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Objective
Brivaracetam (BRV) and levetiracetam (LEV) are antiepileptic drugs that bind synaptic vesicle glycoprotein 2A (SV2A). In vitro and in vivo animal studies suggest faster brain penetration and SV2A occupancy (SO) after dosing with BRV than LEV. We evaluated human brain penetration and SO time course of BRV and LEV at therapeutically relevant doses using the SV2A positron emission tomography...
Despite availability of effective antiepileptic drugs (AEDs), many patients with epilepsy continue to experience refractory seizures and adverse events. Achievement of better seizure control and fewer side effects is key to improving quality of life. This review describes the rationale for the discovery and preclinical profile of brivaracetam (BRV), currently under regulatory review as adjunctive...
ObjectiveThe 6 Hz model of focal seizures has been increasingly used to identify anticonvulsant compounds with potential activity against therapy‐resistant epilepsy, but the protective response to anticonvulsants in this model could be dependent on experimental conditions and selection of mouse strains.
MethodsSeizure thresholds in the 6 Hz model were compared in CF‐1, NMRI, and C57Bl/6J male mice...
Levetiracetam’s (Keppra) binding site and its subsequent identification as the synaptic vesicle protein 2A (SV2A) enabled the discovery of high affinity SV2A ligands with promising anticonvulsant properties. Among these, brivaracetam was selected for further development. SV2A represents an important antiepileptic drug target validated in both preclinical and clinical studies. For an expanded treatment...
Levetiracetam (Keppra ® ) is a new generation antiepileptic drug characterized by a unique profile of activity in experimental models of epilepsy. It also has a distinct binding site in the brain, i.e. the synaptic vesicle protein type 2 (SV2A). Levetiracetam has been reported to have antiepileptogenic and disease-modifying properties. In the present study the effects of chronic treatment...
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