Catalog No.S3024 Synonyms: BW-430C
Molecular Weight(MW): 256.09
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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|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.|
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, 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 . Lamotrigine inhibits high-frequency sustained repetitive firing of sodium-dependent action potentials, indicating a direct effect on voltage-activated sodium channels.  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. 
|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.  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. |
|In vitro||DMSO||10 mg/mL (39.04 mM)|
|Ethanol||3 mg/mL (11.71 mM)|
|In vivo||0.5% methylcellulose||30 mg/mL|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02821338||Recruiting||Healthy||Food and Drug Administration (FDA)|Vince & Associates Clinical Research, Inc.|Algorithme Pharma Inc||June 2016||Phase 4|
|NCT02707965||Not yet recruiting||Epilepsy||Food and Drug Administration (FDA)|University of Maryland||March 2016||--|
|NCT02513654||Completed||Bipolar Disorder||GlaxoSmithKline||September 2015||Phase 1|
|NCT02556060||Recruiting||Addiction||Taipei City Hospital|Chang Gung Memorial Hospital||September 2015||Phase 2|Phase 3|
|NCT02708849||Active, not recruiting||Mental Disorders||Yale University||June 2015||Phase 1|
|NCT02428439||Recruiting||Depression|Suicidal Ideation||Asan Medical Center||April 2015||--|
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