Catalog No.S3024

Lamotrigine 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.

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Lamotrigine Chemical Structure

Lamotrigine Chemical Structure
Molecular Weight: 256.09

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Quality Control & MSDS

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Product Description

Biological Activity

Description Lamotrigine 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.
In vitro Lamotrigine stabilises presynaptic neuronal membranes by blockade of voltage-dependent sodium channels, thus preventing the release of excitatory neurotransmitters, particularly glutamate and aspartate. [1] 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 . [2]Lamotrigine inhibits high-frequency sustained repetitive firing of sodium-dependent action potentials, indicating a direct effect on voltage-activated sodium channels. [3] 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. [4]
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. [4] 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. [5]

Protocol(Only for Reference)

Kinase Assay: [3]

Electrophysiology In electrophysiological experiments, neurons bathed in control medium responds to 500-ms depolarizing pulses with trains of action potentials termed sustained repetitive firing (SRF). Increasing the magnitude of depolarization results in an increased number and frequency of action potentials. Typically a depolarizing current step of l-l.5 nA is sufficient to evoke SRF. To test the anticonvulsant effect, the blocking of SRF throughout the depolarizing current pulse is analyzed.

Animal Study: [3]

Animal Models Dog/Rat
Dosages 4.5 and 11.7 mg /kg in dogs and rats, respectively
Administration i.v.
Solubility 0.5% methylcellulose, 30 mg/mL


Chemical Information

Download Lamotrigine SDF
Molecular Weight (MW) 256.09


CAS No. 84057-84-1
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Syonnyms N/A
Solubility (25°C) * In vitro DMSO 10 mg/mL (39 mM)
Water <1 mg/mL (<1 mM)
Ethanol 3 mg/mL (11 mM)
In vivo 0.5% methylcellulose, 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 6-(2,3-dichlorophenyl)-1,2,4-triazine-3,5-diamine

Preparing Stock Solutions

Stock Solution (1ml DMSO) 1mM 10mM 20mM 30mM
Mass(mg) 0.25609 2.5609 5.1218 7.6827

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