Lamotrigine-¹³C₂,¹⁵N₂,d₃  (Synonyms: LTG-13C2,15N2,d3; BW430C-13C2,15N2,d3)

Lamotrigine-¹³C₂,¹⁵N₂,d₃ is ¹⁵N and deuterated labeled Lamotrigine (HY-B0495). Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na⁺ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy,?focal seizure, et al^[1][2].

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1].
Lamotrigine inhibits Veratrine evoked release of glutamate and aspartate with ED₅₀ values of 21 μM for both amino acids, but Lamotrigine is less potent in the inhibition of GABA release (ED₅₀=44 μM. At concentrations up to 300 μM, LTG has no effect on patassium-evoked amino acid^[2].
? Lamotrigine is some five times less potent in the inhibition of Veratrine-evoked [³H]acetylcholine release (ED₅₀=100 μM) than in glutamate or aspartate release^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Lamotrigine (IP, 30 min before pentylenetetrazol; 10 mg/kg, 15 mg/kg or 20 mg/kg) decreases the seizure intensity?at the higher doses, it increases the latency to the first pentylenetetrazol-induced seizure?in all studied doses compared with the controls^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

264.09

C₇¹³C₂H₅D₃Cl₂N₃¹⁵N₂

N[13CH]1N=[13C](N)C(C2=C(Cl)C(Cl)=C([2H])C([2H])=C2[2H])=[15N][15N]1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.  [Content Brief]

  [2]. M J Leach, et al. Pharmacological studies on lamotrigine, a novel potential antiepileptic drug: II. Neurochemical studies on the mechanism of action. Epilepsia. Sep-Oct 1986;27(5):490-7.  [Content Brief]

  [3]. Damianka P Getova, et al. A study of the effects of lamotrigine on mice using two convulsive tests. Folia Med (Plovdiv). Apr-Jun 2011;53(2):57-62.  [Content Brief]