生物活性

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.

化学数据

不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的K_m系数（3），再除以大鼠的K_m系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。

储备液配制

以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。