TABLE 1

Affinities of CDPPB analogs at the allosteric mGluR5 antagonist MPEP binding site obtained from [3H]methoxyPEPy competition binding using membrane prep from the rmGluR5 stable cell line and their potencies as allosteric mGluR5 potentiators from glutamate-induced calcium release in cultured rat cortical astrocytes

Data are average ± S.E.M. from three or four independent experiments in duplicate.




Ki

EC50
nM
CDPPB 1340 ± 233 44.8 ± 20.8
VU-20 3800 ± 854 175 ± 46.4
VU-21 1400 ± 428 87.1 ± 22.2
VU-22 1310 ± 162 228 ± 39
VU-23 604 ± 180 41.4 ± 17.8
VU-24 606 ± 263 26.2 ± 9.4
VU-28 920 ± 362 46.5 ± 18.6
VU-29 244 ± 90 9.0 ± 1.5
VU-35 287 ± 64 16.9 ± 6.2
VU-36
94.9 ± 41
10.6 ± 3.0