Lamotrigine
作者：齐岳
发布时间：2023-09-13
17:22:07
点击数：
产品名称：Lamotrigine
产品描述：
| 产品描述 | Lamotrigine is an Anti-epileptic Agent and Mood Stabilizer. The physiologic effect of lamotrigine is by means of Decreased Central Nervous System Disorganized Electrical Activity. |
| 靶点活性 | 5-HT (rat brain synaptosomes):474 μM, 5-HT (human platelets):240 μM |
| 体外活性 | 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. |
| 体内活性 | 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。 |
| 激酶实验 | 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 |
| 别名 | BW430C, 拉莫三嗪, LTG |
| 分子量 | 256.09 |
| 分子式 | C9H7Cl2N5 |
| CAS No. | 84057-84-1 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 25.6 mg/mL (100 mM)
Ethanol: 2.6 mg/mL (10 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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