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Lamotrigine

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Chemical Structure| 84057-84-1 同义名 : LTG;BW430C;Lamotrigine, Lamictal, BW-430C, Crisomet, Lamictin, Lamitor
CAS号 : 84057-84-1
货号 : A551325
分子式 : C9H7Cl2N5
纯度 : 98%
分子量 : 256.091
MDL号 : MFCD00865333
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(97.62 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • 5-HT

    5-HT (rat brain synaptosomes), IC50:474 μM

    5-HT (human platelets), IC50:240 μM

  • Sodium Channel
描述 Lamotrigine belongs to the second generation of antiepileptic drugs (AEDs)[3]. Co-application of lamotrigine (1 ~ 300 µM) resulted in a concentration-dependent reduction in peak amplitude of currents induced by 3 µM of 5-HT for an IC50 value of 28.2 ± 3.6 µM with a Hill coefficient of 1.2 ± 0.1[4]. Moreover, intrathecally administered lamotrigine could prevent the activation of the glutamate receptors involved in pain transmission and central sensitization, such as AMPA, NMDA, and metabotropic receptors[5]. Studies showed lamotrigine could ameliorate executive dysfunction and brain inflammatory response in the mouse model of AD[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00206778 Mixed Mania Bipolar Disorder Phase 2 Completed - United States, New York ... 展开 >> Beth Israel Medical Center New York, New York, United States, 10003 收起 <<
NCT00104416 Epilepsy, Tonic-Clonic Phase 3 Completed - -
NCT02283801 Epilepsy Phase 1 Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.90mL

0.78mL

0.39mL

19.52mL

3.90mL

1.95mL

39.05mL

7.81mL

3.90mL
参考文献

[1]Goa KL, Ross SR, et al. Lamotrigine. A review of its pharmacological properties and clinical efficacy in epilepsy. Drugs. 1993 Jul;46(1):152-76.

[2]Leach MJ, Marden CM, et al. Pharmacological studies on lamotrigine, a novel potential antiepileptic drug: II. Neurochemical studies on the mechanism of action. Epilepsia. 1986 Sep-Oct;27(5):490-7.

[3] Lovrić M, Čajić I, Petelin Gadže Ž, Klarica Domjanović I, Božina N. Effect of antiepileptic drug comedication on lamotrigine concentrations. Croat Med J. 2018 Feb 28;59(1):13-19.

[4]Kim KJ, Jeun SH, Sung KW. Lamotrigine, an antiepileptic drug, inhibits 5-HT3 receptor currents in NCB-20 neuroblastoma cells. Korean J Physiol Pharmacol. 2017 Mar;21(2):169-177.

[5]Jun IG, Kim SH, Yoon YI, Park JY. Intrathecal lamotrigine attenuates antinociceptive morphine tolerance and suppresses spinal glial cell activation in morphine-tolerant rats. J Korean Med Sci. 2013 Feb;28(2):300-7.

[6]Wang K, Fernandez-Escobar A, Han S, Zhu P, Wang JH, Sun Y. Lamotrigine Reduces Inflammatory Response and Ameliorates Executive Function Deterioration in an Alzheimer's-Like Mouse Model. Biomed Res Int. 2016;2016:7810196