Carisbamate

Carisbamate is an antiepileptic agent.¹,² In vivo, administration of carisbamate (10-60 mg/kg) dose-dependently reduces spike and wave discharges in the frontoparietal cortex in a rat model of absence seizures.¹ Carisbamate (10 mg/kg) increases latency to the first running episode in the Wistar audiogenic sensitive rat model of convulsive seizures. It also reduces motor seizure frequency in a rat model of spontaneous seizures in a dose-dependent manner.² Carisbamate blocks Na_v1.2 channels (IC₅₀ = 68 μM for rat channels) and inhibits repetitive firing of action potentials in rat hippocampal neurons in a dose-dependent manner.³ It also reduces T-type Ca²⁺ currents in HEK cells transfected with human recombinant Ca_v3.1 channels at a concentration of 300 μM.⁴

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1. François, J., Boehrer, A., and Nehlig, A. Effects of carisbamate (RWJ-333369) in two models of genetically determined generalized epilepsy, the GAERS and the audiogenic Wistar AS. Epilepsia 49(3), 393-399 (2008).

2. Grabenstatter, H.L., and Dudek, F.E. A new potential AED, carisbamate, substantially reduces spontaneous motor seizures in rats with kainate-induced epilepsy. Epilepsia 49(10), 1787-1794 (2008).

3. Liu, Y., Yohrling, G.J., Wang, Y., et al. Carisbamate, a novel neuromodulator, inhibits voltage-gated sodium channels and action potential firing of rat hippocampal neurons. Epilepsy Res. 83(1), 66-72 (2009).

4. Kim, D.Y., Zhang, F.X., Nakanishi, S.T., et al. Carisbamate blockade of T-type voltage-gated calcium channels. Epilepsia 58(4), 617-626 (2017).