The AMPA receptor bound to a glutamate antagonist showing the amino terminal, ligand binding, and transmembrane domain, PDB 3KG2
The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (also known as AMPA receptor, AMPAR, or quisqualate receptor) is an ionotropic transmembrane receptor for glutamate (iGluR) and predominantly Na+ ion channel that mediates fast synaptic transmission in the central nervous system (CNS). It has been traditionally classified as a non-NMDA-type receptor, along with the kainate receptor. Its name is derived from its ability to be activated by the artificial glutamate analog AMPA. The receptor was first named the "quisqualate receptor" by Watkins and colleagues after a naturally occurring agonist quisqualate and was only later given the label "AMPA receptor" after the selective agonist developed by Tage Honore and colleagues at the Royal Danish School of Pharmacy in Copenhagen.[1] The GRIA2-encoded AMPA receptor ligand binding core (GluA2 LBD) was the first glutamate receptor ion channel domain to be crystallized.[2]
^Honoré T, Lauridsen J, Krogsgaard-Larsen P (January 1982). "The binding of [3H]AMPA, a structural analogue of glutamic acid, to rat brain membranes". Journal of Neurochemistry. 38 (1): 173–8. doi:10.1111/j.1471-4159.1982.tb10868.x. PMID 6125564. S2CID 42753770.
^Armstrong N (2000). "Armstrong and Gouaux (2000) Mechanisms for Activation and Antagonism of an AMPA-Sensitive Glutamate Receptor: Crystal Structures of the GluR2 Ligand Binding Core". Neuron. 28 (1): 165–181. doi:10.1016/S0896-6273(00)00094-5. PMID 11086992. S2CID 3128719.
protein receptors such as NMDA and AMPAreceptors. Post-synaptic AMPAreceptor: AMPAReceptors are trans-membrane protein ionotropic receptors that open...
Ampakines or AMPAkines are a subgroup of AMPAreceptor positive allosteric modulators with a benzamide or closely related chemical structure. They are...
non-NMDA-type receptor, along with the AMPAreceptor. KARs are less understood than AMPA and NMDA receptors, the other ionotropic glutamate receptors. Postsynaptic...
Glutamate ionotropic receptorAMPA type subunit 2 (Glutamate receptor 2, or GluR-2) is a protein that in humans is encoded by the GRIA2 (or GLUR2) gene...
in excessive stimulation of receptors. For example, when glutamate receptors such as the NMDA receptor or AMPAreceptor encounter excessive levels of...
AMPAreceptor positive allosteric modulators are positive allosteric modulators (PAMs) of the AMPAreceptor (AMPR), a type of ionotropic glutamate receptor...
impermeable in over 99% of AMPAreceptors. Like AMPAreceptors, kainate receptors are tetrameric, transmembrane, ionotropic glutamate receptors on glutamatergic...
antiepileptic drug in the class of selective non-competitive antagonist of AMPAreceptors. The drug label has a black box warning that the drug may cause serious...
neurotransmitters receptors pre-mRNa are substrates for ADARs. This includes 5 subunits of the glutamate receptor ionotropic AMPA glutamate receptor subunits (Glur2...
NMDA-type glutamate receptors but no AMPA-type glutamate receptors. These synapses are named "silent" because normal AMPAreceptor-mediated signaling is...
activation of the AMPAreceptor. Overall signal can be increased by preventing the desensitization of a receptor. Desensitization prevents a receptor from activating...
delivery to the postsynaptic cell in inducing LTP is more complicated. The AMPAreceptor (AMPAR) is the engine that drives excitatory postsynaptic potentials...
this receptor. In addition to this GABAergic effect, barbiturates also block AMPA and kainate receptors, subtypes of ionotropic glutamate receptor. Glutamate...
ionotropic glutamate receptor antagonist, which is a non-competitive AMPAreceptor antagonist (IC50 values are 10-20, ~ 450 and >> 50 μM for AMPA-, kainate- and...
sedative or stimulant. Piracetam is a positive allosteric modulator of the AMPAreceptor, although this action is very weak and its clinical effects may not...
metabotropic glutamate receptors. It is inactive at group III mGluRs. Ibotenic acid also acts as a weak agonist of the AMPA and kainate receptors. In addition,...
modulators of the AMPAreceptor. Racetams are understood to work by allosterically modulating glutamate receptors, specifically AMPAreceptors, leading to Ca2+...
glutamate receptors, such as NMDA (N-methyl-D-aspartate), AMPA (α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid), and kainate receptors, have distinct...
that increases synaptic capacity for AMPAreceptors. This is what leads to a long-term increase in AMPAreceptors and thus synaptic strength and plasticity...
neurotransmitter receptors, are highly mobile in the plasma membrane due to lateral diffusion. Fast movements of AMPA-type glutamate receptors (AMPARs) are...
endogenous AMPAreceptor ligand is glutamate and ampakines mirror glutamate's interaction with the receptors. Ligand binding causes AMPAreceptors to open...
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