Lamotrigine-¹³C₂,¹⁵N₂,d₃  (Synonyms: 拉莫三嗪-¹³C₂; LTG-13C2,15N2,d3; BW430C-13C2,15N2,d3)

Lamotrigine-¹³C₂,¹⁵N₂,d₃ is ¹⁵N and deuterated labeled Lamotrigine (HY-B0495). Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na⁺ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy, focal seizure, et al^[1][2].

氢、碳和其他元素的稳定重同位素已被纳入药物分子中，主要作为药物开发过程中定量的示踪剂。氘化引起了人们的关注，因为它可能影响药物的药代动力学和代谢谱^[1]。
Lamotrigine 抑制藜芦碱引起的谷氨酸和天冬氨酸释放，两种氨基酸的 ED₅₀ 值为 21 μM，但 Lamotrigine 抑制 GABA 释放的效力较低 (ED₅₀= 44 μM。在浓度高达 300 μM 时，LTG 对钾诱发的氨基酸没有影响^[2]。
Lamotrigine 抑制藜芦碱诱发的氨基酸的效力大约低五倍[³H]乙酰胆碱释放 (ED₅₀=100 μM) 低于谷氨酸或天冬氨酸释放^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Lamotrigine（腹腔注射，在戊四氮前 30 分钟；10 mg/kg、15 mg/kg 或 20 mg/kg）会降低较高剂量下的癫痫发作强度，与对照组相比，在所有研究剂量中 Lamotrigine 都会增加首次戊四氮诱发癫痫发作的潜伏期^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

264.09

C₇¹³C₂H₅D₃Cl₂N₃¹⁵N₂

84057-84-1

拉莫三嗪-¹³C₂；那蒙特金-¹³C₂

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.  [Content Brief]

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

  [3]. Damianka P Getova, et al. A study of the effects of lamotrigine on mice using two convulsive tests. Folia Med (Plovdiv). Apr-Jun 2011;53(2):57-62.  [Content Brief]