Compound | Species | Dose | mGlu5 RO Measured | mGlu5 RO Predicted from [plasma]ub | mGlu5 RO Predicted from [brain]ub |
---|---|---|---|---|---|
Rat: mg/kg Human: mg | % | ||||
Mavoglurant | Rat | 3 | 45 ± 4 | 85 | 64 |
10 | 73 ± 2 | 95 | 86 | ||
30 | 83 ± 3 | 98 | 95 | ||
Basimglurant | Rat | N/A | 50a | 41 | 36 |
Human | 0.5 | 25 | 27 | 30 | |
1.5 | 53 | 51 | 56 | ||
Dipraglurant | Human | 100 | 27 ± 9 | 66 | 43 |
200 | 44 ± 23 | 80 | 60 | ||
300 | 54 ± 30 | 85 | 69 |
↵a Quoted EC50 (Lindemann et al., 2015).