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Lamotrigine

Catalog No. T0680   CAS 84057-84-1
Synonyms: LTG, BW430C

Lamotrigine (BW430C) is an Anti-epileptic Agent and Mood Stabilizer. The physiologic effect of lamotrigine is by means of Decreased Central Nervous System Disorganized Electrical Activity.

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Lamotrigine Chemical Structure
Lamotrigine, CAS 84057-84-1
Pack Size Availability Price/USD Quantity
200 mg In stock $ 31.00
500 mg In stock $ 46.00
1 g In stock $ 72.00
5 g In stock $ 271.00
1 mL * 10 mM (in DMSO) In stock $ 48.00
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Purity: 99.91%
Purity: 99.76%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Lamotrigine (BW430C) is an Anti-epileptic Agent and Mood Stabilizer. The physiologic effect of lamotrigine is by means of Decreased Central Nervous System Disorganized Electrical Activity.
Targets&IC50 5-HT (human platelets):240 μM, 5-HT (rat brain synaptosomes):474 μM
In vitro Lamotrigine is active in electrically induced EEG after-discharge tests, indicating its ability to counteract simple and complex partial seizures. It demonstrates antiepileptic effects in mice and rats, preventing hind-limb extension induced by both MES (maximal electroshock) and pentylenetetrazole. The peak effects of Lamotrigine occur 1 hour post-administration, with a duration exceeding 24 hours. Intravenous administration of Lamotrigine at doses greater than 5 mg/kg in rats results in a dose-dependent reduction in after-discharge duration.
In vivo In rat cortical brain tissues cultured with 10 mg/L veratridine, Lamotrigine inhibited the release of glutamate and aspartate (both with an ED50 of 5.38 mg/L) twice as effectively as it inhibited the release of GABA (ED50 of 11.2 mg/L), without affecting the basal release of glutamate. Lamotrigine stabilizes presynaptic neuronal membranes by blocking voltage-dependent sodium channels, thereby preventing the release of excitatory neurotransmitters, especially glutamate and aspartate. It does not induce phencyclidine (PCP)-like central nervous system effects, does not act through direct inhibition of NMDA receptors, and may avoid the adverse effects associated with NMDA blockade.
Kinase Assay Whole Cell [3H]R1881 Binding Assay: Fibroblasts are grown to confluence in five or six 150 cm2 tissue culture flasks for routine assay. This usually requires 4-6 weeks from the time of the initial seeding of the cell line. All studies are performed between passages 3-20. Two days before assay, the medium is changed to one lacking fetal calf serum. This is repeated again 24 hours before assay. Competition assays are performed with 0.5-1.0 nM [3H]R1881 and increasing amounts of the nonradioactive compounds. Binding to low affinity sites is determined in the presence of 5 × 10-7 M R1881 and is subtracted from whole cell binding of [3H]R 1881 obtained in the absence of any inhibitor to assess binding to 5 high affinity site
Synonyms LTG, BW430C
Molecular Weight 256.09
Formula C9H7Cl2N5
CAS No. 84057-84-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 25.6 mg/mL (100 mM)

Ethanol: 2.6 mg/mL (10 mM)

TargetMolReferences and Literature

1. Goa KL, et al. Drugs, 1993, 46(1), 152-176. 2. Leach MJ, et al. Epilepsia, 1986, 27(5), 490-497. 3. Cheung H, et al. Epilepsy Res, 1992, 13(2), 107-112. 4. Miller AA, et al. Epilepsia, 1986, 27(5), 483-489. 5. Wheatley PL, et al. Epilepsia, 1989, 30(1), 34-40.

TargetMolCitations

1. Lipecki Y, Haen E. Simultaneous Quantification of 11 Antiseizure Medications and Metabolites in Serum for Therapeutic Drug Monitoring Using High-Performance Liquid Chromatography with Ultraviolet Detection: A Short Communication. Therapeutic Drug Monitoring. 2022, 44(2): 345-350. 2. Weigel B, Tegethoff J F, Grieder S D, et al.MYT1L haploinsufficiency in human neurons and mice causes autism-associated phenotypes that can be reversed by genetic and pharmacologic intervention.Molecular Psychiatry.2023: 1-14.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Neurodegenerative Disease Compound Library GPCR Compound Library Anti-Cancer Drug Library Inhibitor Library Anti-Cancer Approved Drug Library Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Anti-Alzheimer's Disease Compound Library Orally Active Compound Library Endoplasmic Reticulum Stress Compound Library

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Keywords

Lamotrigine 84057-84-1 Autophagy GPCR/G Protein Membrane transporter/Ion channel Neuroscience Sodium Channel 5-HT Receptor Lennox-Gastaut syndrome tonic-clonic seizure Na+ channels epilepsy inhibit seizure Na channels LTG BW430C focal seizure Inhibitor inhibitor

 

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