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Biochem/physiol Actions
Lacosamide is an orally active anticonvulsant that blocks voltage-gated sodium channels (VGSCs) selectively in their inactivated state (IC50 = 16 μM/Nav1.8, 182 μM/Nav1.7, 415 μM/Nav1.3) over resting state by enhancing slow inactivation. In addition to in vivo anticonvulsant activity (ED50 = 4.5 mg/kg in mice via i.p., 3.9 mg/kg in rats via p.o. by maximal electroshock seizure test), lacosamide also shows therapeutic efficacy in various pain models (10-30 mg/kg in rats via i.p.).
Orally active anticonvulsant that blocks voltage-gated sodium channels (VGSCs) selectively in inactivated over resting state by enhancing slow inactivation.
| Quality Level | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| optical activity | [α]/D 13 to 18° (C=0.5g/100mL, MeOH) |
| drug control | USDEA Schedule V |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | 2-8°C |
| SMILES string | N([C@H](COC)C(=O)NCc1ccccc1)C(=O)C |
| InChI | 1S/C13H18N2O3/c1-10(16)15-12(9-18-2)13(17)14-8-11-6-4-3-5-7-11/h3-7,12H,8-9H2,1-2H3,(H,14,17)(H,15,16)/t12-/m1/s1 |
| InChI key | VPPJLAIAVCUEMN-GFCCVEGCSA-N |
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