Stable expression of homomeric AMPA-selective glutamate receptors in BHK cells

Eur J Pharmacol. 1996 Sep 5;311(1):95-100. doi: 10.1016/0014-2999(96)00399-8.

Abstract

cDNAs encoding glutamate receptor glu1, glu2 (Q and R) or glu4 under control of a constitutively active metallothionine promoter, were transfected into baby hamster kidney cells. Following the addition of selection agent, transfectants expressing high levels of glutamate receptor as measured by [3H]alpha-amino-3-hydroxyl-5-methyl-isoxalazole-4-propionate (AMPA) binding, were selected for further studies. Using glutamate receptor antibodies, the receptor proteins were visualized in Western blotting as having a molecular weight of approximately 100 kDa. [3H]AMPA binding to the glutamate receptor expressing cell lines revealed that glu1, glu2 (Q), and glu4 receptors displayed a single site in Scatchard analysis with Kd values of 12, 15.7 and 21 nM, respectively. However, the Ca2+ impermeable variant of the glu2 receptor, glu2 (R) displayed a curvilinear Scatchard plot. Computer resolution suggested the presence of a high and low affinity state (KH = 2.9 nM; KL = 40.7 nM). The pharmacological profile of the [3H]AMPA binding to these recombinant receptors resembled the high affinity [3H]AMPA binding site in rat brain showing high affinity for glutamate, quisqualate, and medium affinity for 6-cyano-7-nitro-quinoxaline-2,3-dione, CNQX; 6,7-dinitro-quinoxaline-2,3-dione, DNQX; and 6-nitro-7-sulphanyl-benzo(f)quinoxaline-2,3,dione, NBQX. Kainate displayed low affinity and N-methyl-D-aspartate (NMDA), was inactive in inhibiting specific [3H]AMPA binding. These cell lines will prove to be important tools in the study of glutamate receptors.

MeSH terms

  • Animals
  • Blotting, Western
  • Cell Line
  • Cell Membrane / metabolism
  • Cricetinae
  • DNA / biosynthesis
  • Kidney / metabolism
  • Ligands
  • Molecular Weight
  • Polymerase Chain Reaction
  • Proteins / metabolism
  • Rats
  • Receptors, AMPA / drug effects*
  • alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid / metabolism*

Substances

  • Ligands
  • Proteins
  • Receptors, AMPA
  • alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid
  • DNA