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抑制剂描述:

产品名称:Lamotrigine

产品别名:见爱必信官网

英文别名:Lamotrigine

靶点:Sodium Channel

CAS:84057-84-1

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

Lamotrigine is a novel anticonvulsant drug for inhibition of 5-hydroxytryptamine (5-HT) uptake in both human platelets and rat brain synaptosomes with IC50 of 240 μM and 474 μM, respectively. Lamotrigine inhibits the synaptosomal uptake of noradrenaline and dopamine with IC50 of 239 μM and 322 μM, respectively. Lamotrigine is believed to mediate its anticonvulsant activity by the use- and voltage-dependent blockade of Na+ channels. Lamotrigine may also be useful in the treatment of bipolar illness with efficacy against depressive breakthroughs and rapid cycling bipolar disorder. The reduction in the uptake of label caused by 1 mM lamotrigine incubated in the presence of 10 nM 5-HT is reversed by increasing the substrate concentration 10-fold. The inhibition of the p-chloroamphetamine-induced 5-HT syndrome in rats suggests that lamotrigine also inhibits 5-HT uptake. Lamotrigine is a new generation broad-spectrum anticonvulsant.

溶解性:Ethanol :2.6 mg/mL (10 mM)
DMSO :25.6 mg/mL (100 mM)

体外研究:

Lamotrigine stabilises presynaptic neuronal membranes by blockade of voltage-dependent sodium channels, thus preventing the release of excitatory neurotransmitters, particularly glutamate and aspartate. In rat cerebral cortex tissue incubated with veratrine 10 mg/L, lamotrigine is twice as potent in inhibiting the release of glutamate and aspartate (ED 50 = 5.38 mg/L for each) than the release of GABA (ED50 = 11.2 mg/L), and is much less potent in inhibiting acetylcholine release (ED50 = 25.6 mg/L) when cortical slices is exposed to veratrine 75 mg/L. Basal glutamate release is unaffected . Lamotrigine inhibits high-frequency sustained repetitive firing of sodium-dependent action potentials, indicating a direct effect on voltage-activated sodium channels. Lamotrigine does not induce PCP-like central nervous system (CNS) effects, does not act by direct inhibition at the NMDA receptor, and would be expected to be devoid of the undesirable effects associated with NMDA blockade.

体内研究:In mice and rats, lamotrigine prevents MES- and pentetrazol-induced hindlimb extension, suggesting an antiepileptic profile in animals. These effects peak 1 hour after lamotrigine administration and persist for more than 24 hours. Lamotrigine is active in the electrically evoked EEG after-discharge test, which is thought to indicate activity against both simple and complex partial seizures. After-discharge duration is reduced dose-dependently by lamotrigine in rats at intravenous doses >5 mg/kg.

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