Lamotrigine (hydrate)

Lamotrigine hydrate is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine hydrate selectively blocks voltage-gated Na⁺ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine hydrate can be used for the research of epilepsy, focal seizure, et al^[1][2]. In Vitro: Lamotrigine hydrate inhibits Veratrine evoked release of glutamate and aspartate with ED₅₀ values of 21 μM for both amino acids, but Lamotrigine hydrate is less potent in the inhibition of GABA release (ED₅₀=44 μM. At concentrations up to 300 μM, LTG has no effect on patassium-evoked amino acid^[1].
Lamotrigine hydrate is some five times less potent in the inhibition of Veratrine-evoked [³H]acetylcholine release (ED₅₀=100 μM) than in glutamate or aspartate release^[1].
In Vivo: Lamotrigine hydrate (IP, 30 min before pentylenetetrazol; 10 mg/kg, 15 mg/kg or 20 mg/kg) decreases the seizure intensity at the higher doses, it increases the latency to the first pentylenetetrazol-induced seizure in all studied doses compared with the controls^[2].