Lamotrigine

Catalog No.S3024 1 Product Citations

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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Lamotrigine Chemical Structure

Lamotrigine Chemical Structure
Molecular Weight: 256.09

Validation & Quality Control

Quality Control & MSDS

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Product Description

Biological Activity

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.
Targets Sodium channel [1]
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 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]
Features

Protocol(Only for Reference)

Kinase Assay: [3]

Electrophysiology In electrophysiological experiments, neurons bathed in control medium responds to 500-ms depolarizing pulses with trains of action potentials termed sustained repetitive firing (SRF). Increasing the magnitude of depolarization results in an increased number and frequency of action potentials. Typically a depolarizing current step of l-l.5 nA is sufficient to evoke SRF. To test the anticonvulsant effect, the blocking of SRF throughout the depolarizing current pulse is analyzed.

Animal Study: [3]

Animal Models Dog/Rat
Formulation suspended in 0.25% methylcellulose solution
Dosages 4.5 and 11.7 mg /kg in dogs and rats, respectively
Administration i.v.
Solubility 0.5% methylcellulose, 30 mg/mL
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.80.40.150.080.02
Body Surface Area (m2)0.60.50.240.150.050.0250.020.007
Km factor202012128653
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Goa KL, et al. Drugs, 1993, 46(1), 152-176.

[2] Leach MJ, et al. Epilepsia, 1986, 27(5), 490-497.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2014-10-16)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02256124 Recruiting Neurofibromatosis Type 1 Erasmus Medical Center|Universitaire Ziekenhuizen Leuven|  ...more Erasmus Medical Center|Universitaire Ziekenhuizen Leuven|ZonMw, Netherlands Organisation for Health Research and Development September 2014 Phase 2|Phase 3
NCT02158585 Not yet recruiting Menieres Disease|Ménières Vertigo|Vertigo, Intermittent|Vertigo, Aural Dent Neuroscience Research Center|University at Buffalo|B  ...more Dent Neuroscience Research Center|University at Buffalo|Buffalo ENT Specialists, LLP June 2014 Phase 3
NCT02081287 Not yet recruiting Bipolar Disorder|Manic Depression San Diego Veterans Healthcare System|The Depressive and B  ...more San Diego Veterans Healthcare System|The Depressive and Bipolar Disorder Alternative Treatment Foundation May 2014 Phase 1
NCT02100644 Recruiting Epilepsy GlaxoSmithKline April 2014 Phase 4
NCT02064465 Completed Epilepsy GlaxoSmithKline March 2014 Phase 1

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Chemical Information

Download Lamotrigine SDF
Molecular Weight (MW) 256.09
Formula

C9H7Cl2N5

CAS No. 84057-84-1
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Synonyms
Solubility (25°C) * In vitro DMSO 10 mg/mL (39 mM)
Water <1 mg/mL (<1 mM)
Ethanol 3 mg/mL (11 mM)
In vivo 0.5% methylcellulose 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 6-(2,3-dichlorophenyl)-1,2,4-triazine-3,5-diamine

Research Area

Product Citations (1)

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