| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| L409197-1ml |
1ml |
现货  |
|
| 英文别名 | BW-430C | 6-(2,3-dichlorophenyl)-1,2,4-triazine-3,5-diamine |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Lamotrigine |
| 生化机理 | 拉莫三嗪（BW-430C）是一种新型抗惊厥药物，在人血小板和大鼠脑突触体中抑制 5-HT 的 IC50 值分别为 240 μM 和 474 μM，同时也是一种钠通道阻滞剂。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 封闭剂 |
| 作用机制 | 钠通道α亚基阻断剂 |
| 产品介绍 |
Lamotrigine是一种新型抗惊厥药剂，作用于人类血小板和大鼠脑突触体，抑制5-羟色胺(5-HT)吸收，IC50分别为240 μM和474 μM。A sodium channel protein inhibitor. Information Lamotrigine Lamotrigine (BW-430C) is a novel anticonvulsant drug for inhibition of 5-HT with IC50 of 240 μM and 474 μM in human platelets and rat brain synaptosomes, and also is a sodium channel blocker. 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. In vivo 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. cell lines：Murine cortical neurons and cerebellar granule cells Concentrations： Incubation Time： Powder Purity:≥99% |
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | NC1=NC(=C(N=N1)C2=CC=CC(=C2Cl)Cl)N |
| 分子量 | 256.09 |
| concentration (1mL in DMSO) | 9.0-11.0（mmol/L） |
|---|---|
| NMR Spectrum 1H | Conforms to Structure |
| 1. Rong Wang, Tianfeng Wan, Wenqing Li, Zilin Chen. (2021) Schiff base network-1 incorporated monolithic column for in-tube solid phase microextraction of antiepileptic drugs in human plasma. TALANTA, 226 (122098). [PMID:33676655] [10.1016/j.talanta.2021.122098] |
| 1. Rong Wang, Tianfeng Wan, Wenqing Li, Zilin Chen. (2021) Schiff base network-1 incorporated monolithic column for in-tube solid phase microextraction of antiepileptic drugs in human plasma. TALANTA, 226 (122098). [PMID:33676655] [10.1016/j.talanta.2021.122098] |
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