194085-75-1

Carisbamate is an antiepileptic agent., 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. 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. 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. It also reduces T-type Ca²⁺ currents in HEK cells transfected with human recombinant Ca_v3.1 channels at a concentration of 300 μM.

Carisbamate is being developed for adjuvant treatment of partial onset epilepsy. Carisbamate produces anticonvulsant effects in primary generalized, complex partial and absence-type seizure models, an d exhibits neuroprotective and antiepileptogenic properties in rodent epilepsy models.

Carisbamate is being developed for adjuvant treatment of partial onset epilepsy. Carisbamate produces anticonvulsant effects in primary generalized, complex partial and absence-type seizure models, and exhibits neuroprotective and antiepileptogenic properties in rodent epilepsy models.

Labelled Carisbamate; it is being developed for adjuvant treatment of partial onset epilepsy. Carisbamate produces anticonvulsant effects in primary generalized, complex partial and absence-type seizu re models, and exhibits neuroprotective and antiepileptogenic properties in rodent epilepsy models.

ChEBI: Carisbamate is an organochlorine compound.

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[1] JENNIFER FRAN?OIS  Astrid N  Any Boehrer. Effects of Carisbamate (RWJ-333369) in Two Models of Genetically Determined Generalized Epilepsy, the GAERS and the Audiogenic Wistar AS[J]. Epilepsia, 2007, 49 3: 393-399. DOI: 10.1111/j.1528-1167.2007.01278.x
[2] HEIDI L. GRABENSTATTER  F. E D. A new potential AED, carisbamate, substantially reduces spontaneous motor seizures in rats with kainate-induced epilepsy[J]. Epilepsia, 2008, 49 10: 1787-1794. DOI: 10.1111/j.1528-1167.2008.01657.x
[3] YI LIU . Carisbamate, a novel neuromodulator, inhibits voltage-gated sodium channels and action potential firing of rat hippocampal neurons[J]. Epilepsy Research, 2009, 83 1: Pages 66-72. DOI: 10.1016/j.eplepsyres.2008.09.006
[4] DO YOUNG KIM. Carisbamate blockade of T-type voltage-gated calcium channels[J]. Epilepsia, 2017, 58 4: 617-626. DOI: 10.1111/epi.13710