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Lamotrigine Sodium Channel inhibitor

Cat.No.S3024

Lamotrigine (BW-430C,LTG) 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 this compound also is a sodium channel blocker.
Lamotrigine Sodium Channel inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 256.09

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Quality Control

Batch: S302401 DMSO]10 mg/mL]false]Ethanol]3 mg/mL]false]Water]Insoluble]false Purity: 99.76%
99.76

Solubility

In vitro
Batch:

DMSO : 10 mg/mL (39.04 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 256.09 Formula

C9H7Cl2N5

 Storage (From the date of receipt)
CAS No. 84057-84-1 Download SDF Storage of Stock Solutions

Synonyms BW-430C,LTG SMILES C1=CC(=C(C(=C1)Cl)Cl)C2=C(N=C(N=N2)N)N

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Mechanism of Action

Targets/IC50/Ki
Sodium channel
5-HT (human platelets)
240 μM
5-HT (rat brain synaptosomes)
474 μM
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. In rat cerebral cortex tissue incubated with veratrine 10 mg/L, this compound 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 . This chemical inhibits high-frequency sustained repetitive firing of sodium-dependent action potentials, indicating a direct effect on voltage-activated sodium channels. It 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 this compound administration and persist for more than 24 hours. This chemical 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 this compound in rats at intravenous doses >5 mg/kg.

References
  • [4] https://pubmed.ncbi.nlm.nih.gov/3757935/
  • [5] https://pubmed.ncbi.nlm.nih.gov/2492222/
  • [6] http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=d7e3572d-56fe-4727-2bb4-013ccca22678#nlm34090-1

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-08-25)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06929273 RECRUITING
Bipolar Disorder Type I With Mania
Bristol-Myers Squibb
 2025-07-18 PHASE3
NCT06184581 RECRUITING
Bipolar II Disorder
University Hospital Bispebjerg and Frederiksberg
 2024-05-08 PHASE4
NCT07140913 RECRUITING
Mania; Bipolar Disorder
Bristol-Myers Squibb
 2025-10-08 PHASE3
NCT06729970 COMPLETED
Healthy Volunteers
Karuna Therapeutics, Inc., a Bristol Myers Squibb company
 2024-12-26 PHASE1
NCT05881928 UNKNOWN
Epilepsy; Lamotrigine; Sodium Valproate Adverse Reaction
Assiut University
 2024-07-29 PHASE4
NCT05420350 UNKNOWN
Meniere Disease; Ménière's Vertigo; Vertigo, Intermittent; Vertigo, Aural
Dent Neuroscience Research Center
 2020-12-16 PHASE2

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