Home Transmembrane Transporters Sodium Channel inhibitor - 5-HT Receptor inhibitor Lamotrigine For research use only.

Lamotrigine

Synonyms: BW-430C,LTG

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 also is a sodium channel blocker.

Lamotrigine Chemical Structure

Lamotrigine Chemical Structure

CAS: 84057-84-1

Selleck's Lamotrigine has been cited by 11 publications

Purity & Quality Control

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

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Biological Activity

Description 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 also is a sodium channel blocker.
Targets
Sodium channel [1] 5-HT (human platelets) [1] 5-HT (rat brain synaptosomes) [1]
240 μM 474 μM
In vitro
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 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]
Animal Research Animal Models Dog/Rat
Dosages 4.5 and 11.7 mg /kg in dogs and rats, respectively
Administration i.v.
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

Chemical lnformation & Solubility

Molecular Weight 256.09 Formula

C9H7Cl2N5
CAS No. 84057-84-1 SDF Download Lamotrigine SDF
Smiles C1=CC(=C(C(=C1)Cl)Cl)C2=C(N=C(N=N2)N)N
Storage (From the date of receipt)

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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