AMPA receptor

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]

  1. ^ 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.
  2. ^ 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.

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