Topiramate  (Synonyms: McN 4853; RWJ 17021)

Topiramate (McN 4853) is a broad-spectrum antiepileptic agent. Topiramate is a GluR5 receptor antagonist. Topiramate produces its antiepileptic effects through enhancement of GABAergic activity, inhibition of kainate/AMPA receptors, inhibition of voltage-sensitive sodium and calcium channels, increases in potassium conductance, and inhibition of carbonic anhydrase^[1][2][3].

GluR5 receptor^[1]; GABAergic^[2]; Kainate/AMPA^[2]; Sodium channel^[2]; Calcium channel^[2]; Potassium channel^[2]; Carbonic anhydrase^[2]

Topiramate has been believed to be a type of antiepileptic drug that blocks spread of seizures. Thus far, the mechanisms of its actions have been proven to include use-dependent inhibition of voltage-dependent Na+ channels in neurons, potentiation of GABA (γ-amino-butyric acid)-induced Cl- influx, and inhibitory effects on inward currents by antagonizing kainate/alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptors^[2].

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

339.36

Solid

C₁₂H₂₁NO₈S

97240-79-4

NS(OC[C@]1(OC(C)(C)O2)[C@@H]2[C@H](OC(C)(C)O3)[C@H]3CO1)(=O)=O

Room temperature in continental US; may vary elsewhere.

• [1]. Kaminski RM, et al. Topiramate selectively protects against seizures induced by ATPA, a GluR5 kainate receptor agonist. Neuropharmacology. 2004 Jun;46(8):1097-104.  [Content Brief]

  [2]. Lyseng-Williamson KA, et al. Topiramate: a review of its use in the treatment of epilepsy. Drugs. 2007;67(15):2231-56.  [Content Brief]

  [3]. Nakamura J, et al. Target pharmacology of topiramate, a new antiepileptic drug. Nihon Yakurigaku Zasshi. 2000 Jan;115(1):53-7.  [Content Brief]