Levetiracetam Inhibitor CAS No. 102767-28-2

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KI0699	Levetiracetam	50 mg	$154

Chemical Characteristic

Product Name	Levetiracetam
Synonyms	Keppra, UCB L059
CAS No.	102767-28-2
Molecular Weight	170.21
Formula	C₈H₁₄N₂O₂
Chemical Structure

Biological activities

Levetiracetam is an anticonvulsant and antiepileptic agent. Levetiracetam is the S-enantiomer of etiracetam. Levetiracetam dose-dependently reduces the [Ca²⁺]_{ι increase. In rat hippocampal pyramidal neurons, levetiracetam inhibits HVACC by a specific blockade of N-type Ca²⁺ channels. Levetiracetam similarly inhibits caffeine-induced [Ca²⁺]_{ι transients and epileptiform potentials in hippocampal neurons. In rat neocortical neurons, levetiracetam concomitantly decreases the epileptiform paroxysmal depolarizing shifts (PDSs) and the associated [Ca²⁺]_{ι increases, by inhibiting HVACCs, preferentially the N-type channels, and partially the P/Q-type channels.^[1] Levetiracetam decreases reactive gliosis and expression levels of IL-1β system in the hippocampus and the piriform cortex.^[2] Levetiracetam binds to a synaptic vesicle glycoprotein, synaptic vesicle protein 2A (SV2A).^[3] Levetiracetam is binding to SV2A in human recombinant SV2A expressed in CHO cells in vitro.^[4] In vitro, levetiracetam also inhibits Na⁺-dependent Cl^-/HCO3^- exchange of adult hippocampal CA3 neurons from guinea-pigs.^[5] Intraperitoneal (i.p.) administration of levetiracetam at the doses of 2.5閳?0 mg/kg dose-dependently decreases DBA/2 audiogenic seizure severity score. Levetiracetam produces an additive anticonvulsant effect when administered in combination with some classical anticonvulsants, most notably carbamazepine, diazepam.^[6] Levetiracetam dose-dependently protects against different seizure parameters in fully amygdala-kindled rats by significantly reducing seizure severity and after discharge duration.^[7] Levetiracetam decreases the size of NMDA-bursts to the same extent as the size of synaptically evoked bicuculline-bursts but has little effect on bursting frequency.^[8] Levetiracetam has no significant γ-aminobutyric acid-related effect on paired-pulse interaction in the dentate gyrus of rats.^[9] Levetiracetam has ED50 values generally within the range of 5.0-30.0 mg/kg, in inhibiting audiogenic seizures, electrically induced convulsions and convulsions induced chemically by pentylenetetrazole (PTZ), bicuculline, picrotoxin and N-methyl-D-aspartate (NMDA). Levetiracetam retards the development of PTZ-induced kindling in mice and reduces PTZ-induced EEG spike wave discharge in rats.[10] Levetiracetam administration also reduces spontaneous recurrent seizures in the rat pilocarpine model of temporal lobe epilepsy.^[11] In 4-aminopyridine-treated slices from adult guinea-pigs, levetiracetam (10-100 µM) reduces the frequency of action potentials and epileptiform bursts of CA3 neurons by 30-55%.^[5] Furthermore, levetiracetam treatment (54 mg/kg) also normalises chlordiazepoxide withdrawal-induced anxiety in mice.^[12]}}}

Protocols

In vivo: Levetiracetam is dissolved in saline.^[9]

References

[1] Martella G, et al. Seletracetam (ucb 44212) inhibits high-voltage-activated Ca²⁺ currents and intracellular Ca²⁺ increase in rat cortical neurons in vitro. Epilepsia. 2009, 50(4): 702-710. 閵嗏偓閵嗏偓 [2] Kim JE, et al. Levetiracetam inhibits interleukin-1 beta inflammatory responses in the hippocampus and piriform cortex of epileptic rats. Neurosci Lett. 2010, 471(2): 94-99. 閵嗏偓閵嗏偓 [3] Lynch BA, et al. The synaptic vesicle protein SV2A is the binding site for the antiepileptic drug levetiracetam. Proc Natl Acad Sci U S A. 2004, 101(26): 9861-9866. 閵嗏偓閵嗏偓 [4] Gillard M, et al. Binding characteristics of levetiracetam to synaptic vesicle protein 2A (SV2A) in human brain and in CHO cells expressing the human recombinant protein. Eur J Pharmacol. 2006, 536(1-2): 102-108. [5] Leniger T, et al. Levetiracetam inhibits Na⁺-dependent Cl-/HCO3- exchange of adult hippocampal CA3 neurons from guinea-pigs. Br J Pharmacol. 2004, 142(7): 1073-1080. 閵嗏偓閵嗏偓 [6] Donato Di Paola E, et al. Influence of levetiracetam on the anticonvulsant efficacy of conventional antiepileptic drugs against audiogenic seizures in DBA/2 mice. Epilepsy Res. 2007, 75(2-3): 112-121. 閵嗏偓閵嗏偓 [7] Klitgaard H. Levetiracetam: the preclinical profile of a new class of antiepileptic drugs? Epilepsia. 2001, 42(Suppl 4):13-18. 閵嗏偓閵嗏偓 [8] Birnstiel S, et al. Levetiracetam (ucb LO59) affects in vitro models of epilepsy in CA3 pyramidal neurons without altering normal synaptic transmission. Naunyn Schmiedebergs Arch Pharmacol. 1997, 356(5): 611-618. 閵嗏偓閵嗏偓 [9] Margineanu DG, et al. Levetiracetam has no significant gamma-aminobutyric acid-related effect on paired-pulse interaction in the dentate gyrus of rats. Eur J Pharmacol. 2003, 466(3): 255-261. 閵嗏偓閵嗏偓 [10] Gower AJ, et al. ucb L059, a novel anti-convulsant drug: pharmacological profile in animals. Eur J Pharmacol. 1992, 222(2-3): 193-203. [11] Glien M, et al. Effects of the novel antiepileptic drug levetiracetam on spontaneous recurrent seizures in the rat pilocarpine model of temporal lobe epilepsy. Epilepsia. 2002, 43(4): 350-357. [12] Lamberty Y, et al. The new antiepileptic drug levetiracetam normalises chlordiazepoxide withdrawal-induced anxiety in mice. Eur J Pharmacol. 2002, 439(1-3): 101-106.

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