Table 1

Comparison of affinity for the [3H]CP-526,427 binding site and potency for inhibition of a functional AMPA receptor mediated response. IC50 values were determined for inhibition of binding of 3 nM [3H]CP-526,427 binding to rat forebrain membranes (Binding IC50) and for inhibition of 45Ca2+uptake in primary cultures of rat cerebellar granule neurons induced by 100 μM kainate (Functional IC50) as described underMaterials and Methods.

CompoundBinding IC50(μM)nFunctional IC50(μM)n
CP-526,4270.0031-a 40.005  ± 0.0018
CP-465,0220.025  ± 0.01460.039  ± 0.0033
CP-465,021>103>33
CP-471,2360.057  ± 0.0830.028  ± 0.0036
CP-471,237>1042.7  ± 0.163
GYKI-52,46612.6  ± 1.24221
  • n, number of experiments.

  • 1-a K d.