Lamotrigine-d₃

Lamotrigine-d₃ is intended for use as an internal standard for the quantification of lamotrigine (Item No. 15428) by GC- or LC-MS. Lamotrigine is an anticonvulsant.¹ It inhibits voltage-gated sodium channels (Na_v) in HEK293 cells expressing recombinant human Na_v1.2, Na_v1.5, or Na_v1.8 (IC₅₀s = 10, 62, and 96 μM, respectively), as well as high voltage-activated calcium currents in isolated rat cortical neurons (IC₅₀ = 12.3 µM), an effect that can be reversed by the N-type calcium channel blocker ω-conotoxin GVIA (Item No. 24114) and P-type calcium channel blocker ω-agatoxin IVA (Item No. 21605).^1,2 Lamotrigine protects against seizures induced by maximal electroshock (MES) in mice and rats (ED₅₀s = 10.1 and 7.4 µmol/kg, respectively).³ It also decreases mechanical allodynia in a rat model of neuropathic pain induced by spinal nerve ligation (ED₅₀ = 47 µmol/kg).¹ Formulations containing lamotrigine have been used in the treatment of epilepsy and bipolar disorder.

WARNING This product is not for human or veterinary use.

1. Drizin, I., Gregg, R.J., Scanio, M.J., et al. Discovery of potent furan piperazine sodium channel blockers for treatment of neuropathic pain. Bioorg. Med. Chem. 16(12), 6379-6386 (2008).

2. Stefani, A., Spadoni, F., Siniscalchi, A., et al. Lamotrigine inhibits Ca²⁺ currents in cortical neurons: Functional implications. Eur. J. Pharmacol. 307(1), 113-116 (1996).

3. Miller, A.A., Wheatley, P., Sawyer, D.A., et al. Pharmacological studies on lamotrigine, a novel potential antiepileptic drug: I. Anticonvulsant profile in mice and rats. Epilepsia 27(5), 483-489 (1986).