Like lamotrigine, both GSK2 and GSK3 were able to prevent the deficit in reversal learning produced by PCP, thus confirming their potential in the treatment of cognitive symptoms of schizophrenia. However, higher doses than those required for anticonvulsant efficacy of the drugs were needed for activity in the reversal-learning model, suggesting a lower therapeutic window relative to mechanism-dependent central side effects for this indication. CNV1014802 received orphan-drug designation from the US Food and Drug Administration in July 2013.
| Cell Experiment | |
|---|---|
| Cell lines | HEK cells |
| Preparation method | Activity of CNV1014802 was assessed in HEK cells heterologously expressing NaV1.1–NaV1.8 using FLIPR membrane potential assays. |
| Concentrations | 1 mM |
| Incubation time | 5 minutes |
| Animal Experiment | |
|---|---|
| Animal models | adult male C57BL/6J mice |
| Formulation | phosphate-buffered saline/10% DMSO |
| Dosages | 30 mg/kg |
| Administration | i.v. |
| Molecular Weight | 314.35 |
| Formula | C18H19FN2O2 |
| CAS Number | 934240-30-9 |
| Solubility (25°C) | 10 mM in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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