TABLE 1

Selectivity profile of GLUK5 ligands Functional and receptor binding assays were performed as described under Materials and Methods. Results are means ± S.E.M. from at least three separate determinations.


Compound

GLUK5 IC50a

GLUK6 IC50a

[3H]ATPA Kib

[3H]Kainate Kib
μM
ATPA 0.21 ± 0.03 >300 0.0094 ± 0.0010 >100
NS1209 0.63 ± 0.09 65 ± 4 0.62 ± 0.11 13 ± 4.0
NS3763
1.6 ± 0.2
>30
>30
>30
  • a Functional selectivity at recombinant homomeric GLUK5 and homomeric GLUK6 receptors expressed in HEK293 cells, determined by measurements of intracellular calcium. IC50 values were calculated from percentage of inhibition of domoate-induced calcium influx

  • b Selectivity in ligand binding assays to homomeric GLUK5 and homomeric GLUK6 receptors expressed in HEK293 cells. Ki values for NS1209 are from Varming et al. (2001)