TABLE 2

Effect of CDPPB on FLIPR agonist concentration-response curves: human and rat mGluR5


Agonist

Control Agonist EC50

EC50 Change at 1 μM CDPPB*
-fold
Human mGluR5a CHO cells
    Glutamate 447 ± 42 nM (3) 9.1
    3,5-DHPG 1.6 ± 0.22 μM (3) 8.7
    Quisqualate 8.9 ± 0.6 nM (3) 2.7
Rat mGluR5 CHO cells
    Glutamate 892 ± 92 nM (3) 6.8
    3,5-DHPG 2.65 ± 0.22 μM (3) 6.0
    Quisqualate
24 ± 0.9 nM (3)
3.9
  • * Calculated from the EC50 values determined by nonlinear curve fitting of the meaned data (see Fig. 3).