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Lamotrigine-d3 is the deuterium labeled Lamotrigine[1]. 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[2][3]. | [Biological Activity]
Lamotrigine-d3 is intended for use as an internal standard for the quantification of lamotrigine by GC- or LC-MS. Lamotrigine is an anticonvulsant.1 It inhibits voltage-gated sodium channels (Nav) in HEK293 cells expressing recombinant human Nav1.2, Nav1.5, or Nav1.8 (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 and P-type calcium channel blocker ω-agatoxin IVA .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. | [References]
1.Drizin, I., Gregg, R.J., Scanio, M.J., et al.Discovery of potent furan piperazine sodium channel blockers for treatment of neuropathic painBioorg. Med. Chem.16(12)6379-6386(2008)
2.Stefani, A., Spadoni, F., Siniscalchi, A., et al.Lamotrigine inhibits Ca2+ currents in cortical neurons: Functional implicationsEur. 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 ratsEpilepsia27(5)483-489(1986)
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