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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 (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.
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