Table 15.
Receptor occupancy and exposures for 203 and 210 in rats
| Entry | mGlu5 IC50 (nM) | mGlu5 Ki (nM) | % RO | plasma levels (nM) | brain levels (nM) | RO50 (mg/kg) |
|---|---|---|---|---|---|---|
| 203 | 28 | 17 | 45 | 2490 | 1290 | > 30 |
| 210 | 16 | 17 | 82 | 1430 | 1100 | 0.9 |
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