Seletracetam lithium bromide

Seletracetam (Ucb 44212) lithium bromide, an analog of the antiepileptic agent Levetiracetam, is a SV2A modulator for the research of epilepsy[1][2][3].

Signaling Pathways >> Others >> Others

Research Areas >> Neurological Disease

IC50: SV2A[1]

Seletracetam displays one-log-unit higher affinity (pKi=7.1) than Levetiracetam (6.1) to the LEV-binding site[2]. Seletracetam lithium bromide inhibits high-voltage-activated Ca2+ currents and intracellular Ca2+ increase in rat cortical neurons in vitro[2]. Seletracetam (1-10 μM) lithium bromide reduces both the amplitude and repetitive firing of population spikes induced by a high K+/low Ca2+ concentration fluid (HKLCF) in rat hippocampal slices[3].

Seletracetam (intraperitoneal injection) lithium bromide displays potent protection against secondary generalised motor seizures in fully corneally-kindled mice (ED50 0.31 mg/kg). In audiogenic seizure susceptible mice, Seletracetam (i.p) protects against clonic convulsion expression with an ED50 of 0.17 mg/kg[3]. Seletracetam (0.0074 mg/kg to 74 mg/kg; intraperitoneal injection) lithium bromide increases the generalized seizure threshold current and decreases the duration of the after-discharge and the seizure severity observed at the after-discharge threshold current, and generally has a much more potent effect than previously observed for Levetiracetam[3]. Animal Model: Female Wistar rats (200-220 g) (Amygdala-kindled rats)[3] Dosage: 0.0074,7.4, 74 mg/kg Administration: Intraperitoneal injection; 60 min before seizure threshold determination Result: Markedly increased the generalized seizure threshold at all doses tested, with increases of 190% (0.0074 mg/kg), 302% (0.074 mg/kg), 429% (0.74 mg/kg), 433% (7.4 mg/kg) and 679% (74 mg/kg).

[1]. Pollard JR, et al. Seletracetam, a small molecule SV2A modulator for the treatment of epilepsy. Curr Opin Investig Drugs. 2008 Jan;9(1):101-7.

[2]. 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 Apr;50(4):702-10.

[3]. Matagne A, et al. Profile of the new pyrrolidone derivative seletracetam (ucb 44212) in animal models of epilepsy. Eur J Pharmacol. 2009;614(1-3):30-37.