrated to control fast synaptic transmission.
Some AMPA receptor potentiator agents have been explored in rodent models and are now entering clinical trials.
Research complexity for these agents arises from the multiple AMPA receptor subtypes on which the molecules can act differentially, as well as from the distribution of AMPA receptors and the difficulty in studying cognition in naive rodents.
nootropics.com /ampakines/ampa-enhancers.html   (264 words)

  
 FRAXA - Fragile X Research Foundation
Stimulation of AMPA-class glutamate receptors leads to a normalization of spine shape and stimulates brain neurons to synthesize increased levels of Brain-Derived Neurotrophic Factor (BDNF).
BDNF is known to reduce spine number and length, as well as to increase AMPA receptor protein levels.
These findings suggest that in Fragile X (and in the mouse model), increases in both AMPA receptor and BDNF signaling may effect changes in synapses that should ameliorate deficits in neurotransmission.
www.fraxa.org /ra_Lauterborn.aspx   (168 words)

  
 Stargazin is an AMPA receptor auxiliary subunit.
AMPA (alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptors mediate fast excitatory synaptic transmission in brain and underlie aspects of synaptic plasticity.
However, the relative contributions of these proteins to the composition of native AMPA receptor complexes in brain remain uncertain.
In contrast, other AMPA receptor-interacting proteins, such as synapse-associated protein 97, glutamate receptor-interacting protein 1, protein kinase Calpha binding protein, N-ethylmaleimide-sensitive fusion protein, AP2, and protein 4.1N, do not show significant association with AMPA receptor complexes on native gels.
www.medscape.com /medline/abstract/15630087   (239 words)

  
 Synergistic analgesic effects of intrathecal midazolam and NMDA or AMPA receptor antagonists in rats -- Nishiyama et ...
NMDA and AMPA receptors in acute and persistent inflammatory
Kainate GluR5 receptor subtype mediates the nociceptive response to formalin in the rat.
Role of excitatory amino acid receptors in the mediation of the nociceptive response to formalin in the rat.
www.cja-jca.org /cgi/content/full/48/3/288   (2398 words)

  
 Hengye Man
AMPA type glutamate receptors (AMPA receptors) mediate the vast majority of excitatory synaptic transmission in the brain.
Phosphorylation of the AMPA receptor GluR1 subunit is required for synaptic plasticity and retention of spatial memory.
Activation of synaptic NMDA receptors induces membrane insertion of new AMPA receptors and LTP in cultured hippocampal neurons.
www.bu.edu /biology/Faculty_Staff/man.html   (833 words)

  
 AMPA Selective
Prototypical and defining agonist for the AMPA subgroup of ionotropic glutamate receptors.
Peptide inhibitor of the interaction between the C-terminus of the GluR2 (AMPA receptor) subunit and N-ethylmaleimide-sensitive fusion protein (NSF), a protein that regulates AMPA receptor function.
(1999) Surface expression of AMPA receptors in hippocampal neurons is regulated by an NSF-dependent mechanism.
www.komabiotech.co.kr /product/neuro/category/AMPA_Selective.htm   (1208 words)

  
 BioMed Central | Full text | Bi-directional modulation of AMPA receptor unitary conductance by synaptic activity
There is evidence that AMPA receptors are inserted into the postsynaptic membrane during LTP [13-15] and removed from the synapse upon induction of LTD [16,17].
Furthermore, since pep2m causes the removal of AMPA receptors from the membrane surface, as determined immunocytochemically [38,42], it is most likely that de novo LTD is due to the physical elimination of synaptic AMPA receptors.
Since AMPA receptors are known to have multiple conductance states [32,33] we have postulated that the proportion of time spent in different conductance states is the modifiable parameter [18].
www.biomedcentral.com /1471-2202/5/44   (5038 words)

  
 Clinical Trial: Effect of Talampanel (an AMPA Receptor Blocker) on Brain Activity
The purpose of this pilot study is to identify human neurophysiological parameters that are sensitive to talampanel, as assessed by transcranial magnetic stimulation (TMS) and electroencephalography (EEG).
We plan to administer a low (25 mg) and high (50 mg) dose of talampanel and placebo to normal volunteers and measure various TMS and EEG parameters that we hypothesize may be influenced by AMPA receptor blockade.
Because talampanel is a highly selective AMPA receptor antagonist, we will be able to infer that the parameters that are sensitive to talampanel can be used as empirical assays of AMPA receptor function in humans.
clinicaltrials.gov /ct/show/NCT00057460   (1087 words)

  
 Domain Interactions Regulating AMPA Receptor Desensitization -- Partin 21 (6): 1939 -- Journal of Neuroscience
Glutamate receptors mediate rapid excitatory synaptic transmission in the CNS.
Cotton JLS, Partin KM (2000) The contributions of Glu2 to allosteric modulation of AMPA receptors.
Mano I, Lamed Y, Teichberg VI (1996) A Venus flytrap mechanism for activation and desensitization of AMPA receptors.
www.jneurosci.org /cgi/content/full/21/6/1939   (5027 words)

  
 LP-BM5 virus-infected mice produce activating autoantibodies to the AMPA receptor -- Koustova et al. 107 (6): 737 -- ...
AMPA or IgG in the presence of cyclothiazide dose dependently increased LDH release from granule neurons.
Autoantibodies to glutamate receptor GluR3 in Rasmussen’s encephalitis.
Gahring, L.C., Rogers, S.W., and Twyman, R.E. Antibodies to glutamate receptor subunit GluR2 in nonfamilial olivopontocerebellar degeneration.
www.jci.org /cgi/content/full/107/6/737   (4222 words)

  
 Serotonin 5-HT1A Receptors Regulate AMPA Receptor Channels through Inhibiting Ca2+/Calmodulin-dependent Kinase II in ...
The 5-HT Modulation of AMPA Currents in PFC Neurons Is Dependent on the Inhibition of PKA-- We next examined the signal transduction pathways mediating the modulation of AMPA currents by 5-HT receptors.
5-HT receptors decreased the autophosphorylation of CaMKII and CaMKII phosphorylation of GluR1 subunit in a PP1-dependent manner in PFC slices.
causes the dissociation of AMPA receptors from the anchoring
www.jbc.org /cgi/content/full/277/39/36553   (6879 words)

  
 Functional studies and distribution define a family of transmembrane AMPA receptor regulatory proteins -- Tomita et al. ...
Surface expression of the AMPA receptor subunit GluR2 is dramatically decreased in stg/stg cultures, whereas NMDAR subunits NR2A are not significantly altered.
Localization of AMPA receptors in the hippocampus and cerebellum of the rat using an anti-receptor monoclonal antibody.
Association of AMPA receptors with a subset of glutamate receptor-interacting protein in vivo.
www.jcb.org /cgi/content/full/161/4/805   (6603 words)

  
 Analysis of AMPA Receptor Properties During Postnatal Development of Mouse Hippocampal Astrocytes -- Seifert et al. 78 ...
Receptor desensitization was fitted by a single or a double exponential according to the equation
receptors, the analysis was extended to the cells at P5 and P35.
The Proteoglycan NG2 Is Complexed with alpha -Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptors by the PDZ Glutamate Receptor Interaction Protein (GRIP) in Glial Progenitor Cells.
jn.physiology.org /cgi/content/full/78/6/2916   (4243 words)

  
 IMMUNOHISTOCHEMICAL LOCALIZATION OF AMPA RECEPTOR SUBUNIT 2 IN THE RAT OLFACTORY BULB
One type of ion fluxing glutamate receptor, alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptors seems to play an important role in the regulation of calcium entry.
AMPA receptor subunit 2 (GluR2) regulates the calcium permeability of AMPA receptors.
Electrophysiological, immunoprecipitation, and northern blot data has shown that different types of AMPA receptors are expressed in the brain; however, their specific localization and stoichiometry in the OB is undocumented.
dscholarship.lib.fsu.edu /undergrad/88   (194 words)

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