| Description |
Carisbamate (RWJ-333369) is an orally active neuromodulator. Carisbamate prevents the development and production of epilep-like discharges and has a neuroprotective effect after in vitro epilepticus-like injury. Carisbamate has good antiepileptic activity in genetic models of generalized and nonconvulsive epilepsy[1][2][3].
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| Related Catalog |
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| In Vitro |
Carisbamate (200 µM; 12 h) exhibits antiepileptic effects on SREDs model of hippocampal cells[1]. Carisbamate (200 µM; 24 h) shows long lasting effects on the hippocampal neurons that are independent from antiepileptic effects in vitro[1]. Carisbamate not only inhibits the development and expression of SREDs in the majority of neurons, but also decreases seizure frequency and duration in the few neurons that still has an occasional epileptiform event[1]. Carisbamate (200 µM) shows neuroprotective effects on hippocampal cells with SE (status epilepticus)-like injury[1]. Cell Viability Assay[1] Cell Line: Hippocampal cells (from 2-day postnatal Sprague-Dawley rat; spontaneous recurrent epileptiform discharges (SREDs) model) Concentration: 200 µM Incubation Time: 12 h Result: Acutely inhibited SREDs with greater than 95% of the neurons exhibited an in vitro antiepileptic effect. Cell Viability Assay[1] Cell Line: Hippocampal cells (SREDs model) Concentration: 200 µM Incubation Time: 24 h Result: Exhibited cells evaluated the day after treatment were still free of in vitro seizure activity and did not develop SREDs.
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| In Vivo |
Carisbamate (10, 30, 60 mg/kg; i.p.; single) dose dependently reduces the expression of spike-and-wave discharges (SWD) in absence seizures rat model[2]. Carisbamate (20, 30 mg/kg; i.p.; single) shows no wild running episode or tonic seizure occurres in any of the rats tested[2]. Animal Model: Male genetic absence epilepsy rat (absence seizures model)[2]. Dosage: 10, 30, 60 mg/kg Administration: Intraperitoneal injection; single. Result: Completely inhibited SWD when at 60 mg/kg after 120 min, and restored the duration of SWD to the control level when at 30 mg/kg after 100 min. Animal Model: Male Wistar audiogenic sensitive rat (convulsive seizures model)[2]. Dosage: 10, 20, 30 mg/kg Administration: Intraperitoneal injection; single. Result: Showed no wild running episode or tonic seizure occurred in any of the rats tested when at 20 and 30 mg/kg. Increased by 327% the latency to the tonic seizure that still occurred in the six of eight rats studied when at 10 mg/kg.
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