Levetiracetam (UCB-L059) Levetiracetam (UCB-L059, SIB-S1) is an anticonvulsant medication used to treat epilepsy. Levetiracetam (UCB-L059, SIB-S1) is an agonist of muscarinic acetylcholine receptors (mAChR) . Levetiracetam modulates the presynaptic P/Q- In vitro
Levetiracetam and related compounds bind to SV2A expressed in fibroblasts, indicating that SV2A is sufficient for Levetiracetam binding. Levetiracetam irreversibly inhibits the high-voltage-activated (HVA) calcium current by approximately 18% on the average in freshly isolated CA1 hippocampal neurons of rats. Levetiracetam selectively inhibits N-type Ca2+ channels of CA1 pyramidal hippocampal neurons. Levetiracetam reverses the inhibitory effect of DMCM on GABA-elicited currents in hippocampal neurons.
In vivo
Levetiracetam (17 mg/kg) produces a potent suppression of sound-induced clonic convulsions in mice, and this protective effect is significantly abolished by co-administration of the beta-carboline FG 7142. Levetiracetam exerts potent anticonvulsant activity against both focal and secondarily generalized seizures in fully amygdala-kindled rats, i.e. , a model of temporal lobe epilepsy. Levetiracetam (13 mg/kg, 27 mg/kg or 54 mg/kg, i.p.) dose-dependently suppresses the increase in seizure severity and duration induced by repeated amygdala stimulation. Levetiracetam has a relatively short half-life (about 2-3 hours) in rats. Levetiracetam (5.4 mg/kg to 96 mg/kg i.p.) dose-dependently inhibits both wild running and tonic-clonic convulsions in the audiogenic-seizure prone rat. Levetiracetam markedly suppresses spontaneous spike-and-wave discharge (SWD) but leaves the underlying EEG trace normal in the GAERS model of petit mal epilepsy. Cell Data
