PMID: 9166736Jun 1, 1997Paper

Stable expression of recombinant AMPA receptor subunits: binding affinities and effects of allosteric modulators

Journal of Neurochemistry
M HennegriffG Lynch

Abstract

Homomeric AMPA (alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid)-type glutamate receptors (GluRs) were stably expressed in kidney cells from cDNAs encoding GluR1 flop, GluR2 flip, GluR2 flop, and GluR3 flop subunits. The recombinant receptors were of the expected size and showed functional properties in whole-cell recording as previously reported. [3H]AMPA binding to all subunits was increased to a similar extent by the chaotropic ion thiocyanate (SCN-). Significant differences were found in the Scatchard plots, however, which were linear and of high affinity for GluR1 and -3 receptors (K(D) values of 33 and 52 nM, respectively) but showed curvature for GluR2 receptors, indicating the presence of two components with distinct affinities. As with brain AMPA receptors, solubilization of GluR2 receptors reduced the number of lower-affinity sites and correspondingly increased the number of higher-affinity sites. The sulfhydryl reagent p-chloromercuriphenylsulfonic acid, which increases binding to brain receptors, produced only minor changes except in the case of GluR2 flip. These results indicate that GluR2, among the subunits examined here, most closely resembles the native AMPA receptors in brain membranes. [3H]AMPA bindi...Continue Reading

Citations

Nov 20, 2002·The Journal of Pharmacology and Experimental Therapeutics·Amy C AraiMarkus Kessler
Feb 26, 2005·Psychopharmacology·James N C Kew, John A Kemp
Feb 14, 2006·Proceedings of the National Academy of Sciences of the United States of America·Sergio FucileFabrizio Eusebi
May 1, 1999·Natural Toxins·D R Hampson, J L Manalo
Mar 27, 2003·The Journal of Biological Chemistry·Dustin DemingVasanthi Jayaraman
Aug 19, 2010·Pharmacological Reviews·Stephen F TraynelisRay Dingledine
Jan 27, 2004·Journal of Neuroscience Research·Linda M ChicoineBen A Bahr
Jan 28, 2005·The European Journal of Neuroscience·Francesco FornaiKaren Gale
Dec 16, 1998·European Journal of Pharmacology·B S NielsenD S Pickering
May 3, 2003·Pharmacology & Therapeutics·C Allison, J A Pratt

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