TABLE 5

Measured and predicted mGlu5 RO for mavoglurant, dipraglurant, and basimglurant. ub, unbound

CompoundSpeciesDosemGlu5 RO MeasuredmGlu5 RO Predicted from [plasma]ubmGlu5 RO Predicted from [brain]ub
Rat: mg/kg
Human: mg
%
MavoglurantRat345 ± 48564
1073 ± 29586
3083 ± 39895
BasimglurantRatN/A50a4136
Human0.5252730
1.5535156
DipraglurantHuman10027 ± 96643
20044 ± 238060
30054 ± 308569
  • a Quoted EC50 (Lindemann et al., 2015).