Lamotrigine (BW430C) is an Anti-epileptic Agent and Mood Stabilizer. The physiologic effect of lamotrigine is by means of Decreased Central Nervous System Disorganized Electrical Activity.

5-HT (rat brain synaptosomes):474 μM, 5-HT (human platelets):240 μM

Lamotrigine在电诱发的EEG后放电测试中是活跃的,这表明其能够抵抗简单和复杂的部分性发作.Lamotrigine在小鼠和大鼠体内具有抗癫痫作用,防止MES和戊四氮诱导的后肢伸展.Lamotrigine给药后1小时这些作用达到最大值,并且能够持续超过24小时.静脉内给大鼠>5 mg/kg Lamotrigine,后放电持续时间剂量依赖性减少.

用10 mg/L藜芦碱培育的大鼠大脑皮层组织,Lamotrigine抑制谷氨酸和天冬氨酸(两者ED 50 = 5.38 mg/L)的释放,比抑制GABA (ED50 = 11.2 mg/L)的释放有效两倍。基础谷氨酸的释放不受影响。Lamotrigine通过阻断电压依赖性钠通道稳定突触前神经元膜,从而防止兴奋性神经递质尤其是谷氨酸和天冬氨酸的释放。 Lamotrigine不会诱导PCP样中枢神经系统效应,不会通过直接抑制NMDA受体发挥作用,并可能导致与NMDA阻断相关的不良效应缺乏。

Whole Cell [3H]R1881 Binding Assay: Fibroblasts are grown to confluence in five or six 150 cm2 tissue culture flasks for routine assay. This usually requires 4-6 weeks from the time of the initial seeding of the cell line. All studies are performed between passages 3-20. Two days before assay, the medium is changed to one lacking fetal calf serum. This is repeated again 24 hours before assay. Competition assays are performed with 0.5-1.0 nM [3H]R1881 and increasing amounts of the nonradioactive compounds. Binding to low affinity sites is determined in the presence of 5 × 10-7 M R1881 and is subtracted from whole cell binding of [3H]R 1881 obtained in the absence of any inhibitor to assess binding to 5 high affinity site