Table 1.
Effect of prototype compounds in mouse models of seizure and chronic network hyperexcitability. Effective doses are listed where calculated (mg/kg)
| Generic name | ASP ID # | Mouse I.P identification | Mouse P.O. identification | Mouse I.P. quantification | Mouse P.O. quantification | Mouse CKM (I.P.) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| MES | 44 mA | TOX | MES | 44 mA | TOX | MES (ED50) | 44 mA (ED50) | TOX (TD50) | MES (ED50) | 44 mA (ED50) | TOX (TD50) | ID | Quant | ||
| Acetaminophen | 490002 | − | − | − | − | − | − | NT | NT | NT | NT | NT | NT | + | >450 |
| Carbamazepine | 490003 | + | + | + | + | + | + | 8.38 | 31.4 | 45.6 | 11.35 | 63.7 | 95.4 | + | 6.42 |
| Levetiracetam | 490004 | − | + | − | − | + | − | NT | >1500 | >1500 | NT | >500 | >500 | + | Inc |
| Retigabine | 490005 | + | + | - | + | + | + | 25.7 | 32.5 | 129 | 57.0 | 75.1 | >500 | + | 13.65 |
| Clobazam* | 490006 | + | + | + | + | + | − | 16.5 | 4.5 | 26.1 | 29.9 | 6.99 | 196.7 | + | 2.53 |
| Tiagabine* | 490007 | − | + | − | − | + | − | NT | 1.03 | 5.84 | NT | 1.87 | 33.2 | NT | NT |
| N6-Cyclopentyladenosine | 490008 | + | + | + | + | + | + | 1.01 | 0.19 | 0.94 | 4.43 | 1.36 | 6.94 | − | NT |
| m-CPP | 490009 | − | − | + | − | − | − | >60 | >55 | 52.6 | NT | NT | NT | − | NC |
| Valproic acid | 490010 | - | + | − | − | − | − | >60 | 239.2 | >300 | >300 | >300 | <300 | + | 94.02 |
NT Not Tested due to inactivity in screen
NC ED50 Could Not Be Calculated
(+) Effect observed at at least one dose and time point tested
(−) No effect observed at any dose and time point tested
Inc. Incomplete, testing started but not completed
*
Starting doses reduced from default