Nav1.2 Ki | Electroshock | Reversal Learning | Motor Behavior | ||||||||
---|---|---|---|---|---|---|---|---|---|---|---|
Med | Route | Free Plasma | Med | Route | Free Plasma | NOAEL | Route | Free Plasma | Electroshock | ||
mg/kg | ng/ml | mg/kg | ng/ml | mg/kg | ng/ml | fold | |||||
GSK2 | 1.6 | 3 | Subcutaneous | 54 | 60 | Oral | 786a | 60 | Oral | 786 | 14.6 |
GSK3 | 0.9 | 2 | Subcutaneous | 40 | 30 | Oral | 175a | <30b | Subcutaneous | 325 | <8.1 |
Lamotrigine | 24 | 3 | Oral | 930 | 25 | Intraperitoneal | 3470a | <3b | Oral | 675 | <0.7 |
Ki, affinity for the inactivated state of human recombinant Nav1.2 channels; Med, minimal statistically significant effect; NOAEL, no adverse event limit (the highest dose tested that did not impair behavior in the test).
↵a Data extrapolated from independent pharmacokinetic studies using the same route of administration.
↵b Significant effect at this dose on vertical activity; no effect on horizontal activity.