Molecular structure and pharmacological characterization of humEAA2, a novel human kainate receptor subunit

Abstract

A cDNA encoding a novel human glutamate receptor subunit protein was isolated from a human hippocampal library. This cDNA, termed humEAA2, is most closely related to rat cDNAs for kainate receptor proteins and, when expressed in COS cells, is associated with high affinity kainate receptor binding. The relative potency of compounds in displacing [3H]kainate binding was kainate > quisqualate > domoate > L-glutamate ≫ 6,7-dinitroquinoxaline-2,3-dione > dihydrokainate > 6-cyano-7-nitroquinoxaline-2,3-dione > (RS)-α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid. Homomeric expression of humEAA2 does not appear to elicit ligand-gated channel activity. Nevertheless, the molecular structure and ..