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 lines||HEK cells|
|Preparation method||Activity of CNV1014802 was assessed in HEK cells heterologously expressing NaV1.1–NaV1.8 using FLIPR membrane potential assays.|
|Incubation time||5 minutes|
|Animal models||adult male C57BL/6J mice|
|Formulation||phosphate-buffered saline/10% DMSO|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||10 mM in DMSO|
Analgesic Effects of GpTx-1, PF-04856264 and CNV1014802 in a Mouse Model of NaV1.7-Mediated Pain.
Deuis JR, et al. Toxins (Basel). 2016 Mar 17;8(3). pii: E78. PMID: 26999206.
Novel design for a phase IIa placebo-controlled, double-blind randomized withdrawal study to evaluate the safety and efficacy of CNV1014802 in patients with trigeminal neuralgia.
Zakrzewska JM, et al. Trials. 2013 Nov 23;14:402. PMID: 24267010.
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