Home Transmembrane Transporters Sodium Channel inhibitor - 5-HT Receptor inhibitor Lamotrigine

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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

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

Solubility

In vitro
Batch:

DMSO : 10 mg/mL ( (39.04 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble

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In vivo
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Mechanism of Action

Targets/IC50/Ki
Sodium channel [1]
5-HT (human platelets) [1]
240 μM
5-HT (rat brain synaptosomes) [1]
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. [1] 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 . [2]This chemical inhibits high-frequency sustained repetitive firing of sodium-dependent action potentials, indicating a direct effect on voltage-activated sodium channels. [3] 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. [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 this compound administration and persist for more than 24 hours. [4] 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. [5]
References
  • https://pubmed.ncbi.nlm.nih.gov/3757935/
  • https://pubmed.ncbi.nlm.nih.gov/2492222/
  • 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 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06049095 Recruiting
Healthy
Latigo Biotherapeutics
 October 17 2023 Phase 1
NCT05420350 Recruiting
Meniere Disease|Ménière''s Vertigo|Vertigo Intermittent|Vertigo Aural
Dent Neuroscience Research Center|Cures Within Reach|Dent Family Foundation
 December 16 2020 Phase 2

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